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67

抑制剂 & 化合物

11

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T6031	GNE0877 GNE 0877,GNE-0877	LRRK2	Autophagy
	GNE0877 (GNE 0877) 是一种高效且特异性的富含亮氨酸的重复激酶 2(LRRK2) 抑制剂，IC50为3 nM，Ki 为0.7 nM
T6714	URB-597 KDS-4103,FAAH Inhibitor II	Mitophagy; FAAH; Autophagy	Autophagy; Metabolism; Neuroscience
	URB-597 (FAAH Inhibitor II) 是一种可口服的选择性FAAH 抑制剂。它抑制大鼠脑膜、体外大鼠神经元和人肝微粒体中的 FAAH 活性，IC50分别为 5、0.5和 3 nM。它具有抗抑郁样作用，可研究缓解疼痛。
T3424	Ezutromid BMN 195,VOX-C1100,依珠曲米,SMT C1100	Others	Others
	Ezutromid (BMN 195) 是一种具有口服活性的、首创的苯并恶唑 utrophin 调节剂，EC50=0.91 μM。它抑制人肝微粒体 CYP1A2 酶活性，IC50=5.4 μM。它可用于 Duchenne 型肌营养不良症 (DMD) 的研究。
T13373	YM17E	Acyltransferase; AChR	Metabolism; Neuroscience
	YM17E 是一种 ACAT 抑制剂，在体外兔肝微粒体中的 IC50 为 44 nM。
T22148	(S)-Lisofylline	Others	Others
	(S)-Lisofylline 是抗炎剂 (R)-lisofylline 的非活性光学对映异构体。 (S)-Lisofylline 在人肝微粒体中专门转化为己酮可可碱。
T20373	1-Phenylpyrrole NSC16581,NSC-16581,1-苯基吡咯,NSC 16581	Others	Others
	1-Phenylpyrrole (NSC-16581) 可抑制大鼠肝脏微粒体中 CYP450 依赖性单加氧酶活性。
T19526	Pradefovir mesylate Pradefovir mesilate,Remofovir mesylate,Hepavir B,甲磺酸帕拉德福韦	P450	Metabolism
	Pradefovir mesylate (Hepavir B) 是一种肝脏 CYP3A4 底物。在人肝微粒体中，Pradefovir 能够转化为 9-[2-(磷酸甲氧基)乙基]腺嘌呤，其Km=60 μM。
T73040	CYP1B1-IN-4	P450	Metabolism
	CYP1B1-IN-4为选择性CYP1B1抑制剂（IC50=0.2 nM），属2,4-二芳基噻唑类化合物。其对细胞的毒性低，且在人类及大鼠肝微粒体中表现出稳定性。
T27918	LY 43578 LY-43578,LY43578	P450; Aromatase	Endocrinology/Hormones; Metabolism
	LY 43578 是一种具有口服活性的芳香酶 (aromatase) 抑制剂。LY 43578 对大鼠肝微粒体 P-450依赖的 p-nitroanisole 的 O -去甲基化和 ethylmorphine 的 N -去甲基化有抑制作用，IC50 分别为 0.3 和 5 μΜ。LY 43578 可用于研究神经系统疾病和心血管疾病。
T14983	Clomethiazole Distraneurin,Chlormethiazole,氯美噻唑,5-(2-CHLOROETHYL)-4-METHYLTHIAZOLE	P450; GABA Receptor	Membrane transporter/Ion channel; Metabolism; Neuroscience
	Clomethiazole (Distraneurin) 是口服GABAA 激动剂，可抑制人肝微粒体中的细胞色素 P450 异构体，CYP2A6 和 CYP2E1。它有抗惊厥作用，具有治疗惊厥性癫痫持续状态的潜力。
T3647	HTHQ HX 1171,HTHQ(1-O-Hexyl-2,3,5-trimethylhydroquinone),1-O-hexyl-2,3,5-trimethylhydroquinone	Reactive Oxygen Species	Immunology/Inflammation; Metabolism; NF-κB
	HTHQ (HTHQ(1-O-Hexyl-2,3,5-trimethylhydroquinone)) 是一种强力的亲脂性酚类抗氧化剂。它通过与活性氧直接反应，清除 ROS，从而形成更稳定的自由基，具有很强的抗氧化活性。
T37149	Carbamazepine 10,11-epoxide	Others	Others
	Carbamazepine 10,11-epoxide 是抗惊厥药卡马西平 (carbamazepine) 的活性代谢物。它由卡马西平通过微粒体中的细胞色素 P450 (CYP) 同种型 CYP3A4 和 CYP2C8 形成，微粒体分别由表达 CYP3A4 或 CYP2C8 的 HepG2 细胞制备。它对小鼠电击诱发的癫痫发作具有抗惊厥活性。
T27061	CP-24879 hydrochloride CP-24879 HCl	Others	Others
	CP-24879 hydrochloride (CP-24879 HCl) 是选择性的 delta5D/delta6D 联合抑制剂。它能显著降低肝细胞内脂质积聚和炎症损伤。它在脂肪-1 和 ω-3 处理的肝细胞中表现出优越的抗脂肪变性和抗炎作用，可用于非酒精性脂肪性肝炎的研究。
T25428	Flufiprole Rizazole,Butene-fipronil
	Flufiprole is used as a phenylpyrazole pesticide. It has enantioselective metabolism in human and rat liver microsomes.
T37430	Mirtazapine N-oxide
	Mirtazapine N-oxide is a metabolite of mirtazapine.1It is formed from mirtazapine by the cytochrome P450 (CYP) isoforms CYP1A2 and CYP3A4 in human liver microsomes.
T36666	Dehydro Warfarin
