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Search Results for " microsomes "

20

Compounds

Cat No. Product Name Synonyms Targets
T12490 Pitavastatin lactone Others
Pitavastatin lactone is a major Pitavastatin metabolite in humans. Pitavastatin is a potent competitive inhibitor of HMG-CoA reductase little metabolized in hepatic microsomes.
T6031 GNE0877 GNE 0877,GNE-0877 LRRK2
GNE0877 (GNE 0877) is a highly effective and specific leucine-rich repeat kinase 2 (LRRK2) inhibitor (Ki: 0.7 nM).
T6714 URB-597 KDS-4103,FAAH Inhibitor II Mitophagy , FAAH , Autophagy
URB-597 (FAAH Inhibitor II) is an effective, orally bioavailable FAAH inhibitor (IC50: 4.6 nM), and no effect on other cannabinoid-related targets.
T3424 Ezutromid BMN 195,VOX-C1100,SMT C1100 Others
Ezutromid (BMN 195) is a translation modulator of Small utrophin (EC50: 0.4 uM). Ezutromid is an orally bioavailable small molecule that transcriptionally upregulates the utrophin gene, increasing both utrophin mRNA and ...
T13373 YM17E Acyltransferase , AChR
YM17E is an inhibitor of ACAT with IC50 of 44 nM in rabbit liver microsomes in vitro.
T20373 1-Phenylpyrrole NSC16581,NSC-16581,NSC 16581 Others
1-Phenylpyrrole (NSC-16581) is an inhibitor of CYP450 dependant monooxygenase activity in microsomes from rat liver.
T22148 (S)-Lisofylline Others
(S)-Lisofylline is the inactive optical enantiomer of (R)-lisofylline which is an anti-inflammatory agent. (S)-Lisofylline is exclusively converted to pentoxifylline in human liver microsomes.
T19526 Pradefovir mesylate Pradefovir mesilate,Remofovir mesylate,Hepavir B P450
Pradefovir mesylate (Hepavir B) is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with Km of 60 μM.
T73040 CYP1B1-IN-4 P450
CYP1B1-IN-4, a 2,4-diarylthiazole compound, exhibits selective inhibition of CYP1B1 (IC50=0.2 nM), demonstrating minimal cytotoxicity and high stability in human and rat liver microsomes [1].
T11339 Furegrelate sodium U-63557A PPAR
Furegrelate sodium (U-63557A) is a selective thromboxane synthase inhibitor with oral activity. Furegrelate sodium(U-63557A) inhibits thromboxane A2 (TXA2) synthase in human platelet microsomes with an IC50 of 15 nM.
T27918 LY 43578 LY-43578,LY43578 P450 , Aromatase
LY 43578 is an orally active aromatase inhibitor. LY43578 could inhibit O-demethylation of P-450-dependent p-nitroanisole and N-demethylation of ethylmorphine (IC50 of 0.3 and 5 μm, respectively) in rat liver microsomes....
T14983 Clomethiazole Distraneurin,Chlormethiazole,5-(2-CHLOROETHYL)-4-METHYLTHIAZOLE P450 , GABA Receptor
Clomethiazole (Distraneurin) is an orally active GABAA agonist and it is an anticonvulsant agent. It also has the potential for treating convulsive status epilepticus. Chlormethiazole inhibits cytochrome P450 isoforms: C...
T27371 FR-167356 FR167356,FR 167356 ATPase
FR-167356 is a specific inhibitor of a3 isoform vacuolar type H⁺-ATPase with IC50s of 170 nM, 370 nM and 220 nM for osteoclast plasma membranes, renal brush border membranes and macrophage microsomes. FR-167356 reduces b...
T21254 Vonoprazan Fumarate TAK-438,TAK 438,Vonoprazan Fumurate,TAK438 Proton pump
Vonoprazan Fumarate (TAK438) , a novel potassium-competitive acid blocker, inhibits gastric acid secretion. Vonoprazan Fumarate (TAK438) inhibited H+,K+-ATPase activity in porcine gastric microsomes with IC50 value of 19...
T3647 HTHQ HX 1171,HTHQ(1-O-Hexyl-2,3,5-trimethylhydroquinone),1-O-hexyl-2,3,5-trimethylhydroquinone Reactive Oxygen Species
HTHQ (HTHQ(1-O-Hexyl-2,3,5-trimethylhydroquinone)), a hydroquinone monoalkyl ether, is an effective anti-oxidative agent. HTHQ is a potent anti-lipid-peroxidative compound and its antioxidation activity to be extremely e...
T28449 Pradefovir ICN-2001-3,MB-6866,ICN-20013,MB-06866,Remofovir HBV
Pradefovir (Remofovir) is a reverse transcriptase inhibitor potentially for treatment of chronic HBV infection. Pradefovir is also a liver-targeted prodrug of adefovir. After metabolic activation, Pradefovir was converte...
T37149 Carbamazepine 10,11-epoxide Others
Carbamazepine 10,11-epoxide is an active metabolite of the anticonvulsant carbamazepine.1,2It is formed from carbamazepine by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP2C8 in microsomes prepared from HepG2 cells e...
T23549 YM 511 P450 , Aromatase
YM 511 is a highly specific non-steroidal aromatase inhibitor. YM 511 inhibits aromatase activities in microsomes from rat ovary and human placenta competitively (IC50s of 0.4 and 0.12 nM, respectively). YM 511 slightly ...
T27061 CP-24879 hydrochloride CP-24879 HCl Others
CP-24879 hydrochloride (CP-24879 HCl), a Δ5D/Δ6D dual-inhibitor, can significantly reduce intracellular lipid accumulation and inflammatory injury in hepatocytes. CP-24879 hydrochloride exhibits superior antisteatotic an...
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.
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