Acyltransferase

亜型選択性的な製品

ACAT ACAT1 ACAT2 DGAT DGAT1 DGAT2

Acyltransferase製品

All (12)
Acyltransferase阻害剤 (12)
新製品

製品コード	製品名称	製品説明	文献中Selleckの製品使用例
S2187	Avasimibe	Avasimibe inhibits ACAT with IC50 of 3.3 μM, also inhibits human P450 isoenzymes CYP2C9, CYP1A2 and CYP2C19 with IC50 of 2.9 μM, 13.9 μM and 26.5 μM, respectively.	Nat Commun, 2024, 15(1):8301 PLoS Pathog, 2023, 19(5):e1011323 Hepatol Int, 2023, 10.1007/s12072-023-10490-4
S7889	Xanthohumol	Xanthohumol, a prenylated chalcone from hop, inhibits COX-1 and COX-2 activity and shows chemopreventive effects. Xanthohumol inhibits diacylglycerol acyltransferase 1 (DGAT1) and DGAT2 with both IC50 of 40 μM. Xanthohumol is also a potent antiviral agent against a series of DNA and RNA viruses. Xanthohumol induces growth inhibition and apoptosis in cancer cells. Phase 1.	Antiviral Res, 2022, 207:105416 Oxid Med Cell Longev, 2022, 2022:9523491 Int J Mol Sci, 2021, 22(22)12134
S3021	Rimonabant (SR141716)	Rimonabant (SR141716) is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane. Rimonabant is also a dual inhibitor of acyl CoA:cholesterol acyltransferases(ACAT) 1 and 2 and inhibits mycobacterial MmpL3.	Toxicol Lett, 2023, 374:48-56 Int J Biol Sci, 2022, 18(4):1401-1414 Mol Metab, 2022, 65:101597
S2674	A922500	A922500 (DGAT-1 Inhibitor 4a) is an inhibitor for human and mouse DGAT-1 with IC50 of 7 nM and 24 nM, respectively, good selectivity over related acyltransferases, hERG, and a panel of anti-targets.	Nature, 2023, 621(7977):171-178 Nature, 2023, 621(7977):171-178 Cell Rep, 2022, 41(11):111827
S7192	PF-04620110	PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM.	J Pharm Biomed Anal, 2019, 170:176-186 J Cell Biol, 2018, 217(3):975-995
S0820	RP-64477	RP-64477 is a potent inhibitor of the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT). RP-64477 inhibits ACAT activity with IC50 of 113 nM, 503 nM, and 180 nM in human intestinal (CaCo-2), hepatic (HepG2) and monocytic (THP-1) cell assays, respectively.
S0359	T863 (DGAT-3)	T863 (DGAT-3) is a potent, selective and orally active inhibitor of Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) tht acts on the acyl-CoA binding site of DGAT1 and inhibits DGAT1-mediated triacylglycerol formation in cells.
S4189	Cyclandelate	Cyclandelate (BS 572,3,5,5-Trimethylcyclohexyl mandelate) is an effective inhibitor of rat hepatic acycloenzyme A: cholesterol acyltransferase (ACAT) with IC50 of 80 μM.
S9162	Rubimaillin	Rubimaillin (Mollugin), found in the Chinese medical plant Rubia cordifola, is a dual inhibitor of acetyl-CoA cholesterol acyltransferase 1 (ACAT1) and acetyl-CoA cholesterol acyltransferase 2 (ACAT2), but is more selective for the ACAT2 isozyme.
E0941	K-604 dihydrochloride	K-604 dihydrochloride, a potent and selective inhibitor of Acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1), suppresses the development of atherosclerosis in an animal model without affecting plasma cholesterol levels.
S9921	PF-06424439	PF-06424439 is a first orally bioavailable small-molecule inhibitor of DGAT2 with an IC50 of 14 nM.
S6971	Ervogastat	Ervogastat (PF-06865571, DGAT2i) is a potent diacylglycerol acyltransferase 2 (DGAT2) inhibitor that reduces steatosis and hepatic triglyceride levels in non-alcoholic steatohepatitis (NASH).