	Dehydro warfarin is a metabolite of (±)-warfarin .1It is formed from (±)-warfarin by rat liver microsomes. 1.Kaminsky, L.S., Fasco, M.J., and Guengerich, F.P.Comparison of different forms of liver, kidney, and lung microsomal cytochrome P-450 by immunological inhibition of regio- and stereoselective metabolism of warfarinJ. Biol. Chem.254(19)9657-9662(1979)
T40239	Tenofovir-C3-O-C15-CF3 ammonium Tenofovir-C3-O-C15-CF3 ammonium
	Tenofovir-C3-O-C15-CF3 (ammonium) demonstrates prolonged half-life values compared to tenofovir in human liver microsomes. It exhibits potent anti-HIV activity in vitro and enhances pharmacokinetic properties in vivo.
T37229	(±)8,9-DiHETE
	(±)8,9-DiHETE is a major metabolite of the 20:5 ω-3 fatty acid eicosapentaenoic acid .[1] It is produced in rat liver microsomes, but not renal microsomes, by the generation of the unstable intermediate 8,9-epoxy eicosatetraenoic acid from EPA by cytochrome P450 monooxygenases. Dietary EPA supplementation in humans results in substantial urinary excretion of vicinal diols, including 8,9, 11,12, and 14,15 forms.[2]
T35715	N-desmethyl Eletriptan
	N-desmethyl Eletriptan is a metabolite of eletriptan .1It is formed from eletriptan primarily by the cytochrome P450 (CYP) isoform CYP3A4 in human liver microsomes. 1.Evans, D.C., O’Connor, D., Lake, B.G., et al.Eletriptan metabolism by human hepatic CYP450 enzymes and transport by human P-glycoproteinDrug Metab. Dispos.31(7)861-869(2003)
T40238	Tenofovir-C3-O-C12-trimethylsilylacetylene ammonium Tenofovir-C3-O-C12-trimethylsilylacetylene ammonium
	Tenofovir-C3-O-C12-trimethylsilylacetylene (ammonium) displays a prolonged half-life (t1/2) compared to tenofovir in human liver microsomes. Moreover, it demonstrates potent in vitro anti-HIV activity and improves in vivo pharmacokinetic properties.
T35512	(±)16-HDHA
	(±)16-HDHA is an autoxidation product of docosahexaenoic acid (DHA) in vitro. It is also produced from incubations of DHA in rat liver, brain, and intestinal microsomes. (±)16-HDHA is a potential marker of oxidative stress in brain and retina where DHA is an abundant polyunsaturated fatty acid.
T36607	(±)8-HDHA
	(±)8-HDHA is an autoxidation product of docosahexaenoic acid (DHA) in vitro. It is also produced from incubations of DHA in rat liver, brain, and intestinal microsomes. (±)8-HDHA is a potential marker of oxidative stress in brain and retina where DHA is an abundant polyunsaturated fatty acid.
T25826	MMV024101 MMV-024101,TCMDC 134293,TCMDC134293,TCMDC-134293,MMV 024101
	MMV024101 is a PI4K inhibitor. MMV024101 exhibits submicromolar potency against P. falciparum NF54 (IC50 =543 nM), low aqueous solubility (<5 μM), and rapid clearance by mouse liver microsomes with only 2% of parent compound remaining after 30 min of incu
T13658	DMEA-PNU-159682	Others	Others
	DMEA-PNU-159682 (molecule D12) is an ADC cytotoxin molecule, including neomycin (MMDX) metabolites from liver microsomes and effective ADC cytotoxin PNU-159682.
T64190	Keap1-Nrf2-IN-12
	eap1-Nrf2-IN-12 是一种 Keap1-Nrf2 的有效抑制剂 (IC50: 2.30 μM)。Keap1-Nrf2-IN-12 在人肝微粒体中具有代谢稳定性。
T36794	Dolutegravir O-β-D-Glucuronide
