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91

抑制剂 & 化合物

12

天然产物

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Cat. No. Product Name Target Signaling Pathways
T12490 Pitavastatin lactone

Others 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。
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。
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。
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。
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

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.
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]
T35919 N-hydroxy Riluzole

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)
T27567 IAA-94

IAA94,IAA 94

IAA-94 is an inhibitor of chloride channels, it binds channels in bovine kidney cortex microsomes with a Ki value of 1 µM.
T70091 IACS-4759

IACS-4759 is a novel potent and selective MTH1 inhibitor with excellent cell permeability and good metabolic stability in microsomes.
T37210 5-hydroxy Indomethacin

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)
T37306 6-hydroxy Chlorzoxazone

6-hydroxy Chlorzoxazone,NSC 24955

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.
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.
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.
T32912 Lu49888 HCl

Azidopamil,LU49888,LU 49888,Ludopamil,LU-49888

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.
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].
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.
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
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。
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.
T28156 Nepaprazole

TY-11345,TY11345,TY 11345

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.
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.
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.
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。
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].
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。
T81200 S-Benzylglutathione

S-Benzylglutathione为竞争性谷胱甘肽酶抑制剂,能够经大鼠肾微粒体转化为相应的半胱氨酸衍生物。该化合物适用于研究谷胱甘肽酶系统对谷胱甘肽代谢的分解作用。
T73148 ACT-777991

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。
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。
T36045 1a,1b-dihomo Prostaglandin E2

1a,1b-dihomo Prostaglandin E2

1a,1b-dihomo Prostaglandin E2 (PGE2) is a rare polyunsaturated fatty acid first identified in extracts of sheep vesicular gland microsomes, known to contain COX, incubated with adrenic acid . 1a,1b-dihomo PGE2 has also been identified in conditioned media of RAW 264.7 macrophages stimulated with endotoxin and arachidonic acid . This product is thought to be produced by elongation of AA to adrenic acid, which is then metabolized sequentially by COX and PGE synthase.

