|
T5313
|
Sobetirome
IACS-010759,QRX-431
|
Thyroid hormone receptor(THR) |
Endocrinology/Hormones |
|
Sobetirome (IACS-010759) 是一种甲状腺激素受体 β (TRβ) 激动剂，能够选择性的结合到TRβ-1(EC50:0.16 μM)。 |
|
T40548
|
NH-3
|
Thyroid hormone receptor(THR) |
Endocrinology/Hormones |
|
NH-3是一种高效的口服活性甲状腺激素受体（THR）拮抗剂，具有可逆行为，其IC 50为55 nM。NH-3源自选择性甲状腺激素模拟物GC-1，有效地抑制甲状腺激素与相应受体的结合，从而阻碍辅因子的招募。 |
|
TP1267L
|
CEF27, Epstein-Barr Virus BRLF-1 lytic 148-156 acetate
CEF27, Epstein-Barr Virus BRLF-1 lytic 148-156 acetate(254110-79-7 free base)
|
Others |
Others |
|
CEF27, Epstein-Barr Virus BRLF-1 lytic 148-156 acetate(254110-79-7 free base) 对应于 BRLF1 的氨基酸 148-156。 BRLF1 是一种转录激活因子，可直接与一些 Epstein-Barr 病毒 (EBV) 裂解基因启动子中的富含 GC 的基序结合。 |
|
T78573
|
Glucocerebrosidase
GCase,Glucosylceramidase
|
Endogenous Metabolite |
Metabolism |
|
Glucocerebrosidase (Glucosylceramidase; GBA) 是溶酶体内的酶，负责催化GC中的β-糖苷键裂解，从而生成葡萄糖和神经酰胺。 |
|
T76274
|
Dolcanatide
|
|
|
|
Dolcanatide为一种对GC-C(鸟苷酸环化酶-C)具有口服活性的激动剂，展现出通便、抗痛及抗炎效果，适用于炎症性肠病研究。 |
|
T73940
|
S-Phenylmercapturic acid
|
|
|
|
S-Phenylmercapturic acid，苯的代谢物，作为生物标志物使用，可通过GC、HPLC（UV或荧光检测）、GC-MS、LC-MS/MS或免疫测定进行检测。 |
|
T83247
|
7-Deaza-dGTP tetralithium
|
|
|
|
7-Deaza-dGTP tetralithium可用于高效扩增富含GC序列的DNA。 |
|
T35515
|
3-Acetyldeoxy Nivalenol-13C17
3-Acetyldeoxy Nivalenol-13C17
|
|
|
|
3-Acetyldeoxy nivalenol-13C17is intended for use as an internal standard for the quantification of 3-acetyldeoxy nivalenol by GC- or LC-MS. 3-Acetyldeoxy nivalenol is a mycotoxin that has been found inF. graminearum.1In vivo, 3-acetyldeoxy nivalenol (40 mg/kg) induces duodenal and splenic cell necrosis, as well as lethality (LD50= 70 mg/kg) in mice.2
1.Jiao, F., Kawakami, A., and Nakajima, T.Effects of different carbon sources on trichothecene production and Tri gene expression by Fusarium grami... |
|
T78165
|
SPEN inhibitor 1
|
Others |
Others |
|
SPEN-IN-1（compound X1）是一种针对蛋白因子SPEN的抑制剂，其Kd值达47 nM。该化合物对于RepA显示出高度的选择性，RepA为Xist（非编码RNA原型）中包含431个核苷酸的结构域，由8.5个GC-rich基序构成，这些基序参与基因的沉默作用。 |
|
T37928
|
13C6 Glucosylsphingosine (d18:1)
|
|
|
|
13C6 Glucosylsphingosine (d18:1) is an isotopically enriched form of 1-β-D-glucosylsphingosine (d18:1) that is intended for use as an internal standard for the quantification of 1-β-D-glucosylsphingosine by GC- or LC-MS. 1-β-D-Glucosylsphingosine is a lysolipid derivative of glucosylcerebroside that decreases activity of glucocerebrosidase in LA-N-2 cells in a dose-dependent manner. |
|
T70035
|
Tasimelteon-d5
|
|
|
|
Tasimelteon-d5 is intended for use as an internal standard for the quantification of tasimelteon by GC- or LC-MS. Tasimelteon is a melatonin (MT) receptor agonist. It selectively binds MT1 and MT2 receptors over a panel of 160 additional receptors and enzymes at 10 µM. Tasimelteon inhibits forskolin-induced cAMP accumulation with EC50 values of 0.79 and 1 nM in NIH3T3 cells expressing the MT1 or MT2 receptor, respectively. Formulations containing tasimelteon have been used in the treatment of no... |
|
T36537
|
Nitrofurantoin-13C3
Nitrofurantoin-13C3
|
|
|
|
Nitrofurantoin-13C3is intended for use as an internal standard for the quantification of nitrofurantoin by GC- or LC-MS. Nitrofurantoin is a nitrofuran antibiotic.1In vivo, nitrofurantoin (25-100 mg/kg) reducesE. colireplication and abscess formation in the renal medulla of infected rats in a dose-dependent manner. It prevents kidney and bladder infection in rats following bladder inoculation with clinical isolates ofP. mirabilis. Nitrofurantoin also prevents alkalization of urine, as well as ca... |
