“angiotensin converting enzyme ace”的搜索结果
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CYP17 抑制剂
Abiraterone Acetate是Abiraterone的醋酸盐形式,是一种甾体类细胞色素CYP17抑制剂。
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CETP 抑制剂
Anacetrapib (MK-0859)是一种有效的,选择性,可逆的rhCETP和突变CETP(C13S)抑制剂,IC50分别为7.9 nM和11.8 nM,提高HDL-C,降低LDL-C,不提高醛固酮和血压。
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Androgen Receptor 拮抗剂
Cyproterone acetate是17-羟孕酮的合成衍生物,可作为雄激素受体拮抗剂以及具有弱孕激素和糖皮质激素活性的弱孕激素受体激动剂。
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HMG-CoA Reductase 抑制剂
Clinofibrate是一种脂质清除剂,似乎可以改变脂质代谢,减少类固醇诱导的骨细胞内脂质堆积。它还可以有效降低血浆纤维蛋白原水平。抑制hydroxymethylglutaryl coenzyme A reductase (HMGCR)(羟甲基戊二酰辅酶A还原酶),IC50为0.47 mM。
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cytochrome P4503A4 抑制剂
Clarithromycin是一种大环内酯类抗生素。它通过干扰细菌的蛋白质合成来防止细菌生长。
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- Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Takashi Azuma, .et al. Removal of pharmaceuticals in water by introduction of ozonated microbubbles, SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. Distribution of six anticancer drugs and a variety of other pharmaceuticals, and their sorption onto sediments, in an urban Japanese river, Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. Detection of pharmaceuticals and phytochemicals together with their metabolites in hospital effluents in Japan, and their contribution to sewage treatment plant influents, Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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CETP 抑制剂
Evacetrapib (LY2484595)是一种强效选择性CETP抑制剂,IC50为5.5 nM,可在不增加醛固酮或血压的情况下升高HDL胆固醇。
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Geranylgeranylacetone可以诱导HSP70,HSPB8和HSPB1的表达。
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PDE 抑制剂
GSK256066是一种选择性PDE4B(与A-D型同等亲和力)抑制剂,IC50为3.2 pM,对PDE1/2/3/5/6的选择性> 380,000倍,对PDE4B与PDE7的选择性> 2500倍。
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Liver-targeting SCD 抑制剂?
MK-8245 Trifluoroacetate是硬脂酰辅酶A去饱和酶(SCD)的肝靶向抑制剂,对人SCD1的IC50为1 nM,对大鼠SCD1和小鼠SCD1的IC50为3 nM,具有抗糖尿病和抗血脂异常的功效。
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Carbonic Anhydrase 抑制剂
Acetazolamide是一种有效的碳酸酐酶(CA)抑制剂,在临床实践中通常用作迅速降低眼内压(IOP)的直接且容易获得的选择。
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MAO-A inhibitor
Minaprine is a reversible inhibitor of MAO-A; weakly inhibit acetylcholinesterase; an antidepressant for treatment of depression.
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PDE5/HDAC-1 inhibitor
CM-675 is a dual phosphodiesterase 5 (PDE5) and class I histone deacetylases-selective inhibitor, with IC50 values of 114 nM and 673 nM for PDE5 and HDAC1, respectively. CM-675 has potential to treat Alzheimer??s disease.
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ACC inhibitor
ND-646 is an orally bioavailable and steric inhibitor of acetyl-CoA carboxylase (ACC) with IC50s of 3.5 nM and 4.1 nM for recombinant hACC1 and hACC2, respectively.
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ACCA inhibitor
TOFA (RMI14514;MDL14514) is an allosteric inhibitor of acetyl-CoA carboxylase-α (ACCA ).
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ACC inhibitor
Olumacostat glasaretil is a small molecule inhibitor of acetyl coenzyme A carboxylase (ACC).
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Monoamine oxidase inhibitor
Rasagiline 13C3 mesylate racemic is the deuterium labeled Rasagiline, which is an irreversible inhibitor of monoamine oxidase.
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dual α/γ PPAR activator
Peliglitazar racemate is the racemate of Peliglitazar. Peliglitazar is a novel dual α/γ PPAR activator.
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PDE1 inhibitor
ITI-214 is a picomolar PDE1 inhibitor with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters, and ion channels, exhibits potent PDE1 inhibitory activity (Ki = 58 pM).
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ACC inhibitor
PF-05175157 is broad spectrum acetyl-CoA carboxylase (ACC) inhibitor with IC50s of 27.0, 33.0, 23.5 and 50.4 nM for ACC1 (human), ACC2 (human), ACC1 (rat), ACC2 (rat), respectively.
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FASN inhibitor
HS-80 is an enantiomer of Fasnall, which is a selective fatty acid synthase (FASN) inhibitor. HS-80 is able to inhibit the incorporation of tritiated acetate into lipids with an IC50 of 7.13 μM.
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PDE9 inhibitor
BAY 73-6691 racemate is a phosphodiesterase 9 inhibitor extracted from patent WO 2017070293 A1.
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ACC inhibitor
CP-640186 hydrochloride is a potent and cell-permeable Acetyl-CoA carboxylase (ACC) inhibitor with IC50s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively.
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picomolar PDE1 inhibitor
ITI-214 (free base) is a picomolar PDE1 inhibitor with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters, and ion channels, exhibits potent PDE1 inhibitory activity (Ki = 58 pM).
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ACC inhibitor
Firsocostat (ND-630; GS-0976; NDI-010976) is an acetyl-CoA carboxylase (ACC) inhibitor; inhibits human ACC1 and ACC2 with IC50 values of 2.1 and 6.1 nM, respectively.
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15-PGDH enzyme 抑制剂
SW033291是15-PGDH的小分子抑制剂(Ki = 0.1 nM),可增加骨髓和其他组织中前列腺素PGE2的水平。
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Nampt inhibitor
CB30865(ZM 242421) is a potent inhibitor of Nampt , an enzyme present in the NAD biosynthetic pathway.
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FAAH inhibitor
PF 750 is a selective and covalent fatty acid amide hydrolase (FAAH) inhibitor, with IC50s varied from 16.2-595 nM in different pre-incubation times. Covalently modifies the enzyme??s active site serine nucleophile.
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CYP3A4 enzyme inhibitor
Bergaptol is a hydroxylated psoralen that acts as a potent inhibitors of debenzylation activity of CYP3A4 enzyme with an IC50 value of 24.92 uM. Recent studies suggest that it may have antiproliferative and anticancer properties.
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