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T18588
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Propargyl-PEG5-Ms
Propargyl-PEG6-Ms
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Others;
PROTAC Linker |
Others;
PROTAC |
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Propargyl-PEG5-Ms (Propargyl-PEG6-Ms) 是一种属于 PEG 类的 PROTAC linker，可用于 PROTAC 分子的合成。 |
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T9146
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ms48107
Benzenemethanol, 2-[4-amino-6-[[(4-phenoxyphenyl)methyl]amino]-1,3,5-triazin-2-yl]-3-fluoro-
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Others |
Others |
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MS48107 是 G 蛋白偶联受体 68 (GPR68) 的选择性正变构调节剂，对GPR68的选择性高于密切相关的神经递质转运蛋白，质子 GPCR 和 hERG 离子通道。它可以穿越过小鼠的血脑屏障。 |
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T14541
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Benzyl-PEG5-Ms
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Others |
Others |
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Benzyl-PEG5-Ms is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells. |
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T15894
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m-PEG5-Ms
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Others |
Others |
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m-PEG5-Ms is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1]. |
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T17650
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Boc-N-Amido-PEG5-Ms
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Others |
Others |
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Boc-N-Amido-PEG5-Ms is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells. |
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T6923
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Ozanimod
奥扎莫德,RPC-1063
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S1P Receptor;
LPL Receptor |
GPCR/G Protein |
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Ozanimod (RPC-1063) 是一种选择性S1P1和S1P5受体激动剂，在[35S]-GTPγS 结合实验中，EC50分别为 410 pM 和 11 nM。它可研究治疗克罗恩病、溃疡性结肠炎、多发性硬化症和复发性多发性硬化症的试验。 |
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T16150
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Ms-PEG5-t-butyl ester
Ms-PEG4-t-butyl ester
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Others |
Others |
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Ms-PEG5-t-butyl ester is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells. |
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T23029
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MS 245 oxalate
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Others |
Others |
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MS 245 oxalate is a 5-HT6 antagonist. |
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T62732
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S1P1 agonist 5
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S1P1 agonist 5 是一种选择性的、口服具有活力的 S1P1 激动剂。S1P1 agonist 5 可以抑制淋巴细胞从淋巴组织排出到外周血。S1P1 agonist 5 具有潜力进行多发性硬化症 (MS) 的研究。 |
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T36895
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5-Fluorouracil-13C,15N2
5-Fluorouracil-13C,15N2
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5-Fluorouracil-13C,15N2 is intended for use as an internal standard for the quantification of 5-flurouracil by GC- or LC-MS. 5-Fluorouracil is a pyrimidine analog that irreversibly inhibits thymidylate synthase, blocking the synthesis of thymidine which is required for DNA synthesis. Intracellular metabolites of 5-fluorouracil exert cytotoxic effects by either inhibiting thymidylate synthetase, or through incorporation into RNA and DNA, ultimately initiating apoptosis. |
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T41156
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MS 39
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MS 39是突变型表皮生长因子受体(EGFR)的高效、高亲和力和选择性降解剂，具有的高效、高亲和力和选择性。MS 39 由吉非替尼通过连接物偶联至 VHL 配体，能有效地诱导突变型 EGFR 的降解（在 HCC827(外显子19 del)和 H3255 (L858R 突变)肺癌细胞系中的 DC50值分别为5 nM 和3.3 nM)，但在浓度高达10 μM 的野生型 EGFR 细胞系中无显著作用。MS 39在体外抑制 H3255肺癌细胞的增殖，并且在给药后在小鼠中具有生物利用性。 |
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T38037
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Caffeic Acid-13C3
Caffeic Acid-13C3
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Caffeic acid-13C3 is an isotopically enriched form of caffeic acid that is intended for use as an internal standard for the quantification of caffeic acid by GC- or LC-MS. Caffeic acid is an inhibitor of 5-LO , with IC50 values of 3.7-72 μM, and 12-LO, with IC50 values of 5.1-30 μM. |
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T71211
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Rizatriptan-d6 benzoate salt
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Rizatriptan-d6 is intended for use as an internal standard for the quantification of rizatriptan by GC- or LC-MS. Rizatriptan is an agonist of the serotonin
receptor subtypes 5-HT1B and 5-HT1D. It is selective for 5-HT1B and 5-HT1D receptors over 5-HT1A receptors. Rizatriptan induces vasoconstriction in isolated human middle meningeal arteries. In vivo, rizatriptan reduces head grooming, the number of oculotemporal strokes, eye blinking, and one-eye closures in a Cacna1a mutant transgenic mou... |
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T71893
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Clobetasol Propionate-d5