	Dolutegravir O-β-D-glucuronide is a metabolite of the HIV integrase inhibitor dolutegravir .1It is formed from dolutegravir primarily by the UDP-glucuronosyltransferase (UGT) isoform UGT1A1in vivobut is also metabolized by UGT1A9 in human liver and kidney microsomes and UGT1A3 in human intestinal microsomes.2,1 1.Liu, S.N., Lu, J.B., Watson, C.J.W., et al.Mechanistic assessment of extrahepatic contributions to glucuronidation of integrase strand transfer inhibitorsDrug Metab. Dispos.47(5)535-544...
T75006	Antitubercular agent 34
	Antitubercular agent 34 (compound 42g) 是一种表现出对MtbH37Rv生长抑制能力的抗结核剂，MIC90为1.25 μg/mL。该化合物能够抵抗人肝微粒体代谢的降解作用，适用于结核病研究。
T36606	(±)7-HDHA
	(±)7-HDHA is an autoxidation product of docosahexaenoic acid (DHA) in vitro. It is also produced from incubations of DHA in rat liver, brain, and intestinal microsomes. Enzymatic transformation of DHA by RBL-1 cells and human neutrophils also produces 7-HDHA. However, the enzymatic product is most likely the S-isomer. (±)7-HDHA is a potential marker of oxidative stress in brain and retina where DHA is an abundant polyunsaturated fatty acid.
T18292	Mal-PEG4-VC-PAB-DMEA-PNU-159682	Others	Others
	Mal-PEG4-VC-PAB-DMEA-PNU-159682 is a drug-linker conjugate designed for antibody-drug conjugate (ADC) therapy. It combines the ADC linker, Mal-PEG4-VC-PAB, with the potent ADC cytotoxin, DMEA-PNU-159682. The cytotoxin, DMEA-PNU-159682, is derived from metabolites of nemorubicin (MMDX) found in liver microsomes, as well as the ADC cytotoxin PNU-159682[1].
T36058	Dibutyl-3-Hydroxybutyl Phosphate
	Dibutyl 3-hydroxybutyl phosphate is a compound produced from the metabolism of the organophosphorus solvent, tributyl phosphate (TBP). Incubation of goldfish liver microsomes in the presence of NADPH has been shown to convert TBP into dibutyl-3-hydroxybutyl phosphate and dibutyl phosphate. Dibutyl-3-hydroxybutyl phosphate has also been produced during radiolysis of TBP.
T17802	DBCO-PEG4-VC-PAB-DMEA-PNU-159682	Others	Others
	DBCO-PEG4-VC-PAB-DMEA-PNU-159682, a drug-linker conjugate for antibody-drug conjugates (ADC), comprises the ADC linker DBCO-PEG4-VC-PAB and the potent ADC cytotoxin DMEA-PNU-159682. The cytotoxin includes metabolites of nemorubicin (MMDX) from liver microsomes and the ADC cytotoxin PNU-159682[1].
T18302	Mal-Phe-C4-VC-PAB-DMEA-PNU-159682	Others	Others
	Mal-Phe-C4-VC-PAB-DMEA-PNU-159682 is a drug-linker conjugate utilized in antibody-drug conjugate (ADC) therapy. It comprises the ADC linker Mal-Phe-C4-VC-PAB and the potent ADC cytotoxin DMEA-PNU-159682. DMEA-PNU-159682 encompasses metabolites of nemorubicin (MMDX) derived from liver microsomes, as well as the ADC cytotoxin PNU-159682[1].
T35543	Methyl Diethyldithiocarbamate
	Methyl diethyldithiocarbamate is an active metabolite of the aldehyde dehydrogenase inhibitor disulfiram .1It is produced by methylation of the disulfiram metabolite diethyldithiocarbamate in mouse liver microsomes.2Methyl diethyldithiocarbamate inhibits liver low Kmaldehyde dehydrogenase (ALDH) in rats (ID50= 15.5 mg/kg).1It decreases mean arterial pressure (MAP) and increases heart rate during ethanol challenge in rats when administered at a dose of 20.6 mg/kg. 1.Hart, B.W., Yourick, J.J., and...
T61136	Enpp-1-IN-11