|
T69193
|
SN-28049
|
|
|
|
SN-28049 SN is a DNA intercalating drug that binds selectively to GC-rich DNA and shows curative activity against the Colon 38 adenocarcinoma in mice. SN 28049 has a complex action that may involve poisoning of topo IIalpha, suppression of topo I and inhibition of gene transcription from promoters with SP-1 sites. These actions may contribute to the promising experimental solid tumour anticancer activity of SN 28049. |
|
T35519
|
Aflatoxin B2-13C17
Aflatoxin B2-13C17
|
|
|
|
Aflatoxin B2-13C17(AFB2-13C17) is intended for use as an internal standard for the quantification of AFB2by GC- or LC-MS. AFB2is a mycotoxin that has been found inA. terricola.1It induces hepatic autophagy and apoptosis in broiler chickens when administered at doses of 0.2, 0.4, and 0.8 mg/kg.2AFB2(0.5 and 1 mg/animal) also induces parenchymal cell hyperplasia in rats.3
1.Moubasher, A.H., el-Kady, I.A., and Shoriet, A.Toxigenic Aspergilli isolated from different sources in EgyptAnn. Nutr. Alimen... |
|
T36021
|
Flumequine-13C3
Flumequine-13C3
|
|
|
|
Flumequine-13C3is intended for use as an internal standard for the quantification of flumequine by GC- or LC-MS. Flumequine is a fluoroquinolone antibiotic.1It is active againstS. aureus, S. pyogenes, B. subtilis, E. coli, P. aeruginosa, S. faecalis, andK. pneumoniae(MICs = 1-100 μg/ml). Flumequine is also active against field isolates of B. hyodysenteriae (MICs = 6.25-200 μg/ml).2It inhibits DNA gyrase, disrupting supercoiling of bacterial DNA to block transcription and replication.3In vivo, fl... |
|
T35520
|
Aflatoxin G1-13C17
Aflatoxin G1-13C17
|
|
|
|
Aflatoxin G1-13C17is intended for use as an internal standard for the quantification of aflatoxin G1by GC- or LC-MS. Aflatoxin G1is a mycotoxin that has been found inA. terricola.1In vivo, aflatoxin G1is lethal to ducklings (LD50= 1.18 mg/kg).2It induces hepatocellular carcinoma tumor formation and lethality in rats when administered at doses of 1.4 and 3 mg/animal, respectively. Aflatoxin G1also inhibits liver and kidney succinate dehydrogenase and fumarase, as well as kidney cytochrome oxidase... |
|
T35521
|
Aflatoxin G2-13C17
Aflatoxin G2-13C17
|
|
|
|
Aflatoxin G2-13C17is intended for use as an internal standard for the quantification of aflatoxin G2by GC- or LC-MS. Aflatoxin G2is a mycotoxin that has been found inAspergillus.1It is lethal to ducklings (LD50= 2.83 mg/kg) but is non-toxic to rats when administered at a dose of 200 mg/kg.2
1.Bennett, J.W., and Klich, M.MycotoxinsClin. Microbiol. Rev.16(3)497-516(2003) 2.Wogan, G.N., Edwards, G.S., and Newberne, P.M.Structure-activity relationships in toxicity and carcinogenicity of aflatoxins a... |
|
T35513
|
13C15-Nivalenol
13C15-Nivalenol
|
|
|
|
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... |
|
T71285
|
Metaxalone-d6
|
|
|
|
Metaxalone-d6 is intended for use as an internal standard for the quantification of metaxalone by GC-or LC-MS. Metaxalone is a skeletal muscle relaxant. It inhibits the proliferation of, and induces apoptosis in, RAW 264.7 cells in vitro when used at concentrations ranging from 1 to 100 µM. Metaxalone also reduces LPS-induced increases in COX-1, COX-2, and NF-kB levels and inhibits LPS-induced production of TNF-α, IL-6, and prostaglandin E2 in RAW 264.7 cells. Formulations containing metaxalone ... |
|
T36384
|
DL-Tyrosine-13C9,15N
L-Tyrosine-13C9,15N
|
|
|
|