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Clobetasol propionate-d5 is intended for use as an internal standard for the quantification of clobetasol propionate by GC- or LC-MS. Clobetasol propionate is a corticosteroid. It binds to glucocorticoid receptors in a cell-free assay and inhibits proliferation of primary human skin fibroblasts when used at a concentration of 5 µg/ml. Topical administration of clobetasol propionate reduces croton oil-induced ear edema in mice. Formulations containing clobetasol propionate have been used in the t... |
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T36556
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(±)5(6)-DiHET lactone
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5,6-DiHET lactone is a lactonized form of 5,6-EET and 5,6-DiHET. In solution, 5(6)-EET degrades into 5(6)-DiHET and 5(6)-δ-lactone, which can be converted to 5(6)-DiHET and quantified by GC-MS. 5,6-DiHET potently induces vasodilation of isolated canine coronary arterioles, with 41 and 100% inhibition occurring at 0.01 and 100 pM, respectively. It also induces vasodilation in isolated human microvessels and increases intracellular calcium levels in a dose-dependent manner, an effect that can be b... |
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T35513
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13C15-Nivalenol
13C15-Nivalenol
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13C15-Nivalenol is intended for use as an internal standard for the quantification of nivalenol by GC- or LC-MS. Nivalenol is a trichothecene mycotoxin that has been found inFusarium.1It is lethal to mice (LD50= 6.9 mg/kg).2Nivalenol (5, 10, and 15 mg/kg) also induces thymic, splenic, and Peyer's patch cell apoptosis in mice.3
1.Yang, Z., Concannon, J., Ng, K.S., et al.Tetrandrine identified in a small molecule screen to activate mesenchymal stem cells for enhanced immunomodulationSci. Rep.63026... |
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T71302
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Norfluoxetine-d5 HCl
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Norfluoxetine-d5 is intended for use as an internal standard for the quantification of norfluoxetine by GC- or LC-MS. Norfluoxetine is an active metabolite of the antidepressant fluoxetine. It is formed from fluoxetine by the cytochrome P450 (CYP) isoforms CYP2C9, CYP2C19, and CYP3A. Norfluoxetine inhibits serotonin (5-HT) uptake in rat brain synaptosomal membrane preparations (Ki = 44.7 nM) and isolated human platelets (IC50 = ~15 nM). It has been found in the tissues of fish exposed to wastewa... |
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T35718
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N-desmethyl Rosuvastatin (sodium salt hydrate)
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N-desmethyl Rosuvastatin is an active metabolite of the HMG-CoA reductase inhibitor rosuvastatin .1,2N-desmethyl Rosuvastatin is formed when rosuvastatin undergoes demethylation, primarily by the cytochrome P450 (CYP) isoform CYP2C9 and to a lesser extent by CYP2C19 and CYP3A4.1
1.Macwan, J.S., Ionita, I.A., and Akhlaghi, F.A simple assay for the simultaneous determination of rosuvastatin acid, rosuvastatin-5S-lactone, and N-desmethyl rosuvastatin in human plasma using liquid chromatography-tand... |
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T36070
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(±)5(6)-EET
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5(6)-EET is a fully racemic version of the enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes. In solution, 5(6)-EET degrades into 5,6-DiHET and 5(6)-δ-lactone, which can be converted to 5(6)-DiHET and quantified by GC-MS. In neuroendocrine cells, such as the anterior pituitary and pancreatic islets, 5(6)-EET has been implicated in the mobilization of calcium and hormone secretion. 5(6)-EET is an inhibitor of T-type voltage-gated calcium channels (Cav3) that inhib... |
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T71300
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Pentoxifylline-d6
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Pentoxifylline-d6 is intended for use as an internal standard for the quantification of pentoxifylline by GC- or LC-MS. Pentoxifylline is a hemorrheologic agent. It increases the deformability of washed isolated human erythrocytes when used at a concentration of 100 µM. Pentoxifylline (1, 2, and 3 mM) inhibits ADP-induced platelet aggregation in isolated human whole blood. It inhibits thrombus formation induced by ADP in a hamster cheek pouch model when administered at doses of 5, 10, and 20 mg/... |
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T36408
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Rhein-13C4
Rhein-13C4
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Rhein-13C4 is intended for use as an internal standard for the quantification of rhein by GC- or LC-MS. Rhein is an anti-inflammatory anthraquinone found in rhubarb and is the bioactive derivative of its prodrug diacerein . At 10 μM, rhein inhibits IL-1β signaling, suppressing signaling through NF-κB, and reduces the expression of the matrix metalloproteases MMP-1 and MMP-13.1 It inhibits IKKβ (IC50 = 11.8 μM), decreasing iNOS and IL-6 expression in LPS-stimulated macrophages but paradoxically i... |
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T36660
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Olsalazine-13C6
Olsalazine-13C6