	Enpp-1-IN-11 (compound 23) is a highly potent inhibitor of Ecto-nucleotide pyrophosphatase/phosphodiesterases 1 (ENPP1), with a Ki value of 45 nM. It demonstrates excellent stability in human and mouse plasma and exhibits low clearance in both human and mouse liver microsomes. Enpp-1-IN-11 holds promise for anticancer research [1].
T35508	(±)13-HDHA
	(±)13-HDHA is an autoxidation product of docosahexaenoic acid (DHA) in vitro. It is also produced from incubations of DHA in rat liver, brain, and intestinal microsomes. Fresh water hydra was shown to metabolize DHA to 13(R)-HDHA, presumably via the 11R-lipoxygenase activity. (±)13-HDHA is a potential marker of oxidative stress in brain and retina where DHA is an abundant polyunsaturated fatty acid.
T79275	Antiproliferative agent-25	Histone Methyltransferase	Chromatin/Epigenetic
	Antiproliferative agent-25 (Compound 3s4)作为一种选择性PRMT5抑制剂(IC50: 0.11 μM)，能够上调hnRNP E1蛋白水平，并通过与SAM及PRMT5的E444残基形成氢键相互作用。该化合物通过促进apoptosis和抑制细胞迁移，有效抑制A549细胞的增殖。此外，Antiproliferative agent-25在人和大鼠肝微粒体中的高清除率表明，其T1/2分别为21.8和4.7分钟。
T36920	16α-hydroxy Dehydroepiandrosterone
	16α-hydroxy Dehydroepiandrosterone is a metabolite of the endogenous steroid hormone dehydroepiandrosterone .116α-hydroxy Dehydroepiandrosterone is formed from dehydroepiandrosteronevia16-hydroxylation by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP3A5 in adult human liver microsomes, as well as by fetal recombinant CYP3A7. It is a precursor to fetal estrogens, including estriol .2 1.Miller, K.K.M., Cai, J., Ripp, S.L., et al.Stereo- and regioselectivity account for the diversity of dehydro...
T79871	S6K2-IN-1	FGFR	Angiogenesis; Tyrosine Kinase/Adaptors
	S6K2-IN-1（化合物2）为S6K2抑制剂（IC50：22 nM），并对FGFR4亦有抑制作用（IC50：216 nM）。该化合物在小鼠肝微粒体中展现出良好的稳定性。
T36109	L Moses dihydrochloride
	High affinity and selective cell-permeable p300/CBP-associated factor (PCAF) inhibitor (Ki = 47 nM). Exhibits no significant activity against a panel of 48 other bromodomains except GCN5 (Kd = 600 nM). Exhibits >4500-fold selectivity for PCAF over BRD4. Also exhibits metabolic stability in mouse and human liver microsomes and no observable cytotoxicity in peripheral blood mononuclear cells (PBMC). Moustakim et al (2017) Discovery of a PCAF bromodomain chemical probe. Angew.Chem.Int.Ed. 56 827 P...
T79321	nSMase2-IN-1	Phospholipase	Metabolism
	nSMase2-IN-1是一款口服活性的nSMase2抑制剂，具有0.13 ± 0.06 μM的IC50。该化合物在肝脏微粒体内具有良好的代谢稳定性，口服给药后获得较高的脑血浆比值，适用于神经系统疾病研究。
T36840	(R)-Omeprazole (sodium salt)
	(R)-Omeprazole is the inactive isomer of omeprazole , a gastric proton-pump inhibitor. A stereoselective hydroxylation of (R)-omeprazole is mediated primarily by cytochrome P450 (CYP) 2C19, whereas CYP3A4 favors sulfoxidation of the active (S)-enantiomer . (R)-Omeprazole has been shown to act as a reversible direct-acting and metabolism-dependent inhibitor of CYP2C19 in pooled human liver microsomes (IC50 = 8.1 μM).
T35997	22-HDHA
	22-HDHA is an oxidation product of docosahexaenoic acid . In vitro, it is formed upon incubation of rat liver microsomes with DHA and NADPH and also by the human cytochrome P450 (CYP) isoform CYP4F3B in BTI-TN-5B1-4 microsomes. Serum levels of 22-HDHA increase following dietary DHA supplementation in humans.