S2187	Avasimibe	Avasimibe inhibits ACAT with IC50 of 3.3 μM, also inhibits human P450 isoenzymes CYP2C9, CYP1A2 and CYP2C19 with IC50 of 2.9 μM, 13.9 μM and 26.5 μM, respectively.	Nat Commun, 2024, 15(1):8301 PLoS Pathog, 2023, 19(5):e1011323 Hepatol Int, 2023, 10.1007/s12072-023-10490-4
S7889	Xanthohumol	Xanthohumol, a prenylated chalcone from hop, inhibits COX-1 and COX-2 activity and shows chemopreventive effects. Xanthohumol inhibits diacylglycerol acyltransferase 1 (DGAT1) and DGAT2 with both IC50 of 40 μM. Xanthohumol is also a potent antiviral agent against a series of DNA and RNA viruses. Xanthohumol induces growth inhibition and apoptosis in cancer cells. Phase 1.	Antiviral Res, 2022, 207:105416 Oxid Med Cell Longev, 2022, 2022:9523491 Int J Mol Sci, 2021, 22(22)12134
S3021	Rimonabant (SR141716)	Rimonabant (SR141716) is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane. Rimonabant is also a dual inhibitor of acyl CoA:cholesterol acyltransferases(ACAT) 1 and 2 and inhibits mycobacterial MmpL3.	Toxicol Lett, 2023, 374:48-56 Int J Biol Sci, 2022, 18(4):1401-1414 Mol Metab, 2022, 65:101597
S2674	A922500	A922500 (DGAT-1 Inhibitor 4a) is an inhibitor for human and mouse DGAT-1 with IC50 of 7 nM and 24 nM, respectively, good selectivity over related acyltransferases, hERG, and a panel of anti-targets.	Nature, 2023, 621(7977):171-178 Nature, 2023, 621(7977):171-178 Cell Rep, 2022, 41(11):111827
S7192	PF-04620110	PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM.	J Pharm Biomed Anal, 2019, 170:176-186 J Cell Biol, 2018, 217(3):975-995
S0820	RP-64477	RP-64477 is a potent inhibitor of the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT). RP-64477 inhibits ACAT activity with IC50 of 113 nM, 503 nM, and 180 nM in human intestinal (CaCo-2), hepatic (HepG2) and monocytic (THP-1) cell assays, respectively.
S0359	T863 (DGAT-3)	T863 (DGAT-3) is a potent, selective and orally active inhibitor of Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) tht acts on the acyl-CoA binding site of DGAT1 and inhibits DGAT1-mediated triacylglycerol formation in cells.
S4189	Cyclandelate	Cyclandelate (BS 572,3,5,5-Trimethylcyclohexyl mandelate) is an effective inhibitor of rat hepatic acycloenzyme A: cholesterol acyltransferase (ACAT) with IC50 of 80 μM.
S9162	Rubimaillin	Rubimaillin (Mollugin), found in the Chinese medical plant Rubia cordifola, is a dual inhibitor of acetyl-CoA cholesterol acyltransferase 1 (ACAT1) and acetyl-CoA cholesterol acyltransferase 2 (ACAT2), but is more selective for the ACAT2 isozyme.
E0941	K-604 dihydrochloride	K-604 dihydrochloride, a potent and selective inhibitor of Acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1), suppresses the development of atherosclerosis in an animal model without affecting plasma cholesterol levels.
S9921	PF-06424439	PF-06424439 is a first orally bioavailable small-molecule inhibitor of DGAT2 with an IC50 of 14 nM.
S6971	Ervogastat	Ervogastat (PF-06865571, DGAT2i) is a potent diacylglycerol acyltransferase 2 (DGAT2) inhibitor that reduces steatosis and hepatic triglyceride levels in non-alcoholic steatohepatitis (NASH).

Acyltransferase阻害剤の選択性比較

Tags: ACAT