microsomal

Prochloraz (Prelude) is a broad-spectrum contact imidazole fungicide. Prochloraz inhibits human placental microsomal aromatase in vitro (IC50 = 40 nM). Prochloraz also acts as an estrogen receptor (IC50s = 25 μM) and androgen receptor (IC50 = 4 μM) antagonist, and activates aryl hydrocarbon receptors (EC50 = 1 μM).

RPR107393 free base is a selective and potent inhibitor of squalene synthase (SQS) for the study of neurological disorders and endocrine and metabolic disorders.

Dirlotapide (CP742033) is an intestinal selective microsomal triglyceride transfer protein (MTP) inhibitor. It reduces body weight in diabetic dogs.Dirlotapide reduces food intake in a dose-dependent manner, possibly by increasing the release of peptide YY into the circulation.

PF-9184 is a potent and selective inhibitor of human microsomal prostaglandin E synthase-1 (mPGES-1) with an IC50 of 16.5 nM, and it inhibits IL-1β-induced PGE2 synthesis in vitro.

mPGES-1 Inhibitor-1 is a novel selective inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1) with anti-inflammatory and analgesic activity for the study of acute liver injury.

BMS-212122 (UNII-0Z473OO6GB) is a potent inhibitor of microsomal triglyceride transfer protein (MTP) and has shown hypolipidemic effects in animal studies.BMS-212122 significantly reduced lipid content and monocyte-derived (CD68+) cells in atherosclerotic plaques.

Granotapide is a microsomal triglyceride transfer protein (MTP) inhibitor that treats and rather prevents atherosclerosis, coronary artery disease, metabolic syndrome, obesity, diabetes mellitus, prediabetes mellitus, and hypertension.

Ifosfamide (NSC-109724) alkylates and forms DNA crosslinks, thereby preventing DNA strand separation and DNA replication. Ifosfamide is a synthetic analog of the nitrogen mustard cyclophosphamide with antineoplastic activity. This agent is a prodrug that must be activated through hydroxylation by hepatic microsomal enzymes.

(E)-Oct-2-enoic acid (2-Octenoate) is an organic acid produced by hepatic microsomal oxidation of aliphatic aldehydes and is a metabolite naturally present in urine and plasma.

Lomitapide (AEGR-733) is a small molecule inhibitor of microsomal triglyceride transfer protein (MTP), an enzyme located in the lumen of the endoplasmic reticulum responsible for absorbing dietary lipids and transferring triglycerides onto apolipoprotein B (apo-B) in the assembly of very-low-density lipoprotein.

CAY10434 is an active inhibitor of CYP4A hydroxylase with an IC50 value of 8.8 nM in human kidney microsomal test. The maximum contractile value (Emax) of CAY 10434 was 6764 mg in improving the contractile process of angiotensin II.

Estrone O-sulfamate (Estrone 3-O-sulfamate) is a potent inhibitor of steroid sulfatase (STS), showing IC50 values of 18 nM as a placental microsomal inhibitor (P.M.) and 0.83 nM in MCF-7 cells. Estrone O-sulfamate can be used to study cancer.

CHIKV-IN-2, a chemical compound, exhibits potent inhibitory activity against the enzyme Dihydroorotate Dehydrogenase (DHODH), crucial for pyrimidine synthesis affecting various viruses' replication. It serves as an effective Chikungunya virus (CHIKV) inhibitor, demonstrating significant cellular antiviral activity (EC90=270 nM) and enhanced liver microsomal stability[1].

Implitapide Racemate, the racemate of Implitapide, is an inhibitor of microsomal triglyceride transfer protein (MTP).

mPGES1-IN-3 is a potent and selective inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1) .

SC-26196 is an orally active inhibitor of Delta6 desaturase (D6D) with IC50 of 0.2 µM in a rat liver microsomal assay, with antiinflammatory properties.

CP-319340 free base is an inhibitor of microsomal triglyceride transfer protein (MTP).

Beauvericin, a Fusarium mycotoxin, inhibits acyl-CoA:cholesterol acyltransferase (ACAT) in rat liver microsomal enzyme assays with an IC50 value of 3 μM.

Implitapide is an inhibitor of microsomal triglyceride transfer protein (MTP).

PF-02575799 is an inhibitor of microsomal triglyceride transfer protein (MTP) (IC50: 0.77±0.29 nM).

PF-4693627 is an effective and selective microsomal prostaglandin E synthase-1 inhibitor (IC50=3 nM). It is used for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA).

SCH28080 is a reversible and K+-competitive inhibitor of gastric H+/K+-ATPase with an IC50 value of 20 nM (rabbit microsomal membrane).SCH28080 is a potent inhibitor of acid secretion in vivo with anti-ulcer activity, anti-secretory and cytoprotective activity.

SR144528 is an antagonist of the CB2 receptor (Ki = 0.6 nM) and inhibits microsomal ACAT activity (IC50 = 3.6 μM).

Mcl-1 inhibitor20 (compound 47) is an Mcl-1 antagonist with anti-leukemia properties. It binds to the BH3 docking groove of Mcl-1 (Ki=24 nM), occupies the P1 pocket, and interacts with Lys234 and Val249. Mcl-1 inhibitor20 also exhibits good microsomal stability, favorable pharmacokinetic properties, and low cardiotoxicity.