Acyltransferase-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/DGAT.html AcyltransferaseDiacylglycerol acyltransferase; Diglyceride acyltransferase; acyl-CoA:cholesterol acyltransferase; mono-acylglycerol acyltransferaseAcyltransferase (AT) catalyzes the transfer of an acyl moiety from acyl-coenzyme A (acyl-CoA) to an acce

2、ptor. Acyltransferases playimportant roles in the maintenance of homeostasis in the human body and have been linked to various diseases. TheAcyltransferase family includes acyl-CoA:cholesterol AT (ACAT), diacylglycerol AT (DGAT), and monoacylglycerol AT (MGAT) for themetabolism of lipids.ACAT (acyl-

3、coenzyme A:cholesterol acyltransferase) is an intracellular enzyme that catalyzes the formation of cholesterol estersfrom cholesterol and fatty acyl-coenzyme A. In mammals, two isoenzymes, ACAT1 and ACAT2, encoded by two different genes,exist. ACATs play important roles in cellular cholesterol homeo

4、stasis in various tissues.DGAT (acyl-CoA:diacylglycerol acyltransferase) is an integral membrane enzyme that catalyses the last step of triacylglycerolsynthesis from diacylglycerol and acyl-CoA. DGAT activity resides mainly in two distinct membrane bound polypeptides, known asDGAT1 and DGAT2.MGAT (a

5、cyl-CoA:monoacylglycerol acyltransferase) catalyzes the synthesis of diacylglycerol, the precursor of physiologicallyimportant lipids such as triacylglycerol and phospholipids. In the intestine, MGAT plays a major role in the absorption of dietary fatbecause resynthesis of triacylglycerol is require

6、d for the assembly of lipoproteins that transport absorbed fat to other tissues.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/DGAT.html Acyltransferase HYPERLINK https:/www.MedChemE/Targets/DGAT.html HYPERLINK https:/www.MedChemE/Targets/DGAT.html Inhibitors HYPERLINK https:/www.MedChemE/Targ

7、ets/DGAT.html HYPERLINK https:/www.MedChemE/Targets/DGAT.html & HYPERLINK https:/www.MedChemE/Targets/DGAT.html HYPERLINK https:/www.MedChemE/Targets/DGAT.html Activators HYPERLINK https:/www.MedChemE/rac-osmi-1.html (Rac)-OSMI-1 HYPERLINK https:/www.MedChemE/rac-osmi-1.html HYPERLINK https:/www.Med

8、ChemE/1-methyl-2-4z-7z-4-7-tridecadienyl-4-1h-quinolone.html 1-Methyl-2-(4Z,7Z)-4,7-tridecadienyl-4(1H)-quinoloneCat. No.: HY-119738A Cat. No.: HY-N9530(Rac)-OSMI-1 is the racemate of OSMI-1. OSMI-1 isa cell-permeable O-GlcNAc transferase (OGT)inhibitor with an IC value of 2.7 M.501-Methyl-2-(4Z,7Z)

9、-4,7-tridecadienyl-4(1H)-quinolone, a quinolone alkaloid, is a diacylglycerolacyltransferase inhibitor and angiotensin IIreceptor blocker, with IC s of 20.1 M and 34.150M, respectively.Purity: 96.05%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mgPurity: 98%Clinical Data: No Dev

10、elopment ReportedSize: 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/10-12-tricosadiynoic-acid.html 10,12-Tricosadiynoic HYPERLINK https:/www.MedChemE/10-12-tricosadiynoic-acid.html HYPERLINK https:/www.MedChemE/10-12-tricosadiynoic-acid.html acid HYPERLINK https:/www.MedChemE/10-12-tricosadiynoi

11、c-acid.html HYPERLINK https:/www.MedChemE/2-fluoropalmitic-acid.html 2-Fluoropalmitic HYPERLINK https:/www.MedChemE/2-fluoropalmitic-acid.html HYPERLINK https:/www.MedChemE/2-fluoropalmitic-acid.html acidCat. No.: HY-135425 Cat. No.: HY-11765110,12-Tricosadiynoic acid is a highly specific,selective,

12、 high affinity and orally active acyl-CoAoxidase-1 (ACOX1) inhibitor. 10,12-Tricosadiynoicacid can treat high fat diet- or obesity-inducedmetabolic diseases by improving mitochondriallipid and ROS metabolism.2-Fluoropalmitic acid, an acyl-CoA synthetaseinhibitor, acts as a candidate anti-glioma agen