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Olsalazine-13C6is intended for use as an internal standard for the quantification of olsalazine by GC- or LC-MS. Olsalazine is an orally bioavailable prodrug form of the anti-inflammatory agent 5-aminosalicylic acid that is cleaved by bacterial azo reductases in the gut to generate active 5-ASA.1In vitro, olsalazine increases ion transport in isolated rabbit distal ileum when applied to the luminal side (ED50= 0.3 mM) and stimulates fluid transport in rat jejunum when used at a concentration of ... |
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T70960
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Maprotiline-d3 hydrochloride
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Maprotiline-d3 is intended for use as an internal standard for the quantification of maprotiline by GC- or LC-MS. Maprotiline is a tricyclic antidepressant. It binds to the norepinephrine transporter (NET) and is selective for NET over the serotonin and dopamine transporters. Maprotiline also binds to the serotonin (5-HT) receptor subtype 5-HT2A, as well as histamine H1, muscarinic acetylcholine, α1-adrenergic, and dopamine D2 receptors. In vivo, maprotiline inhibits norepinephrine reuptake in r... |
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T71981
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Gliclazide-d4
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Gliclazide-d4 is intended for use as an internal standard for the quantification of gliclazide by GC- or LC-MS. Gliclazide is a sulfonylurea and an inhibitor of pancreatic β-cell ATP-sensitive potassium (KATP) channels. It is selective for pancreatic β-cell over cardiac and arterial smooth muscle cell KATP channels. Gliclazide (5 μM) increases insulin-induced glucose uptake and glucose transporter 4 (GLUT4) translocation to the plasma membrane in a differentiated 3T3L1 adipocyte model of insulin... |
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T35517
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4-deoxy Nivalenol-13C15
4-deoxy Nivalenol-13C15
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4-deoxy Nivalenol-13C15is intended for use as an internal standard for the quantification of 4-deoxy nivalenol by GC- or LC-MS. 4-deoxy Nivalenol is a trichothecene mycotoxin that has been found inFusarium.1It binds to eukaryotic ribosomes and inhibits protein synthesis in mice when administered at doses ranging from 5 to 25 mg/kg. 4-deoxy Nivalenol (0.1 and 0.2 mg/kg) induces emesis in pigs and decreases feed consumption in pigs when administered at a dose of 40 ppb in the diet.2It induces leth... |
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T35783
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Zearalenone-13C18
Zearalenone-13C18
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Zearalenone-13C18is intended for use as an internal standard for the quantification of zearalenone by GC- or LC-MS. Zearalenone is a mycotoxin that has been found inFusariumand has estrogenic activities.1It binds to human estrogen receptor α (ERα) and ERβ (IC50s = 9 and 5.8 nM, respectively).2Zearalenone induces precocious development of mammary tissues in young female pigs and prepucial enlargement in young male pigs.3Zearalenone (1.5-5 mg/kg of diet) induces hyperestrogenism in pigs. It also i... |
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T38118
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Zanamivir-13C,15N2
Zanamivir-13C,15N2
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Zanamivir-13C,15N2is intended for use as an internal standard for the quantification of zanamivir by GC- or LC-MS. Zanamivir is a sialic acid analog that inhibits neuraminidase release of newly replicated influenza virus particles.1It has been shown to selectively inhibit the growth of influenza A and B viruses in plaque reduction assays with IC50values ranging from 5 to 14 nM and to directly inhibit influenza A and B virus neuraminidases with IC50values ranging from 0.6 to 7.9 nMin vitro. Intra... |
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T35695
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Oleic Acid-13C
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Oleic acid-13C is intended for use as an internal standard for the quantification of oleic acid by GC- or LC-MS. Oleic acid is a monounsaturated fatty acid and a major component of membrane phospholipids that has been found in human plasma, cell membranes, and adipose tissue.1,2 It contributes approximately 17% of the total fatty acids esterified to phosphatidylcholine, the major phospholipid class in porcine platelets.1 Oleic acid inhibits collagen-stimulated platelet aggregation by approximate... |
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T71401
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Oxaliplatin-d10
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Oxaliplatin-d10 is intended for use as an internal standard for the quantification of oxaliplatin by GC- or LC-MS. Oxaliplatin is a platinum-containing DNA-crosslinking agent. It induces the formation of DNA inter- and intrastrand crosslinks and DNA-protein adducts, inhibits DNA and RNA synthesis, and induces apoptosis in cancer cells. Oxaliplatin is cytotoxic to cisplatin-sensitive A2780(1A9) and KB-3-1 cells and cisplatin-resistant A2780-E(80) and KB-CP20 cells (IC50s = 0.12, 0.39, 4.7, and 2.... |
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T71328
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Theobromine-d6