T35504	(±)10-HDHA
	(±)10-HDHA is an autoxidation product of docosahexaenoic acid (DHA) in vitro.[1][2] It is also produced from incubations of DHA in rat liver, brain, and intestinal microsomes.[3][4][5] (±)10-HDHA is a potential marker of oxidative stress in brain and retina where DHA is an abundant polyunsaturated fatty acid. Reference：[1]. VanRollins, M., and Murphy, R.C. Autooxidation of docosahexaenoic acid: Analysis of ten isomers of hydroxydocosahexaenoate. J. Lipid Res. 25(5), 507-517 (1984).[2]. Reynaud, ...
T36602	(±)4-HDHA
	(±)4-HDHA is an autoxidation product of docosahexaenoic acid (DHA) in vitro. It is also produced from incubations of DHA in rat liver, brain, and intestinal microsomes. Enzymatic transformation of DHA by RBL-1 cells also produces 4-HDHA. However, the enzymatic product is most likely the S-isomer. (±)4-HDHA is a potential marker of oxidative stress in brain and retina where DHA is an abundant polyunsaturated fatty acid.
T69758	Flutamide-d7
	Flutamide-d7 is intended for use as an internal standard for the quantification of flutamide by GC- or LC-MS. Flutamide is an androgen receptor antagonist and prodrug form of 2-hydroxy flutamide. Flutamide is converted to 2-hydroxy flutamide by the cytochrome P450 (CYP) isoform CYP1A2 in human liver microsomes. It is cytotoxic to PC3 and LNCaP prostate cancer cells with IC50 values of 98.8 and 81.8 µM, respectively. Flutamide (50 mg/kg per day) reduces tumor growth in a PC-82 mouse xenograft mo...
T36681	Sorafenib N-oxide
	Sorafenib N-oxide is an active metabolite of sorafenib , an inhibitor of Raf-1, B-RAF, and receptor tyrosine kinases. Sorafenib N-oxide inhibits FLT3 that contains the internal tandem duplication mutation (FLT3-ITD; Kd = 70 nM) and inhibits proliferation of MV4-11 acute myeloid leukemia (AML) cells expressing FLT3-ITD (IC50 = 25.8 nM). It is selective for AML cell lines containing FLT3-ITD over lines containing wild-type FLT3 (IC50s = 3.9-13.3 μM). Sorafenib N-oxide is also a linear-mixed inhibi...
T28449	Pradefovir ICN-2001-3,MB-6866,帕拉德福韦,ICN-20013,MB-06866,Remofovir	HBV	Microbiology/Virology
	Pradefovir (Remofovir) 是一种逆转录酶抑制剂，可能用于治疗慢性 HBV 感染。它也是阿德福韦的肝脏靶向前药。代谢激活后，它在人肝微粒体中转化为 PMEA(9-(2-膦酰基甲氧基乙基)腺嘌呤)，Km 为 60 microM，最大代谢速率为 228 pmol/min/mg 蛋白质，以及内在的清除率约为 359 ml/min。
T78786	MmpL3-IN-3
	MmpL3-IN-3 (Compound 12) 为一种MmpL3抑制剂，对 H37Rv 的最小抑制浓度(MIC)为 0.1 μM。该化合物在小鼠肝微粒体中具有良好稳定性，适用于抗结核研究。
T36397	TAN 420E
	TAN 420E is a bacterial metabolite originally isolated from Streptomyces. It scavenges 2,2-diphenyl-1-picrylhydrazyl radicals in a cell-free assay (IC50 = 1.3 μM) and reduces thiobarbituric acid reactive substances (TBARS) in rat liver microsomes by 72% when used at a concentration of 100 μg/ml. TAN 420E is active against B. brevis, B. cereus, M. flavus, and S. aureus (MICs = 50-100 μg/ml). It is cytotoxic to P388 and KB lymphocytic leukemia cells (EC50s = 0.022 and 0.3 μg/ml, respectively).
T61956	BACE1/2-IN-1
	BACE1/2-IN-1 (化合物 34) 是有效的BACE1和BACE2抑制剂，IC50分别为 0.01 和 0.0053 μM。BACE1/2-IN-1 具有较低的 Pgp 外排比和改善的被动渗透率。BACE1/2-IN-1 在肝脏微粒体中代谢稳定性降低。