13、t.2-Fluoropalmitic acid suppresses the viability andstem-like phenotype of glioma stem cells (GSCs).2-Fluoropalmitic acid also inhibits proliferationand invasion of glioma cell lines.Purity: 96.71%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical

14、Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/2-Furoic_acid.html 2-Furoic HYPERLINK https:/www.MedChemE/2-Furoic_acid.html HYPERLINK https:/www.MedChemE/2-Furoic_acid.html acid(Furan-2-carboxylic acid) Cat. No.: HY-W012946 HYPERLINK https:/www.MedChemE/24-methylenechole

15、sterol.html 24-Methylenecholesterol(Ostreasterol) Cat. No.: HY-1339682-Furoic acid (Furan-2-carboxylic acid) is anorganic compound produced through furfuraloxidation. 2-Furoic acid exhibits hypolipidemiceffet, lowers both serum cholesterol and serumtriglyceride levels in rats.24-Methylenecholesterol

16、 (Ostreasterol), a naturalmarine sterol, stimulates cholesterolacyltransferase in human macrophages.24-Methylenecholesterol possess anti-aging effectsin yeast. 24-methylenecholesterol enhances honeybee longevity and improves nurse bee physiology.Purity: 98.0%Clinical Data: No Development ReportedSiz

17、e: 10 mM 1 mL, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/A-922500.html A HYPERLINK https:/www.MedChemE/A-922500.html HYPERLINK https:/www.MedChemE/A-922500.html 922500 HYPERLINK https:/www.MedChemE/A-922500.html HYPERLINK https:/www

18、.MedChemE/abt-046.html ABT-046(DGAT-1 Inhibitor 4a) Cat. No.: HY-10038Cat. No.: HY-15197A 922500 (DGAT-1 Inhibitor 4a) is a potent,selective, and orally bioavailable diacylglycerolacyltransferase 1 (DGAT-1) inhibitor with IC s50of 9 and 22 nM against human and mouse DGAT-1,respectively.ABT-046 is a

19、potent, selective, and orallyefficacious acyl CoA:diacylglycerolacyltransferase 1 (DGAT-1) inhibitor (IC = 850nM).Purity: 98.50%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98.13%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg,

20、100 mg HYPERLINK https:/www.MedChemE/Benzeneacetamide,_N-2,3-dihydro-2-_4-hydroxyphenyl_-1H-inden-1-yl-_alpha_-phenyl-,_cis-.html ACAT-IN-1 HYPERLINK https:/www.MedChemE/Benzeneacetamide,_N-2,3-dihydro-2-_4-hydroxyphenyl_-1H-inden-1-yl-_alpha_-phenyl-,_cis-.html HYPERLINK https:/www.MedChemE/Benzene

21、acetamide,_N-2,3-dihydro-2-_4-hydroxyphenyl_-1H-inden-1-yl-_alpha_-phenyl-,_cis-.html cis HYPERLINK https:/www.MedChemE/Benzeneacetamide,_N-2,3-dihydro-2-_4-hydroxyphenyl_-1H-inden-1-yl-_alpha_-phenyl-,_cis-.html HYPERLINK https:/www.MedChemE/Benzeneacetamide,_N-2,3-dihydro-2-_4-hydroxyphenyl_-1H-in

22、den-1-yl-_alpha_-phenyl-,_cis-.html isomer HYPERLINK https:/www.MedChemE/Benzeneacetamide,_N-2,3-dihydro-2-_4-hydroxyphenyl_-1H-inden-1-yl-_alpha_-phenyl-,_cis-.html HYPERLINK https:/www.MedChemE/acat-in-10.html ACAT-IN-10Cat. No.: HY-101648 Cat. No.: HY-139027ACAT-IN-1 cis isomer is a potent ACAT i

23、nhibitorwith an IC of 100 nM.50ACAT-IN-10 is an acyl-Coenzyme A:cholesterolacyltransferase (ACAT) inhibitor extracted frompatent EP1236468A1, example 197. ACAT-IN-10 weaklyinhibits NF-B mediated transcription.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data:

24、No Development ReportedSize: 1 mg, 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/acat-in-10-dihydrochloride.html ACAT-IN-10 HYPERLINK https:/www.MedChemE/acat-in-10-dihydrochloride.html HYPERLINK https:/www.MedChemE/acat-in-10-dihydrochloride.html dihyd