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Theobromine-d6 is intended for use as an internal standard for the quantification of theobromine by GC- or LC-MS. Theobromine is a methylxanthine alkaloid and derivative of caffeine that has been found in cocoa beans and has diverse biological activities. It is an adenosine A1 receptor antagonist. Theobromine increases AMPK phosphorylation and inhibits adipocyte differentiation, ERK and JNK phosphorylation, and IL-6 and TNF-α production in 3T3-L1 preadipocytes cultured in differentiation medium.... |
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T36844
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Inostamycin A
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Inostamycin A is a bacterial metabolite that has been found inStreptomycesand has anticancer activity.1It is an inhibitor of CDP-diacylglycerol:inositol 3-phosphatidyltransferase (IC50= 0.02 μg/ml in A431 cell membranes) and is selective for CDP-diacylglycerol:inositol 3-phosphatidyltransferase over phospholipase C (PLC) and phosphatidylinositol kinase at 10 μg/ml.2Inostamycin A decreases viability of YCU-T892, KCC-TC873, KB, HSC-4, and YCU-T891 oral squamous cell carcinoma (OSCC) cells in a con... |
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T69966
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Roxadustat-d5
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Roxadustat-d5 is intended for use as an internal standard for the quantification of roxadustat by GC- or LC-MS. Roxadustat is an inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH; IC50s = 1.4, 1.26, and 1.32 µM for HIF-PH1, HIF-PH2, and HIF-PH3, respectively). It is selective for HIF-PH over other 2-oxoglutarate-dependent dioxygenases, including lysine-specific demethylase 5A (KDM5A), KDM5B, -5C, -5D, and -6B (IC50s = >100 µM for all). Roxadustat (10-200 µM) stabilizes HIF-1α and ... |
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T70313
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Indoxyl Sulfate-d5 potassium salt
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Indoxyl sulfate-d5 is intended for use as an internal standard for the quantification of indoxyl sulfate by GC- or LC-MS. Indoxyl sulfate is a uremic toxin and a metabolite of tryptophan. It is formed via sulfation of indole, an intermediate generated from tryptophan by intestinal bacteria, by the sulfotransferase (SULT) isoform 1A1 variant 2 (SULT1A1*2) in the liver. Indoxyl sulfate activates the aryl hydrocarbon receptor (AhR) in HepG2 40/6 hepatoma cells (EC50 = 12.1 nM in a reporter assay). ... |
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T35591
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Guanfacine-13C,15N3
Guanfacine-13C,15N3
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Guanfacine-13C,15N3is intended for us as an internal standard for the quantification of guanfacine by GC- or LC-MS. Guanfacine is an α2-adrenergic receptor (α2-AR) agonist with Kivalues of 93, 1,380, and 3,890 nM for α2A-, α2B-, and α2C-ARs, respectively, in a radioligand binding assay.1It has EC50values of 52, 288, and 602 nM for α2A-, α2B-, and α2C-ARs, respectively, for stimulated [35S]GTPγS binding. It also binds to imidazoline receptor 1 (Ki= 19 nM in a radioligand binding assay).2Guanfacin... |
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T35775
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HT-2 Toxin-13C22
HT-2 Toxin-13C22
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HT-2 toxin-13C22is intended for use as an internal standard for the quantification of HT-2 toxin by GC- or LC-MS. HT-2 toxin is a type A trichothecene mycotoxin and an active, deacetylated metabolite of the trichothecene mycotoxin T-2 toxin .1,2Like T-2 toxin, HT-2 toxin inhibits protein synthesis and cell proliferation in plants.2HT-2 toxin also reduces viability of HepG2, A549, HEp-2, Caco-2, A-204, U937, Jurkat, and RPMI-8226 cancer cells with IC50values ranging from 3.1 to 23 ng/ml and human... |
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T35789
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Palmitic acid-1-13C
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Palmitic acid-13C is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid is a 16-carbon saturated fatty acid. It comprises approximately 25% of human total plasma lipids.1 It increases protein levels of COX-2 in RAW 264.7 cells when used at a concentration of 75 μM.2 Palmitic acid is involved in the acylation of proteins to anchor membrane-bound proteins to the lipid bilayer.2,3,4,5,6
|1. Santos, M.J., López-Jurado, M., Llopis, J., et a... |
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T35683
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2-deoxy-D-Glucose-13C6
2-deoxy-D-Glucose-13C6
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2-deoxy-D-Glucose-13C6is intended for use as an internal standard for the quantification of 2-deoxy-D-glucose by GC- or LC-MS. 2-deoxy-D-Glucose is a glucose antimetabolite and an inhibitor of glycolysis.1,2It inhibits hexokinase, the enzyme that converts glucose to glucose-6-phosphate, as well as phosphoglucose isomerase, the enzyme that converts glucose-6-phosphate to fructose-6-phosphate.32-deoxy-D-Glucose (16 mM) induces apoptosis in SK-BR-3 cells, as well as inhibits the growth of 143B oste... |
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T36881
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NHC-diphosphate triammonium
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NHC-triphosphate triammonium is an active phosphorylated intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) as a triphosphate form[1]. NHC-triphosphate triammonium is a weak alternative substrate for the viral polymerase and can be incorporated into HCV replicon RNA[1][2].
