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(CAS: 1610562-74-7 )

Suppliers of BMS-986118

Company Name Email Tel Country
MedKoo Biosciences, Inc. [email protected] 919-279-0682 USA

Fax: 919-980-4831Purity: Brand:

ProbeChem [email protected] 86-21-80183644

Fax: 86-21-68860190Purity: Brand:

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Background Information of BMS-986118

BMS-986118 is a potent and selective G protein-coupled receptor 40 (GPR40) agonist with an EC50 of 70 nM. GPR40, also known as free fatty acid receptor 1 (FFAR1), is a Gq protein-coupled receptor (GPCR) that is predominately expressed in pancreatic β-cells and is also found in the GI tract and brain.  The constellation of GPR40-mediated effects makes it an attractive target for the treatment of type-2 diabetes.

Solubility of BMS-986118

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Storage Condition of BMS-986118

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MSDS Information

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Quality Control and Spectral Data

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Mechanism and Indications

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

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase

Chemical Information

M.Wt Formula CAS No. Synonyms
540.96 C25H28ClF3N4O4 1610562-74-7 BMS986118

Structure Information of BMS-986118

Smiles C1C(Cl)=C(N2C[[email protected]@H](C)[[email protected]](OC3C=CC(N4N=C(C(F)(F)F)[[email protected]@H](C)[[email protected]@H]4CC(O)=O)=CC=3)CC2)C=C(OC)N=1 |&1:6,8,21,23|
InChI InChI=1S/C25H28ClF3N4O4/c1-14-13-32(20-10-22(36-3)30-12-18(20)26)9-8-21(14)37-17-6-4-16(5-7-17)33-19(11-23(34)35)15(2)24(31-33)25(27,28)29/h4-7,10,12,14-15,19,21H,8-9,11,13H2,1-3H3,(H,34,35)/t14-,15+,19+,21-/m1/s1

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AMG 837 (calcium hydrate) 1259389-38-2 C26H22F3O4- 9
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GPR40 Activator 1 1309435-60-6 C31H31NO3S 6
AMG 837 865231-46-5 C26H21F3O3 12
TUG-770 1402601-82-4 C19H14FNO2 13
GW9508 885101-89-3 C22H21NO3 22
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GPR40 Activator 2 1312787-30-6 C28H29NO6S2 6
DC260126 346692-04-4 C32H31N5O 7
M-I C19H22O5S 0
T-1676427 1000414-39-0 C29H32O8S 0
JTT-851 C23H28O3 0
Astellas C27H30N4O4 0
MK-2305 905723-46-8 C19H13ClF3NO4S 0
Mochida 1469495-84-8 C30H35NO6S 0
AM-6226 C32H36F2O4 0
GPR40 agonist 1 1312788-44-5 C24H20O3 0
GPR40 agonist 2 C25H22O3 0
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Chemical and Physical Properties

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[1].Shi J, et al. Discovery of Potent and Orally Bioavailable Dihydropyrazole GPR40 Agonists. J Med Chem. 2018 Feb 8;61(3):681-694.
G protein-coupled receptor 40 (GPR40) has become an attractive target for the treatment of diabetes since it was shown clinically to promote glucose-stimulated insulin secretion. Herein, we report our efforts to develop highly selective and potent GPR40 agonists with a dual mechanism of action, promoting both glucose-dependent insulin and incretin secretion. Employing strategies to increase polarity and the ratio of sp3/sp2 character of the chemotype, we identified BMS-986118 (compound 4), which showed potent and selective GPR40 agonist activity in vitro. In vivo, compound 4 demonstrated insulinotropic efficacy and GLP-1 secretory effects resulting in improved glucose control in acute animal models.

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