25、rochloride HYPERLINK https:/www.MedChemE/acat-in-10-dihydrochloride.html HYPERLINK https:/www.MedChemE/acat-in-2.html ACAT-IN-2Cat. No.: HY-139027A Cat. No.: HY-139019ACAT-IN-10 dihydrochloride is an acyl-CoenzymeA:cholesterol acyltransferase (ACAT) inhibitorextracted from patent EP1236468A1, exampl

26、e 197.ACAT-IN-10 dihydrochloride weakly inhibits NF-Bmediated transcription.ACAT-IN-2 is an acyl-Coenzyme A:cholesterolacyltransferase (ACAT) inhibitor extracted frompatent EP1236468A1, example 187. ACAT-IN-2inhibits NF-B mediated transcription.Purity: 98%Clinical Data: No Development ReportedSize:

27、1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/acat-in-3.html ACAT-IN-3 HYPERLINK https:/www.MedChemE/acat-in-3.html HYPERLINK https:/www.MedChemE/acat-in-4.html ACAT-IN-4Cat. No.: HY-139020 Cat. No.: HY-139021ACAT-IN-3 is an acyl-Coenzyme A

28、:cholesterolacyltransferase (ACAT) inhibitor. ACAT-IN-3inhibits NF-B mediated transcription.ACAT-IN-4 (Example 208) is an acyl-CoenzymeA:cholesterol acyltransferase (ACAT) inhibitor.ACAT-IN-4 inhibits NF-B mediated transcription.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity

29、: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/acat-in-4-hydrochloride.html ACAT-IN-4 HYPERLINK https:/www.MedChemE/acat-in-4-hydrochloride.html HYPERLINK https:/www.MedChemE/acat-in-4-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/acat-in-4

30、-hydrochloride.html HYPERLINK https:/www.MedChemE/acat-in-5.html ACAT-IN-5Cat. No.: HY-139021A Cat. No.: HY-139022ACAT-IN-4 hydrochloride (Example 208) is anacyl-Coenzyme A:cholesterol acyltransferase(ACAT) inhibitor. ACAT-IN-4 hydrochlorideinhibits NF-B mediated transcription.ACAT-IN-5 (example 19)

31、 is an acyl-CoenzymeA:cholesterol acyltransferase (ACAT) inhibitor.ACAT-IN-5 inhibits NF-B mediated transcription.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/acat-in-6.html ACAT-IN-6

32、HYPERLINK https:/www.MedChemE/acat-in-6.html HYPERLINK https:/www.MedChemE/acat-in-7.html ACAT-IN-7Cat. No.: HY-139023 Cat. No.: HY-139024ACAT-IN-6 is an acyl-Coenzyme A:cholesterolacyltransferase (ACAT) inhibitor extracted frompatent EP1236468A1, example 200. ACAT-IN-6potently inhibits NF-B mediate

33、d transcription.ACAT-IN-7 is an acyl-Coenzyme A:cholesterolacyltransferase (ACAT) inhibitor. ACAT-IN-7inhibits NF-B mediated transcription.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/

34、acat-in-8.html ACAT-IN-8 HYPERLINK https:/www.MedChemE/acat-in-8.html HYPERLINK https:/www.MedChemE/acat-in-9.html ACAT-IN-9Cat. No.: HY-139025 Cat. No.: HY-139026ACAT-IN-8 (example 206) is an acyl-CoenzymeA:cholesterol acyltransferase (ACAT) inhibitor.ACAT-IN-8 inhibits NF-B mediated transcription.

35、ACAT-IN-9 is an acyl-Coenzyme A:cholesterolacyltransferase (ACAT) inhibitor extracted frompatent EP1236468A1, example 207. ACAT-IN-9inhibits NF-B mediated transcription.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgw

36、ww.MedChemE 3 HYPERLINK https:/www.MedChemE/amidepsine-a.html Amidepsine HYPERLINK https:/www.MedChemE/amidepsine-a.html HYPERLINK https:/www.MedChemE/amidepsine-a.html A HYPERLINK https:/www.MedChemE/amidepsine-a.html HYPERLINK https:/www.MedChemE/amidepsine-d.html Amidepsine HYPERLINK https:/www.M

37、edChemE/amidepsine-d.html HYPERLINK https:/www.MedChemE/amidepsine-d.html DCat. No.: HY-125319 Cat. No.: HY-129295Amidepsine A is a fungal metabolite isolated fromthe culture broth of Humicola sp. FO-2942 thatinhibits Diacylglycerol acyltransferases (DGAT)activity.Amidepsine D is a fungal metabolite

