95
13
2
2
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T12490 |
Pitavastatin lactone
|
Others; HMG-CoA Reductase | Metabolism; Others |
Pitavastatin lactone 是 Pitavastatin 在人体中的主要代谢产物。Pitavastatin 是 HMG-CoA 还原酶竞争性抑制剂。 | |||
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。 | |||
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。 | |||
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。 | |||
T21254 |
Vonoprazan Fumarate
TAK-438,TAK 438,Vonoprazan Fumurate,TAK438,富马酸沃诺拉赞 |
Proton pump | Membrane transporter/Ion channel |
Vonoprazan Fumarate (TAK438) 是质子泵的有效抑制剂,是口服有效的高效钾竞争性酸阻断剂,具有抗分泌活性。在 pH 为 6.5 时,它抑制猪胃微粒体中的 H+,K+-ATPase 酶活性,IC50为 19 nM。它被开发用于研究酸相关疾病,如消化性溃疡和胃食管反流病。 | |||
T27371 |
FR-167356
FR167356,FR 167356 |
ATPase | Membrane transporter/Ion channel |
FR-167356 是 a3 异构体液泡型 H+-ATPase 的特异性抑制剂,对破骨细胞质膜、肾刷状缘膜和巨噬细胞微粒体的 IC50 分别为 170 nM、370 nM 和 220 nM。 FR-167356 减少 B16-F10 细胞的骨转移。 | |||
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。 | |||
T11235 |
Estradiol 3-sulfamate
E2MATE,BLE 00084,ES-J 995 |
Estrogen Receptor/ERR | Endocrinology/Hormones |
Estradiol 3-sulfamate (BLE 00084) 是一种具有口服活性和高效性的甾体雌酮硫酸酯酶(ES)抑制剂。Estradiol 3-sulfamate 对人胎盘微粒体中ES的 K(i)值为73 nM,可用于研究乳腺癌。 | |||
T11339 |
Furegrelate sodium
U-63557A |
PPAR | DNA Damage/DNA Repair; Metabolism |
Furegrelate sodium (U-63557A) 是口服有效的、血栓素合酶选择性抑制剂,抑制人血小板微粒体血栓素 A2 (TxA2) 合酶的 IC50为 15 nM。它正在开发作为抗血小板药物。 | |||
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。 | |||
T23549 |
YM 511
|
P450; Aromatase | Endocrinology/Hormones; Metabolism |
YM 511 是一种高度特异性的非甾体芳香酶 (aromatase) 抑制剂。YM 511 竞争性抑制大鼠卵巢和人胎盘微粒体中的芳香酶活性 (IC50 分别为 0.4 和 0.12 nM)。YM 511 轻微抑制其他类固醇激素的产生。YM 511 具有用于抑制雌激素依赖性作用研究,不会影响其他类固醇激素的血清水平的潜力。 | |||
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 |
Others | Others |
Flufiprole is used as a phenylpyrazole pesticide. It has enantioselective metabolism in human and rat liver microsomes. | |||
T35919 |
N-hydroxy Riluzole
|
Others | Others |
N-hydroxy Riluzole is a metabolite of the antiglutamatergic agent riluzole .1It is formed from riluzole predominantly by the cytochrome P450 (CYP) isoform CYP1A2 in human hepatic microsomes. 1.Sanderink, G.J., Bournique, B., Stevens, J., et al.Involvement of human CYP1A isoenzymes in the metabolism and drug interactions of riluzole in vitroJ. Pharmacol. Exp. Ther.282(3)1465-1472(1997) | |||
T70091 |
IACS-4759
|
Others | Others |
IACS-4759 is a novel potent and selective MTH1 inhibitor with excellent cell permeability and good metabolic stability in microsomes. | |||
T27567 |
IAA-94
IAA94,IAA 94 |
Others | Others |
IAA-94 is an inhibitor of chloride channels, it binds channels in bovine kidney cortex microsomes with a Ki value of 1 µM. | |||
T37430 |
Mirtazapine N-oxide
|
Others | Others |
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. | |||
T37229 |
(±)8,9-DiHETE
|
Others | Others |
(±)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] | |||
T37306 |
6-hydroxy Chlorzoxazone
6-hydroxy Chlorzoxazone,NSC 24955 |
Others | Others |
6-hydroxy Chlorzoxazone is a metabolite of chlorzoxazone. [1] It is formed by metabolism of chlorzoxazone by the cytochrome P450 (CYP) isoform CYP2E1 in human hepatic microsomes. | |||
T84997 |
Hydroxy Celecoxib
|
Others | Others |
Hydroxy celecoxib, an inactive metabolite of celecoxib, is synthesized through the metabolism of celecoxib by cytochrome P450 (CYP) isoforms CYP2C9, CYP3A4, and CYP2D6 in human liver microsomes. | |||
T37210 |
5-hydroxy Indomethacin
