AMG 837 hemicalcium - CAS# 1291087-14-3


Catalog No. Size PriceQuantity
M16718-C Contact sales@xcessbio.com for quotation $100

Description

AMG 837 hemicalcium is a potent, orally bioavailable and partial agonist of GPR40/FFA1. AMG 837 hemicalcium inhibits specific [3H]AMG 837 binding at the human FFA1 receptor with a pIC50 of 8.13. AMG 837 hemicalcium could enhance insulin secretion and lower glucose levels in rodents.

Product information

CAS Number: 1291087-14-3

Molecular Weight: 457.47

Formula: C52H40CaF6O6

Chemical Name: calcium bis((3S)-3-(4-{[4'-(trifluoromethyl)-[1,1'-biphenyl]-3-yl]methoxy}phenyl)hex-4-ynoate)

Smiles: [Ca+2].CC#C[C@@H](CC([O-])=O)C1C=CC(=CC=1)OCC1=CC(=CC=C1)C1C=CC(=CC=1)C(F)(F)F.CC#C[C@@H](CC([O-])=O)C1C=CC(=CC=1)OCC1=CC(=CC=C1)C1C=CC(=CC=1)C(F)(F)F

InChiKey: WCZAHGONZBHQSA-HRQBZJEISA-L

InChi: InChI=1S/2C26H21F3O3.Ca/c2*1-2-4-21(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;/h2*3,5-15,21H,16-17H2,1H3,(H,30,31);/q;;+2/p-2/t2*21-;/m00./s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

AMG 837 (1 nM-10 μM) stimulates insulin secretion in a glucose-dependent manner with an EC50 of 142±20 nM on islets isolated from mice. AMG 837 stimulates Ca2+ flux with the EC50s of 13.5, 22.6 and 31.7 nM for human, mouse and rat receptors in CHO cells, respectively.

In Vivo:

AMG 837 (0.03-0.3 mg/kg; a single p.o.) improves glucose tolerance and enhances insulin secretion in Sprague-Dawley rats. AMG 837 (0.03-0.3 mg/kg; p.o. once daily for 21 days) reduces glucose levels and increases insulin levels following glucose challenge in vivo. AMG 837 (0.5 mg/kg; p.o.) displays excellent oral bioavailability (F = 84%) and a total plasma Cmax of 1.4 µM.

Products are for research use only. Not for human use.

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