L-Tyrosine-13C9,15N is intended for use as an internal standard for the quantification of L-tyrosine by GC- or LC-MS. L-Tyrosine is a non-essential amino acid.1It is produced by hydroxylation of phenylalanine by phenylalanine hydroxylase but can also be obtained from dietary sources or degradation of endogenous proteins, resulting in L-tyrosine release.1,2L-Tyrosine is a precursor in the biosynthesis of catecholamine neurotransmitters, melanins, and thyroid hormones.3Plasma, skeletal muscle, and... |
|
T71206
|
Tiagabine-d6 hydrochloride
|
|
|
|
Tiagabine-d6 is intended for use as an internal standard for the quantification of tiagabine by GC- or LC-MS. Tiagabine is an inhibitor of GABA transporter 1. It inhibits seizures induced by DMCM in mice. Tiagabine reduces allodynia in a rodent model of neuropathic pain when used at a dose of 72.8 µmol/kg, and it acts synergistically with gabapentin to delay pain responses in mice in the hot plate test. Formulations containing tiagabine have been used as adjunctive therapies in the treatment of ... |
|
T37119
|
1,2,3-Trioctanoyl-rac-glycerol-13C3
1,2,3-Trioctanoyl-rac-glycerol-13C3
|
|
|
|
1,2,3-Trioctanoyl-rac-glycerol-13C3 is intended for use as an internal standard for the quantification of 1,2,3-trioctanoyl-rac-glycerol by GC- or LC-MS. 1,2,3-Trioctanoyl-rac-glycerol is a triacylglycerol that contains octanoic acid at the sn-1, sn-2, and sn-3 positions. Dietary administration of 1,2,3-trioctanoyl-rac-glycerol increases hippocampal levels of the glycolytic metabolites glucose 6-phosphate, fructose 6-phosphate, and β-hydroxybutyrate and the seizure threshold in the 6 Hz psychomo... |
|
T36408
|
Rhein-13C4
Rhein-13C4
|
|
|
|
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... |
|
T37044
|
1,2-Dioleoyl-rac-glycerol-13C3
1,2-Dioleoyl-rac-glycerol-13C3
|
|
|
|
1,2-Dioleoyl-rac-glycerol-13C3 is intended for use as an internal standard for the quantification of 1,2-dioleoyl-rac-glycerol by GC- or LC-MS. 1,2-dioleoyl-rac-glycerol is a diacylglycerol that contains oleic acid at the sn-1 and sn-2 positions. It effectively binds the C1 domain to activate conventional protein kinase C forms and serves as a substrate for diacylglycerol kinases and multisubstrate lipid kinase.1,2,3
|1. Yamaguchi, Y., Shirai, Y., Matsubara, T., et al. Phosphorylation and up-reg... |
|
T71300
|
Pentoxifylline-d6
|
|
|
|
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/... |
|
T37275
|
2,3-dinor-11β-Prostaglandin F2α
2,3-dinor-11β-Prostaglandin F2α
|
|
|
|
2,3-dinor-11β-Prostaglandin F2α (2,3-dinor-11β-PGF2α) was recovered from the urine of both normal monkeys and humans when infused with radiolabeled PGD2, where it represented approximately 1% and 4% of the infused radiolabeled dose, respectively. 2,3-dinor-11β-PGF2α has also been recovered from the urine of mastocytosis patients, where it is excreted in large amounts. In human asthmatic patients, 2,3-dinor-11β-PGF2α represents about 40% (as determined by GC/MS) of the immunoreactive 11β-PGF2α wh... |
|
T70883
|
Moexipril-d5
|
|
|
|
Moexipril-d5 intended for use as an internal standard for the quantification of moexipril by GC- or LC-MS. Moexipril is a prodrug form of the angiotensin converting enzyme (ACE) inhibitor moexiprilat. It is converted to moexiprilat in vivo by side chain ester hydrolysis. Moexipril inhibits ACE in a cell-free assay (IC50 = 2.7 µM for the rabbit enzyme). It also inhibits phosphodiesterase 4 (IC50s = 38, 160, and 230 µM for PDE4B2, PDE4A5 and PDE4D5, respectively). Moexipril (0.1-30 mg/kg per day) ... |
|
T71402
|
Nicorandil-d4
|
|
|
|