化合物

Cat.No: T6031

Synonym: GNE 0877,GNE-0877

Target: LRRK2

Cat.No: T6714

Synonym: KDS-4103,FAAH Inhibitor II

Target: Mitophagy, FAAH, Autophagy

Cat.No: T3424

Synonym: BMN 195,VOX-C1100,依珠曲米,SMT C1100

Target: Others

Cat.No: T13373

Target: Acyltransferase, AChR

(S)-Lisofylline

Cat.No: T22148

Target: Others

1-Phenylpyrrole

Cat.No: T20373

Synonym: NSC16581,NSC-16581,1-苯基吡咯,NSC 16581

Target: Others

Pradefovir mesylate

Cat.No: T19526

Synonym: Pradefovir mesilate,Remofovir mesylate,Hepavir B,甲磺酸帕拉德福韦

Target: P450

Cat.No: T73040

Target: P450

Cat.No: T27918

Synonym: LY-43578,LY43578

Target: P450, Aromatase

Cat.No: T14983

Synonym: Distraneurin,Chlormethiazole,氯美噻唑,5-(2-CHLOROETHYL)-4-METHYLTHIAZOLE

Target: P450, GABA Receptor

Cat.No: T3647

Synonym: HX 1171,HTHQ(1-O-Hexyl-2,3,5-trimethylhydroquinone),1-O-hexyl-2,3,5-trimethylhydroquinone