38、 isolated fromthe culture broth of Humicola sp. FO-2942 thatinhibits Diacylglycerol acyltransferases (DGAT)activity.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Avasimibe.html Avasimib

39、e(CI-1011; PD-148515) Cat. No.: HY-13215 HYPERLINK https:/www.MedChemE/azd3988.html AZD3988Cat. No.: HY-50861Avasimibe (CI-1011; PD-148515) is an orally activeacyl coenzyme A-cholesterol acyltransferase(ACAT; also called SOAT) inhibitor with IC s50of 24 and 9.2 M for ACAT1 and ACAT2,respectively. Av

40、asimibe can be used for theresearch of prostate cancer.AZD3988 is a diacylglycerol acyl transferase-1(DGAT-1) inhibitor with IC s of 6, 5, 11 nM for50human, rat, and mouse DGAT-1, respectively.Purity: 99.58%Clinical Data: Phase 3Size: 10 mM 1 mL, 10 mg, 50 mg, 100 mg, 200 mgPurity: 98.62%Clinical Da

41、ta: No Development ReportedSize: 10 mM 1 mL, 5 mg HYPERLINK https:/www.MedChemE/azd7687.html AZD7687 HYPERLINK https:/www.MedChemE/azd7687.html HYPERLINK https:/www.MedChemE/beauvericin.html BeauvericinCat. No.: HY-15497 Cat. No.: HY-N6739AZD7687 is a potent, selective, reversible andorally active d

42、iacylglycerol acyltransferase 1(DGAT1) inhibitor with an IC of 80 nM for50human DGAT1. AZD7687 can be used for type 2diabetes mellitus and obesity research.Beauvericin is a Fusarium mycotoxin.Beauvericin inhibits acyl-CoA: cholesterolacyltransferase (ACAT) activity with an IC of 350M in an enzyme as

43、say using rat liver microsomes.Purity: 99.04%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 99.11%Clinical Data: No Development ReportedSize: 5 mg HYPERLINK https:/www.MedChemE/bms-963272.html BMS-963272 HYPERLINK https:/www.MedChemE/bms-963272.html HYPERLINK https:/www.MedChemE/D

44、GAT-1-inhibitor-2.html DGAT-1 HYPERLINK https:/www.MedChemE/DGAT-1-inhibitor-2.html HYPERLINK https:/www.MedChemE/DGAT-1-inhibitor-2.html inhibitor HYPERLINK https:/www.MedChemE/DGAT-1-inhibitor-2.html HYPERLINK https:/www.MedChemE/DGAT-1-inhibitor-2.html 2Cat. No.: HY-132924 Cat. No.: HY-50670BMS-9

45、63272 is a potent, selective MGAT2inhibitor (IC = 7.1 nM) for the treatment of50metabolic disorders.DGAT-1 inhibitor 2 is an effective inhibitor ofDGAT-1;antiobesity agents. IC50 value: Target:DGAT-1 Acyl-CoA:diacylglycerol acyltransferase 1(DGAT1) is one of two known DGAT enzymes thatcatalyze the f

46、inal step in triglyceride synthesis.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 95.94%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/DGAT1-IN-1.html DGAT1-IN-1 HYPERLINK https:/www.MedChemE/DGAT1-IN-1.html HYPERLI

47、NK https:/www.MedChemE/dgat1-in-3.html DGAT1-IN-3Cat. No.: HY-12425 Cat. No.: HY-16434DGAT1-IN-1 is a potent DGAT1 inhibitor with IC50of 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/enniatin-a

48、.html Enniatin HYPERLINK https:/www.MedChemE/enniatin-a.html HYPERLINK https:/www.MedChemE/enniatin-a.html A HYPERLINK https:/www.MedChemE/enniatin-a.html HYPERLINK https:/www.MedChemE/enniatin-b.html Enniatin HYPERLINK https:/www.MedChemE/enniatin-b.html HYPERLINK https:/www.MedChemE/enniatin-b.htm

49、l BCat. No.: HY-N6702 Cat. No.: HY-N3806Enniatin A is a Fusarium mycotoxin. Enniatin Ainhibits acyl-CoA: cholesterol acyltransferase(ACAT) activity with an IC of 22 M in an50enzyme assay using rat liver microsomes.Enniatin B is a Fusarium mycotoxin. Enniatin Binhibits acyl-CoA: cholesterol acyltrans