|
Others | Others |
5-hydroxy Indomethacin is a metabolite of indomethacin .1It is formed from indomethacin in rabbit hepatic microsomes. 1.Evans, M.A., Papazafiratou, C., Bhat, R., et al.Indomethacin metabolism in isolated neonatal and fetal rabbit hepatocytesPediatr. Res.15(11)1406-1410(1981) | |||
T36666 |
Dehydro Warfarin
|
Others | Others |
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 |
Others | Others |
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. | |||
T84946 |
Chenodeoxycholic Acid 3-Glucuronide
CDCA-3G |
Others | Others |
Chenodeoxycholic acid 3-glucuronide (CDCA-3G), a metabolite of Chenodeoxycholic acid (CDCA), is synthesized in human liver microsomes. | |||
T36607 |
(±)8-HDHA
|
Others | Others |
(±)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. | |||
T35512 |
(±)16-HDHA
|
Others | Others |
(±)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. | |||
T32912 |
Lu49888 HCl
Azidopamil,LU49888,LU 49888,Ludopamil,LU-49888 |
Others | Others |
LU 49888 is a photoaffinity analog of verapamil that has been used to identify specific binding sites for phenylalkylamines of calcium channels present in rabbit skeletal muscle microsomes. | |||
T84582 |
Prostaglandin H2
PGH2 |
Others | Others |
Prostaglandin H2 (PGH2), initially isolated from the incubation of arachidonic acid with ovine seminal vesicle microsomes, acts as a potent vasoconstrictor. It serves as the precursor for all 2-series prostaglandins (PGs) and thromboxanes (TXs). Moreover, as a TP receptor agonist, PGH2 irreversibly aggregates human platelets at concentrations of 50-100 ng/ml. | |||
T75006 |
Antitubercular agent 34
|
Others | Others |
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
|
Others | Others |
(±)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. | |||
T64190 |
Keap1-Nrf2-IN-12
|
Others | Others |
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
|
Others | Others |
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... | |||
T36058 |
Dibutyl-3-Hydroxybutyl Phosphate
|
Others | Others |
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. | |||
T18292 |
Mal-PEG4-VC-PAB-DMEA-PNU-159682
|
Others; Drug-Linker Conjugates for ADC | Antibody-drug Conjugate/ADC Related; 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]. | |||
T35715 |
N-desmethyl Eletriptan
|
Others | Others |
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 |
Others | Others |
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. | |||
T18302 |
Mal-Phe-C4-VC-PAB-DMEA-PNU-159682
|
Others; Drug-Linker Conjugates for ADC | Antibody-drug Conjugate/ADC Related; 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]. | |||
T13658 |
DMEA-PNU-159682
|
Others; ADC Cytotoxin | Antibody-drug Conjugate/ADC Related; Others |
DMEA-PNU-159682 (molecule D12) is an ADC cytotoxin molecule, including neomycin (MMDX) metabolites from liver microsomes and effective ADC cytotoxin PNU-159682. | |||
T25826 |
MMV024101
MMV-024101,TCMDC 134293,TCMDC134293,TCMDC-134293,MMV 024101 |
Others | Others |
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 | |||
T28156 |
Nepaprazole
TY-11345,TY11345,TY 11345 |
Others | Others |
Nepaprazole is a proton pump inhibitor. TY-11345 potently inhibited H+/K(+)-ATPase activity in isolated rabbit gastric mucosal microsomes, and the inhibitory effect was enhanced under weak acid conditions, the IC50 being 5.8 microM and 9.9 microM at pH 6. | |||
T73148 |
ACT-777991
|
Others | Others |
