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959122-11-3 (A 922500)

1

Identification

A 922500 A 922500
Name A 922500
Formula C26H24N2O4
MW 428.48
CAS No. 959122-11-3
EINECS
Smiles O=C(NC1=CC=C(C2=CC=C(C([[email protected]@H]3CCC[[email protected]]3C(O)=O)=O)C=C2)C=C1)NC4=CC=CC=C4
Synonyms DGAT-1 Inhibitor 4a;A-922500; A922500; (1R,2R)-2-(4'-(3-phenylureido)-[1,1'-biphenyl]-4-carbonyl)cyclopentanecarboxylic acid
InChI InChI=1S/C26H24N2O4/c29-24(22-7-4-8-23(22)25(30)31)19-11-9-17(10-12-19)18-13-15-21(16-14-18)28-26(32)27-20-5-2-1-3-6-20/h1-3,5-6,9-16,22-23H,4,7-8H2,(H,30,31)(H2,27,28,32)/t22-,23-/m1/s1
2

Introduction

A 922500 is a potent, selective, and orally bioavailable DGAT-1 inhibitor with IC50 values of 7 nM and 24 nM for human and mouse DGAT-1 respectively. IC50 Value: 7 nM(human DGAT-1); 24 nM(DGAT-1) [1] Target: DGAT-1 in vitro: A 922500 potently inhibits huDGAT-1 and mseDGAT-1 [1].

Background Information

A922500 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. ......by BOC Sciences
A 922500 is a potent, selective, and orally bioavailable DGAT-1 inhibitor with IC50 values of 7 nM and 24 nM for human and mouse DGAT-1 respectively. IC50 Value: 7 nM(human DGAT-1); 24 nM(DGAT-1) [1] Target: DGAT-1 in vitro: A 922500 potently inhibits huDGAT-1 and mseDGAT-1 [1]. A 922500 inhibits the phylogenetic family members acyl coenzyme A cholesterol acyltransferase-1 and -2 with IC50 of 296 μM [2]. in vivo: Zucker fatty rats and diet-induced dyslipidemic hamsters were dosed orally with A-922500 (0.03, 0.3, and 3-mg/kg), a potent and selective DGAT-1 inhibitor, for 14 days. Serum triglycerides were significantly reduced by the 3 mg/kg dose of the DGAT-1 inhibitor in both the Zucker fatty rat (39%) and hyperlipidemic hamster (53%) [1]. A 922500 confers weight loss and a reduction in liver triglycerides when dosed chronically in DIO mice and depletes serum triglycerides following a lipid challenge in a dose-dependent manner, thus, reproducing major phenotypical characteristics of DGAT-1(-/-) mice [2]. The potent and selective DGAT-1 inhibitorA-922500 (0.03, 0.3 and 3 mg/kg, p.o.), dose-dependently attenuated the maximal postprandial rise in serum triglyceride concentrations in all species tested. At the highest dose of DGAT-1 inhibitor, the postprandial triglyceride response was abolished [3]. Clinical trial: ......by MedChemexpress Co., Ltd.
A922500 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. ......by Selleck Chemicals LLC
A922500 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. ......by Target Molecule Corp.
Diacylglycerol acyltransferase 1 (DGAT-1) inhibitor (IC50 values are 7 and 24 nM at human and mouse DGAT-1 respectively) that is devoid of activity at DGAT-2, ACAT1 or ACAT2. Induces significant weight loss without altering food intake, and decreases liver and plasma triglyceride levels in vivo. Orally active. ......by Tocris Bioscience Inc.
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

Animal Models Thirteen-week-old male Golden Syrian hamsters with hyperlipidemia, Ten-week-old Male Zucker fatty rats
Dosage 0.03, 0.3, and 3 mg/kg
Formulation Polyethylene glycol/hydroxypropyl-β-cyclodextrin (10% w/v)
Administration Oral gavage
Source Selleck Chemicals LLC
4

Physical and Chemical Properties

Appearance:White to off-white solid EBNumber:EB000028858

Storage condition

Desiccate at +4°C by Tocris Bioscience Inc.

Solubility

DMSO 86 mg/ml; Water < 1 mg/ml by MedChemexpress Co., Ltd.
(25°C) * In vitro DMSO 86 mg/mL (200.7 mM); Water<1 mg/mL (<1 mM); Ethanol<1 mg/mL (<1 mM); In vivo 15% Captisol20 mg/mL by Selleck Chemicals LLC
Soluble to 50 mM in DMSO by Tocris Bioscience Inc.
5

Mechanism and Indication

Signaling Pathways Metabolic Enzyme/Protease
Target DGAT
Research Area Metabolic Disease
Indications
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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
A 922500 - Discovery
A 922500 - No Development Reported
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Safety Data of A 922500

8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
BOC Sciences
CHEMSCENE, LLC 5mg/USD105(In stock);10mg/USD147(In stock);50mg/USD469(In stock);100mg/USD700(In stock) USA
MedChemexpress Co., Ltd. 5mg/USD105(In stock);10mg/USD147(In stock);50mg/USD469(In stock);100mg/USD700(In stock) USA
Selleck Chemicals LLC 5mg/USD150(In stock);10mg/USD210(In stock);10mM/1mLIn DMSO/USD260(In stock);50mg/USD670(In stock);200mg/USD1780(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD105(In stock);10mg/USD147(In stock);50mg/USD469(In stock);100mg/USD700(In stock) China
Target Molecule Corp. 5mg/USD76();100mg/USD548() USA
Tocris Bioscience Inc. USA
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Related Products

Other Forms of 959122-11-3

Name CAS No Formula MW
Nigericin sodium salt 28643-80-3 C40H67NaO11 746.94
BH3I-1 300817-68-9 C15H14BrNO3S2 400.31
TPO agonist 1 1033040-23-1 C25H22N8O2 466.49
Ticlopidine 55142-85-3 C14H14ClNS 263.79
Benzamide, 4-methoxy-N-[2-[2-(4-propylphenyl)-2H-tetrazol-5-yl]phenyl]- 1709856-28-9 C24H23N5O2 413.47
SHP099 (hydrochloride) 1801747-11-4 C16H20Cl3N5 388.72
SHP099 1801747-42-1 C16H19Cl2N5 352.26
GR63799 106342-69-2 C34H37NO8 587.66
Brevianamide F 38136-70-8 C16H17N3O2 283.33
NKL 22 537034-15-4 C19H23N3O2 325.4
FPTQ 864863-72-9 C17H12FN5 305.31

Recommended Compounds in DGAT

Name CAS No Formula MW
AZD7687 1166827-44-6 C21H25N3O3 367.44
LCQ-908 956136-95-1 C25H24F3N3O2 455.47
DGAT-1 inhibitor 2 942999-61-3 C24H28N4O3 420.5
ABT-046 1031336-60-3 C20H22N4O2 350.41
PF-04620110 1109276-89-2 C21H24N4O4 396.44
T863 701232-20-4 C22H26N4O3 394.47
Xanthohumol 6754-58-1 C21H22O5 354.4
DGAT1-IN-1 1449779-49-0 C30H28F3N3O4 551.56

Recommended Compounds in Same Indication

Name CAS No Formula MW
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Route of Synthesis

12

References

13

More Information

A 922500

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