In an intracellular metabolism assay, HCV replicon cells are treated with 10 μM 3H-labeled NHC, and intracellular nucleotide levels are determined after 1, 2 and 8 hours incubations. NHC is rapidly convered into the mono... |
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T35791
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Palmitic acid-13C
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Palmitic acid-13C is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid-13C contains 13C at the C2 position and has been used in the study of free fatty acid incorporation into phospholipid fatty acids in soil microbes.1 Palmitic acid is a 16-carbon saturated fatty acid. It comprises approximately 25% of human total plasma lipids.2 It increases protein levels of COX-2 in RAW 264.7 cells when used at a concentration of 75 μM.3 Palmitic ... |
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T38297
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Ribavirin-13C5
Ribavirin-13C5
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Ribavirin-13C5is intended for use as an internal standard for the quantification of ribavirin by GC- or LC-MS. Ribavirin is an antiviral guanosine nucleoside analog.1,2Upon entry into cells, ribavirin is metabolized to an active triphosphate form that induces viral RNA chain termination and inhibits viral polymerases. It reduces replication in a panel of seven RNA and four DNA viruses in Vero cells (EC50s = 2-95 μg/ml).3Ribavirin also reduces replication of severe acute respiratory syndrome coro... |
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T35929
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O-Demethyl Apremilast
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O-Demethyl apremilast is an active metabolite of the phosphodiesterase 4 (PDE4) inhibitor apremilast .1It inhibits the activity of PDE4 isolated from U937 cells and LPS-induced TNF-α production in isolated human peripheral blood mononuclear cells (PBMCs; IC50s = 8.3 and 5.6 μM, respectively). O-Demethyl apremilast is also an oxidative degradation product of apremilast.2,3
1.Hoffmann, M., Kumar, G., Schafer, P., et al.Disposition, metabolism and mass balance of [14C]apremilast following oral admi... |
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T36903
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Rasagiline-13C3 (mesylate)
Rasagiline-13C3 (mesylate)
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Rasagiline-13C3is intended for use as an internal standard for the quantification of rasagiline by GC- or LC-MS. Rasagiline is an inhibitor of monoamine oxidase B (MAO-B; IC50= 4.43 nM for the rat brain enzyme).1It is selective for MAO-B over MAO-A (IC50= 412 nM for the rat brain enzyme). It inhibits serum and NGF withdrawal-induced apoptosis of PC12 cells when used at concentrations ranging from 0.01 to 100 μM.2Rasagiline inhibits rat brain MAO-Bin vivo(ED50= 0.1 mg/kg).1It reduces cerebral ede... |
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T37847
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Zonisamide-13C2,15N
Zonisamide-13C2,15N
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Zonisamide-13C2,15N is intended for use as an internal standard for the quantification of zonisamide by GC- or LC-MS. Zonisamide is an antiepileptic agent.1 It selectively inhibits the repeated firing of sodium channels (IC50 = 2 μg/ml) in mouse embryo spinal cord neurons and inhibits spontaneous channel firing when used at concentrations greater than 10 μg/ml.2 In rat cerebral cortex neurons, zonisamide (1-1,000 μM) inhibits T-type calcium channels with a maximum reduction of 60% of the calcium... |
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