ACT-777991为一种选择性、口服生效的CXCR3拮抗剂,于动物模型中展现出微粒体及肝细胞稳定性,能抑制活化T细胞向CXCL11迁移。 | |||
T35508 |
(±)13-HDHA
|
Others | Others |
(±)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。 |
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. | |||
T13618 |
Citreoviridin
|
Others | Others |
Citreoviridin, a toxin from Penicillium citreoviride NRRL 2579, inhibits brain synaptosomal Na+/K+-ATPase whereas, in microsomes, both Na+/K+-ATPase and Mg2+-ATPase activities are significantly stimulated in a dose-dependent manner. | |||
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), | |||
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。 | |||
T36776 |
Terpendole C
|
Others | Others |
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. | |||
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 |
Others | Others |
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
|
Others | Others |
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
|
Others | Others |
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 ... | |||
TN7278 |
Araguspongin B
|
Others | Others |
Xestospongins and araguspongins, marine natural products originally isolated from sponges in the Pacific basin, exhibit vasodilatory effects. Inositol phosphates (IP) serve as crucial signal transduction messengers, activating IP3 receptors to facilitate Ca2+ release from intracellular stores. Araguspongin B specifically hinders the calcium-releasing function of inositol 1,4,5-trisphosphate at the receptor level within cerebral microsomes, demonstrating an inhibition concentration (IC50) of 0.6 ... | |||
T13678 |
Enniatin A
|
Others | Others |
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. |
Cat. No. | Product Name | Species | Expression System |
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TMPH-01748 |
CYPOR Protein, Human, Recombinant (GST)
NADPH--cytochrome P450 reductase,P450R,CPR,POR,CYPOR |
Human | E. coli |
This enzyme is required for electron transfer from NADP to cytochrome P450 in microsomes. It can also provide electron transfer to heme oxygenase and cytochrome B5. CYPOR Protein, Human, Recombinant (GST) is expressed in E. coli expression system with N-GST tag. The predicted molecular weight is 102.9 kDa and the accession number is P16435. | |||
TMPY-03414 |
ABHD10 Protein, Human, Recombinant (aa 53-306, His)
ABHD10,abhydrolase domain containing 10 |
Human | Baculovirus Insect Cells |
Mycophenolic acid (MPA), the active metabolite of the immunosuppressant mycophenolate mofetil (MMF), is primarily metabolized by glucuronidation to a phenolic glucuronide (MPAG) and an acyl glucuronide (AcMPAG). It is known that AcMPAG, which may be an immunotoxic metabolite, is deglucuronidated in human liver. AcMPAG deglucuronidation activity was detected in both human liver cytosol (HLC) and microsomes (HLM). By purification from HLC with column chromatographic purification steps, the en... |
Cat. No. | Product Name | Target | Signaling Pathways |
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T69758 |
Flutamide-d7
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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... | |||
TMID-0116 |
Carbamazepine-10,11-epoxide-d10 (rings-d10)
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Carbamazepine-10,11-epoxide-d10 (rings-d10) 是 Carbamazepine-10,11-epoxide 的氘代化合物。Carbamazepine-10,11-epoxide 的 CAS 号为 36507-30-9。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。它对小鼠最大电击诱发的癫痫发作具有抗惊厥活性。 |