Target: Reactive Oxygen Species

Carbamazepine 10,11-epoxide

Cat.No: T37149

Target: Others

CP-24879 hydrochloride

Cat.No: T27061

Synonym: CP-24879 HCl

Target: Others

Cat.No: T25428

Synonym: Rizazole,Butene-fipronil

Mirtazapine N-oxide

Cat.No: T37430

Dehydro Warfarin

Cat.No: T36666

Tenofovir-C3-O-C15-CF3 ammonium

Cat.No: T40239

Synonym: Tenofovir-C3-O-C15-CF3 ammonium

Cat.No: T37229

N-desmethyl Eletriptan

Cat.No: T35715

Tenofovir-C3-O-C12-trimethylsilylacetylene ammonium

Cat.No: T40238

Synonym: Tenofovir-C3-O-C12-trimethylsilylacetylene ammonium

Cat.No: T35512

Cat.No: T36607

Cat.No: T25826

Synonym: MMV-024101,TCMDC 134293,TCMDC134293,TCMDC-134293,MMV 024101

DMEA-PNU-159682

Cat.No: T13658

Target: Others

Keap1-Nrf2-IN-12

Cat.No: T64190

Dolutegravir O-β-D-Glucuronide

Cat.No: T36794

Antitubercular agent 34

Cat.No: T75006

Cat.No: T36606

Mal-PEG4-VC-PAB-DMEA-PNU-159682

Cat.No: T18292

Target: Others

Dibutyl-3-Hydroxybutyl Phosphate

Cat.No: T36058

DBCO-PEG4-VC-PAB-DMEA-PNU-159682

Cat.No: T17802

Target: Others

Mal-Phe-C4-VC-PAB-DMEA-PNU-159682

Cat.No: T18302

Target: Others

Methyl Diethyldithiocarbamate

Cat.No: T35543

Cat.No: T61136

Cat.No: T35508

Antiproliferative agent-25

Cat.No: T79275

Target: Histone Methyltransferase

16α-hydroxy Dehydroepiandrosterone

Cat.No: T36920

Cat.No: T79871

Target: FGFR

L Moses dihydrochloride

Cat.No: T36109

Cat.No: T79321

Target: Phospholipase

(R)-Omeprazole (sodium salt)

