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865231-46-5 (AMG 837)

1

Identification

AMG 837 AMG 837
Name AMG 837
Formula C26H21F3O3
MW 438.44
CAS No. 865231-46-5
EINECS
Smiles OC(C[[email protected]](C#CC)C1=CC=C(C=C1)OCC2=CC=CC(C3=CC=C(C(F)(F)F)C=C3)=C2)=O
Synonyms AMG-837;AMG837; (S)-3-(4-((4'-(trifluoromethyl)-[1,1'-biphenyl]-3-yl)methoxy)phenyl)hex-4-ynoic acid
InChI InChI=1S/C26H21F3O3/c1-2-4-21(16-25(30)31)20-9-13-24(14-10-20)32-17-18-5-3-6-22(15-18)19-7-11-23(12-8-19)26(27,28)29/h3,5-15,21H,16-17H2,1H3,(H,30,31)/t21-/m0/s1
2

Introduction

AMG 837 is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents. IC50 value: 13 nM (EC50) [1] Target: GPR40 agonist AMG 837 displayed the expected two-fold increase in potency on GPR4 (EC50 = 13 [±7] nM) compared to the racemic compound and its activity crossed over to the rat and mouse forms of GPR40 (EC50 = 23 and 13 nM, respectively).

Background Information

AMG 837 is a potent, orally bioavailable GPR40 agonist with EC50 of 14 nM. ......by AbMole BioScience
AMG 837 sodium salt is a potent GPR40 agonist with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents. It displayed the expected two-fold increase in potency on GPR4 compared to the racemic compound ......by BOC Sciences
AMG-837 is a potent, orally bioavailable GPR40 agonist. AMG 837 was a potent partial agonist in the calcium flux assay on the GPR40 receptor and potentiated glucose stimulated insulin secretion in vitro and in vivo. Acute administration of AMG 837 lowered glucose excursions and increased glucose stimulated insulin secretion during glucose tolerance tests in both normal and Zucker fatty rats. The improvement in glucose excursions persisted following daily dosing of AMG 837 for 21-days in Zucker fatty rats. Preclinical studies demonstrated that AMG 837 was a potent GPR40 partial agonist which lowered post-prandial glucose levels. These studies support the potential utility of AMG 837 for the treatment of type 2 diabetes. (PLoS One. 2011;6(11):e27270). Shelf life: >2 years if stored properly Drug formulation: ......by MedKoo Biosciences, Inc.
A potent partial GPR40 (FFA1) agonist (EC50=13 nM for hGPR40); exhibits superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents; orally bioactive. ......by ProbeChem
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

4

Physical and Chemical Properties

Appearance: EBNumber:EB000013304

Storage condition

Solubility

DMSO by MedChemexpress Co., Ltd.
5

Mechanism and Indication

Signaling Pathways GPCR/G Protein
Target GPR40
Research Area Metabolic Disease
Indications
6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
AMG 837 - Not Found
AMG 837 - No Development Reported
7

Safety Data of AMG 837

8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AbMole BioScience 10mg/USD180(In stock) USA
Ark Pharm, Inc. 1g/USD2471() USA
BOC Sciences
Biochempartner Co., Ltd China
CHEMSCENE, LLC 5mg/USD156();10mg/USD228() USA
Cayman Chemical Company USA
Matrix Scientific 250mg/USD742() USA
MedChemexpress Co., Ltd. 5mg/USD156();10mg/USD228() USA
MedKoo Biosciences, Inc. USA
ProbeChem
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD156();10mg/USD228() China
Shanghai XingMo Biotechnology Co., Ltd. 1g/USD1400(In stock) CHINA
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Related Products

Other Forms of 865231-46-5

Name CAS No Formula MW
AMG 837 (calcium hydrate) 1259389-38-2 C26H22F3O4- 455.45
AMG 837 (sodium salt) 865231-45-4 C26H20F3NaO3 460.42

Recommended Compounds in GPR40

Name CAS No Formula MW
AMG 837 (calcium hydrate) 1259389-38-2 C26H22F3O4- 455.45
AMG 837 (sodium salt) 865231-45-4 C26H20F3NaO3 460.42
GPR40 Activator 1 1309435-60-6 C31H31NO3S 497.65
TUG-770 1402601-82-4 C19H14FNO2 307.32
GW9508 885101-89-3 C22H21NO3 347.41
TAK-875 1000413-72-8 C29H32O7S 524.63
GW-1100 306974-70-9 C27H25FN4O4S 520.58
GPR40 Activator 2 1312787-30-6 C28H29NO6S2 539.66
DC260126 346692-04-4 C32H31N5O 501.62
M-I C19H22O5S 362.44
T-1676427 1000414-39-0 C29H32O8S 540.62
JTT-851 C23H28O3 352.47
Astellas C27H30N4O4 474.55
MK-2305 905723-46-8 C19H13ClF3NO4S 443.82
Mochida 1469495-84-8 C30H35NO6S 537.67
BMS-986118 1610562-74-7 C25H28ClF3N4O4 540.96
AM-6226 C32H36F2O4 522.62
GPR40 agonist 1 1312788-44-5 C24H20O3 356.41
GPR40 agonist 2 C25H22O3 370.44
GPR40 agonist 3 C23H18O3 342.39

Recommended Compounds in Same Indication

Name CAS No Formula MW
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Route of Synthesis

12

References

13

More Information

AMG 837

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