Nicorandil-d4 is intended for use as an internal standard for the quantification of nicorandil by GC- or LC-MS. Nicorandil is an activator of sulfonylurea receptor 2B (SUR2B) linked to ATP-sensitive potassium channel Kir6.2 (EC50 = ~10 µM) and a nitric oxide (NO) donor. It is selective for SUR2B/Kir6.2 over the SUR2A/Kir6.2 channel (EC50 = >500 µM). Nicorandil activates soluble guanylate cyclase in a cell-free assay and relaxes partially depolarized isolated bovine coronary artery strips (EC50 =... |
|
T35695
|
Oleic Acid-13C
|
|
|
|
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... |
|
T71401
|
Oxaliplatin-d10
|
|
|
|
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.... |
|
T35789
|
Palmitic acid-1-13C
|
|
|
|
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... |
|
T71141
|
Fenspiride-d5
|
|
|
|
Fenspiride-d5 is intended for use as an internal standard for the quantification of fenspiride by GC- or LC-MS. Fenspiride is an antagonist of histamine H1 receptors and a non-steroidal anti-inflammatory drug (NSAID). It inhibits histamine-induced contraction of isolated guinea pig trachea but not histamine-induced inotropy of isolated guinea pig heart. It also inhibits phosphodiesterase 4 (PDE4), PDE5, and PDE3 (IC50s = 69, ~158, and 363 µM, respectively, in isolated human bronchi derived from ... |
|
T69395
|
Nicotinamide-d4
|
|
|
|
Nicotinamide-d4 is intended for use as an internal standard for the quantification of nicotinamide by GC- or LC-MS. Nicotinamide is an amide form of niacin, which is also known as vitamin B3, that can be biosynthesized in vivo or obtained through the diet. It is a precursor in the synthesis of the metabolic cofactor NAD+ and an inhibitor of sirtuin 1 (SIRT1; IC50 = <50 µM). Nicotinamide (10 µM) increases the activity of serine palmitoyltransferase (SPT) and the biosynthesis of ceramide, glucosyl... |
|
T35698
|
Octanoic Acid-13C
|
|
|
|
Octanoic acid-13C is intended for use as an internal standard for the quantification of octanoic acid by GC- or LC-MS. Octanoic acid is a medium-chain saturated fatty acid. It has been found in Teleme cheeses made from goat, ovine, or bovine milk.1 Octanoic acid is active against the bacteria S. mutans, S. gordonii, F. nucleatum, and P. gingivalis (IC80s = <125, <125, 1,403, and 2,294 μM, respectively).2 Levels of octanoic acid are increased in the plasma of patients with medium-chain acyl-CoA d... |
|
T36660
|
Olsalazine-13C6
Olsalazine-13C6
|
|
|
|
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 ... |
|
T38356
|
1,2-Dipalmitoyl-13C-sn-glycero-3-PC
|
|
|
|
1,2-Dipalmitoyl-13C-sn-glycero-3-PC is intended for use as an internal standard for the quantification of 1,2-dipalmitoyl-sn-glycero-3-PC by GC- or LC-MS. 1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.1,2,3,4 It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.3 Incorporation... |
|
T35517
|
4-deoxy Nivalenol-13C15
4-deoxy Nivalenol-13C15
|
|
|
|
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... |
|
T35790
|
Palmitic acid-1,2,3,4-13C4
Palmitic Acid-13C (C1, C2, C3, and C4 labeled)
|
|
|
|
Palmitic acid-13C (C1, C2, C3, and C4 labeled) is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid is a common 16-carbon saturated fat that represents 10-20% of human dietary fat intake and comprises approximately 25 and 65% of human total plasma lipids and saturated fatty acids, respectively.1,2Acylation of palmitic acid to proteins facilitates anchoring of membrane-bound proteins to the lipid bilayer and trafficking of intracellula... |