Cat.No: T36840

Cat.No: T35997

Cat.No: T35504

Cat.No: T36602

Cat.No: T69758

Sorafenib N-oxide

Cat.No: T36681

Cat.No: T28449

Synonym: ICN-2001-3,MB-6866,帕拉德福韦,ICN-20013,MB-06866,Remofovir

Target: HBV

Cat.No: T78786

Cat.No: T36397

Cat.No: T61956

Cat. No.	Product Name	Target	Signaling Pathways
T13679	Enniatin B	ERK	MAPK
	Enniatins B decreases the activation of ERK (p44/p42). Enniatin B is a Fusarium mycotoxin. Enniatin B inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 113 μM in an enzyme assay using rat liver microsomes.
TN3255	7beta-(3-Ethyl-cis-crotonoyloxy)-1alpha-(2-methylbutyryloxy)-3,14-dehydro-Z-notonipetranone	Others	Others
	7beta-(3-Ethyl-cis-crotonoyloxy)-1alpha-(2-methylbutyryloxy)-3,14-dehydro-Z-notonipetranone shows diacylglycerol acyltransferase (DGAT)1 inhibition with IC(50) values of 47.0 microM (for rat liver microsomes) and 160.7 microM (for HepG2 cell microsomes),
T36776	Terpendole C
	Terpendole C is an indole diterpene alkaloid fungal metabolite originally isolated from A. yamanashiensis and an inhibitor of acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 2.1 μM in rat liver microsomes). It also inhibits ACAT in J774 macrophages (IC50 = 0.46 μM) without affecting cell growth.
T11201	Enniatin A1 恩镰孢菌素 A1	ERK	MAPK
	Enniatin A1 possesses anticarcinogenic properties by induction of apoptosis and disruption of ERK signalling pathway. Enniatin A1 inhibits ACAT with an IC50 of 49 μM in rat liver microsomes. Enniatin A1 isolated from Fusarium mycotoxins is a cyclic hexadepsipeptide consisting of alternating D-α-hydroxyisovaleric acids and N-methyl-L-amino acids.
T83241	7-Hydroxy-TSU-68
	7-Hydroxy-TSU-68为TSU-68的衍生物，该化合物为TSU-68在人类肝微粒体内经生物转化途径形成的代谢产物，其含量标识了TSU-68自身诱导的羟基化程度。
T83264	6-Hydroxy-TSU-68
	6-Hydroxy-TSU-68为TSU-68的衍生物，此化合物为TSU-68在人肝微粒体生物转化路径中的代谢产物，其含量反映TSU-68的自诱导羟基化程度。
T35400	β-Muricholic Acid β-MCA,5β-Cholanic Acid-3α,6β,7β-triol,β-Muricholic Acid
	β-Muricholic acid (β-MCA) is a murine-specific primary bile acid.[1],[2] Dietary administration of β-MCA reduces HMG-CoA reductase activity in liver microsomes from mice fed a high cholesterol and cholic acid diet.[3] Dietary administration of β-MCA also dissolves 100% of gallstones in a gallstone-susceptible mouse model of diet-induced cholesterol gallstones.[4]
T37774	Thielavin A
	Thielavin A is a fungal metabolite originally isolated from T. terricola that is related to thielavin B . Thielavin A inhibits COX, blocking both the conversion of arachidonic acid to prostaglandin H2 and the conversion of PGH2 to PGE2 . Thielavin A also inhibits glucose-6-phosphatase in rat liver microsomes (IC50 = 4.6 μM). It is a non-competitive inhibitor of α-glucosidase from S. cerevisiae (IC50 = 23.8 μM; Ki = 27.8 μM).
T37690	Phenylpyropene A
	Phenylpyropene A is a fungal metabolite originally isolated from P. griseofulvum that has enzyme inhibitory and insecticidal activities.1,2,3 It inhibits acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 0.8 μM).1 Phenylpyropene A inhibits diacylglycerol acyltransferase (DGAT) in rat liver microsomes (IC50 = 78.7 μM). It induces mortality in 100% of M. persicae when used at a concentration of 5 ppm.3 \|1. Kwon, O.E., Rho, M.C., Song, H.Y., et al. Phenylpyropene A and B, new inhibitors of ...
T13678	Enniatin A
	Enniatin A is a Fusarium mycotoxin. Enniatin A inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 22 μM in an enzyme assay using rat liver microsomes.
T13680	Enniatin B1 恩镰孢菌素 B1	ERK	MAPK
	Enniatin B1 crosss the blood-brain barrier. Enniatin B1 decreases the activation of ERK (p44/p42). Enniatin B1 inhibits moderately TNF-α-induced NF-κB activation.Enniatin B1 is a Fusarium mycotoxin. Enniatin B1 inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 73 μM in an enzyme assay using rat liver microsomes.

天然产物

Cat.No: T13679

Target: ERK

7beta-(3-Ethyl-cis-crotonoyloxy)-1alpha-(2-methylbutyryloxy)-3,14-dehydro-Z-notonipetranone

Cat.No: TN3255

Target: Others

Cat.No: T36776

Cat.No: T11201

Synonym: 恩镰孢菌素 A1

Target: ERK

7-Hydroxy-TSU-68

Cat.No: T83241

6-Hydroxy-TSU-68

Cat.No: T83264

β-Muricholic Acid

Cat.No: T35400

Synonym: β-MCA,5β-Cholanic Acid-3α,6β,7β-triol,β-Muricholic Acid

Cat.No: T37774

Phenylpyropene A

Cat.No: T37690

Cat.No: T13678

Cat.No: T13680

Synonym: 恩镰孢菌素 B1

Target: ERK

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