50、ferase(ACAT) activity with an IC of 113 M in an50enzyme assay using rat liver microsomes. EnniatinsB decreases the activation of ERK (p44/p42).Purity: 98%Clinical Data: No Development ReportedSize: 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg HYPERLINK https:/www.MedChemE/enniatin

51、-b1.html Enniatin HYPERLINK https:/www.MedChemE/enniatin-b1.html HYPERLINK https:/www.MedChemE/enniatin-b1.html B1 HYPERLINK https:/www.MedChemE/enniatin-b1.html HYPERLINK https:/www.MedChemE/enniatin-complex.html Enniatin HYPERLINK https:/www.MedChemE/enniatin-complex.html HYPERLINK https:/www.MedC

52、hemE/enniatin-complex.html complexCat. No.: HY-N3807 Cat. No.: HY-N6706Enniatin B1 is a Fusarium mycotoxin. EnniatinB1 inhibits acyl-CoA: cholesterol acyltransferase(ACAT) activity with an IC of 73 M in an50enzyme assay using rat liver microsomes. EnniatinB1 crosss the blood-brain barrier.Enniatin c

53、omplex is a mixture ofcyclohexadepsipeptides isolated largely fromFusarium species of fungi, and has ionophoric,antibiotic, and in vitro hypolipidaemicproperties.Purity: 98%Clinical Data: No Development ReportedSize: 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg HYPERLINK ht

54、tps:/www.MedChemE/Urea,_N-2,6-bis_1-methylethyl_phenyl-N_acute_-_4R,5R_-4,5-dimethyl-2-4-_phosphonooxy_phenyl-1,3-dioxolan-2-ylmethyl-.html FCE HYPERLINK https:/www.MedChemE/Urea,_N-2,6-bis_1-methylethyl_phenyl-N_acute_-_4R,5R_-4,5-dimethyl-2-4-_phosphonooxy_phenyl-1,3-dioxolan-2-ylmethyl-.html HYPE

55、RLINK https:/www.MedChemE/Urea,_N-2,6-bis_1-methylethyl_phenyl-N_acute_-_4R,5R_-4,5-dimethyl-2-4-_phosphonooxy_phenyl-1,3-dioxolan-2-ylmethyl-.html 28654 HYPERLINK https:/www.MedChemE/Urea,_N-2,6-bis_1-methylethyl_phenyl-N_acute_-_4R,5R_-4,5-dimethyl-2-4-_phosphonooxy_phenyl-1,3-dioxolan-2-ylmethyl-

56、.html HYPERLINK https:/www.MedChemE/FR-190809.html FR-190809Cat. No.: HY-U00369 Cat. No.: HY-122078FCE 28654 is an inhibitor of acylCoA: cholesterolacyltransferase (ACAT), weakly inhibiting ACATin microsomes from rabbit aorta and intestine, andmonkey liver, with IC s of 2.55, 1.08 and 5.6950M, respc

57、etively.FR-190809 is a potent, nonadrenotoxic, orallyefficacious acyl-CoA:cholesterol O-acyltransferase(ACAT) inhibitor, with an IC of 45 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedCh

58、emE/fumonisin-b1.html Fumonisin HYPERLINK https:/www.MedChemE/fumonisin-b1.html HYPERLINK https:/www.MedChemE/fumonisin-b1.html B1 HYPERLINK https:/www.MedChemE/fumonisin-b1.html HYPERLINK https:/www.MedChemE/fumonisin-b2.html Fumonisin HYPERLINK https:/www.MedChemE/fumonisin-b2.html HYPERLINK https

59、:/www.MedChemE/fumonisin-b2.html B2Cat. No.: HY-N6719 Cat. No.: HY-N6723Fumonisin B1 is a mycotoxin produced fromFusarium moniliforme. Fumonisin B1 is apotent inhibitor of sphingosine N-acyltransferase(ceramide synthase) and disrupts de novosphingolipid biosynthesis. Fumonisin B1 is themost abundant

60、 and toxic fumonisin.Fumonisin B2, a mycotoxin produced by Fusariummoniliforme in various grains, is a potentinhibitor of sphingosine N-acyltransferase(ceramide synthase) and disrupts de novosphingolipid biosynthesis.Purity: 95.0%Clinical Data: No Development ReportedSize: 1 mgPurity: 99.0%Clinical