化合物

Pitavastatin lactone
Cat.No: T12490
Synonym:
Target: Others
GNE0877
Cat.No: T6031
Synonym: GNE 0877,GNE-0877
Target: LRRK2
URB-597
Cat.No: T6714
Synonym: KDS-4103,FAAH Inhibitor II
Target: Mitophagy, FAAH, Autophagy
Ezutromid
Cat.No: T3424
Synonym: BMN 195,VOX-C1100,依珠曲米,SMT C1100
Target: Others
YM17E
Cat.No: T13373
Synonym:
Target: Acyltransferase, AChR
(S)-Lisofylline
Cat.No: T22148
Synonym:
Target: Others
1-Phenylpyrrole
Cat.No: T20373
Synonym: NSC16581,NSC-16581,1-苯基吡咯,NSC 16581
Target: Others
LY 43578
Cat.No: T27918
Synonym: LY-43578,LY43578
Target: P450, Aromatase
CYP1B1-IN-4
Cat.No: T73040
Synonym:
Target: P450
Pradefovir mesylate
Cat.No: T19526
Synonym: Pradefovir mesilate,Remofovir mesylate,Hepavir B,甲磺酸帕拉德福韦
Target: P450
Vonoprazan Fumarate
Cat.No: T21254
Synonym: TAK-438,TAK 438,Vonoprazan Fumurate,TAK438,富马酸沃诺拉赞
Target: Proton pump
FR-167356
Cat.No: T27371
Synonym: FR167356,FR 167356
Target: ATPase
HTHQ
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
Furegrelate sodium
Cat.No: T11339
Synonym: U-63557A
Target: PPAR
Clomethiazole
Cat.No: T14983
Synonym: Distraneurin,Chlormethiazole,氯美噻唑,5-(2-CHLOROETHYL)-4-METHYLTHIAZOLE
Target: P450, GABA Receptor
YM 511
Cat.No: T23549
Synonym:
Target: P450, Aromatase
Carbamazepine 10,11-epoxide
Cat.No: T37149
Synonym:
Target: Others
CP-24879 hydrochloride
Cat.No: T27061
Synonym: CP-24879 HCl
Target: Others
Flufiprole
Cat.No: T25428
Synonym: Rizazole,Butene-fipronil
Target:
Mirtazapine N-oxide
Cat.No: T37430
Synonym:
Target:
(±)8,9-DiHETE
Cat.No: T37229
Synonym:
Target:
N-hydroxy Riluzole
Cat.No: T35919
Synonym:
Target:
IAA-94
Cat.No: T27567
Synonym: IAA94,IAA 94
Target:
IACS-4759
Cat.No: T70091
Synonym:
Target:
5-hydroxy Indomethacin
Cat.No: T37210
Synonym:
Target:
6-hydroxy Chlorzoxazone
Cat.No: T37306
Synonym: 6-hydroxy Chlorzoxazone,NSC 24955
Target:
Dehydro Warfarin
Cat.No: T36666
Synonym:
Target:
Tenofovir-C3-O-C15-CF3 ammonium
Cat.No: T40239
Synonym: Tenofovir-C3-O-C15-CF3 ammonium
Target:
(±)16-HDHA
Cat.No: T35512
Synonym:
Target:
(±)8-HDHA
Cat.No: T36607
Synonym:
Target:
Lu49888 HCl
Cat.No: T32912
Synonym: Azidopamil,LU49888,LU 49888,Ludopamil,LU-49888
Target:
Dolutegravir O-β-D-Glucuronide
Cat.No: T36794
Synonym:
Target:
Antitubercular agent 34
Cat.No: T75006
Synonym:
Target:
(±)7-HDHA
Cat.No: T36606
Synonym:
Target:
Mal-PEG4-VC-PAB-DMEA-PNU-159682
Cat.No: T18292
Synonym:
Target: Others
N-desmethyl Eletriptan
Cat.No: T35715
Synonym:
Target:
Tenofovir-C3-O-C12-trimethylsilylacetylene ammonium
Cat.No: T40238
Synonym: Tenofovir-C3-O-C12-trimethylsilylacetylene ammonium
Target:
MMV024101
Cat.No: T25826
Synonym: MMV-024101,TCMDC 134293,TCMDC134293,TCMDC-134293,MMV 024101
Target:
Keap1-Nrf2-IN-12
Cat.No: T64190
Synonym:
Target:
DMEA-PNU-159682
Cat.No: T13658
Synonym:
Target: Others
Nepaprazole
Cat.No: T28156
Synonym: TY-11345,TY11345,TY 11345
Target:
Dibutyl-3-Hydroxybutyl Phosphate
Cat.No: T36058
Synonym:
Target:
22-HDHA
Cat.No: T35997
Synonym:
Target:
S6K2-IN-1
Cat.No: T79871
Synonym:
Target: FGFR
Mal-Phe-C4-VC-PAB-DMEA-PNU-159682
Cat.No: T18302
Synonym:
Target: Others
nSMase2-IN-1
Cat.No: T79321
Synonym:
Target: Phospholipase
S-Benzylglutathione
Cat.No: T81200
Synonym:
Target:
ACT-777991
Cat.No: T73148
Synonym:
Target:
Antiproliferative agent-25
Cat.No: T79275
Synonym:
Target: Histone Methyltransferase
1a,1b-dihomo Prostaglandin E2
Cat.No: T36045
Synonym: 1a,1b-dihomo Prostaglandin E2
Target:
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),
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。
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

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.
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]
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 ...
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).
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

Enniatin B
Cat.No: T13679
Synonym:
Target: ERK
Citreoviridin
Cat.No: T13618
Synonym:
Target: Others
7beta-(3-Ethyl-cis-crotonoyloxy)-1alpha-(2-methylbutyryloxy)-3,14-dehydro-Z-notonipetranone
Cat.No: TN3255
Synonym:
Target: Others
6-Hydroxy-TSU-68
Cat.No: T83264
Synonym:
Target:
7-Hydroxy-TSU-68
Cat.No: T83241
Synonym:
Target:
Terpendole C
Cat.No: T36776
Synonym:
Target:
Enniatin A1
Cat.No: T11201
Synonym: 恩镰孢菌素 A1
Target: ERK
β-Muricholic Acid
Cat.No: T35400
Synonym: β-MCA,5β-Cholanic Acid-3α,6β,7β-triol,β-Muricholic Acid
Target:
Phenylpyropene A
Cat.No: T37690
Synonym:
Target:
Thielavin A
Cat.No: T37774
Synonym:
Target:
Enniatin A
Cat.No: T13678
Synonym:
Target:
Enniatin B1
Cat.No: T13680
Synonym: 恩镰孢菌素 B1
Target: ERK
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