|
T71212
|
Lornoxicam-d4
|
|
|
|
Lornoxicam-d4 is intended for use as an internal standard for the quantification of lornoxicam by GC- or LC-MS. Lornoxicam is a COX inhibitor and non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory and analgesic properties. It inhibits production of thromboxane B2 from arachidonic acid in HEL human erythroleukemic cells, which endogenously express COX-1, as well as inhibits LPS-induced formation of prostaglandin F1α from arachidonic acid in Mono-Mac-6 cells, which endogenously e... |
|
T36055
|
Nitisinone-13C6
Nitisinone-13C6
|
|
|
|
Nitisinone-13C6is intended for use as an internal standard for the quantification of nitisinone by GC- or LC-MS. Nitisinone is an inhibitor of 4-hydroxyphenylpyruvate dioxygenase (HPPD), which converts 4-hydroxyphenylpyruvate (HPPA) to homogentisate in the tyrosine catabolic pathway.1Nitisinone increases urinary levels of HPPA and 4-hydroxyphenyllactate (HPLA) in rats when administered at a dose of 10 mg/kg. Nitisinone (3 mg/kg) prevents the neonatal lethality of fumarylacetoacetate hydrolase (F... |
|
T69995
|
Chlorhexidine-d8 HCl
|
|
|
|
Chlorhexidine-d8 is intended for use as an internal standard for the quantification of chlorhexidine by GC- or LC-MS. Chlorhexidine is a bis(biguanide) antimicrobial disinfectant and antiseptic agent. It inhibits growth of clinical methicillin-resistant S. aureus (MRSA) isolates (MIC90 = 4 μg/ml). It is also active against canine isolates of MRSA, methicillin-susceptible S. aureus (MSSA), methicillin-resistant S. pseudintermedius (MRSP), and methicillin-susceptible S. pseudintermedius (MSSP; MIC... |
|
T35791
|
Palmitic acid-13C
|
|
|
|
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 ... |
|
T71981
|
Gliclazide-d4
|
|
|
|
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... |
|
T38118
|
Zanamivir-13C,15N2
Zanamivir-13C,15N2
|
|
|
|
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... |
|
T70882
|
Orlistat-d3
|
|
|
|
Orlistat-d3 is intended for use as an internal standard for the quantification of orlistat by GC- or LC-MS. Orlistat is a digestive lipase inhibitor. It inhibits diacylglycerol lipase α (DAGLα), DAGLβ, α/β-hydrolase domain-containing protein 12 (ABHD12), ABHD16A, and platelet-activating factor acetylhydrolase (PAF-AH; IC50s = 0.06, 0.1, 0.08, 0.03, and 0.05 µM, respectively), as well as pancreatic lipase and hormone-sensitive lipase (IC50s = 0.65 and 2.1 µg/ml, respectively) but does not inhibit... |
|
T71303
|
Flufenamic Acid-d4
|
|
|
|
Flufenamic acid-d4 is intended for use as an internal standard for the quantification of flufenamic acid by GC- or LC-MS. Flufenamic acid is a non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor (IC50s = 3 and 9.3 µM for human COX-1 and COX-2, respectively). Flufenamic acid inhibits TNF-α-induced increases in COX-2 levels and NF-κB activation in HT-29 colon cancer cells in a concentration-dependent manner. It inhibits calcium influx induced by fMLP or A23187 in human polymorphonuclear... |
|
T36070
|
(±)5(6)-EET
|
|
|
|
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... |
|
T35591
|
Guanfacine-13C,15N3
Guanfacine-13C,15N3
|
|
|
|
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... |
|
T70313
|
Indoxyl Sulfate-d5 potassium salt
|
|
|
|
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). ... |
|
T35683
|
2-deoxy-D-Glucose-13C6
2-deoxy-D-Glucose-13C6
|
|
|
|
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... |
沪公网安备 31010602006700号