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885101-89-3 (GW9508)

1

Identification

GW9508 GW9508
Name GW9508
Formula C22H21NO3
MW 347.41
CAS No. 885101-89-3
EINECS
Smiles O=C(O)CCC1=CC=C(NCC2=CC=CC(OC3=CC=CC=C3)=C2)C=C1
Synonyms GW 9508;GW-9508; 3-(4-((3-phenoxybenzyl)amino)phenyl)propanoic acid
InChI InChI=1S/C22H21NO3/c24-22(25)14-11-17-9-12-19(13-10-17)23-16-18-5-4-8-21(15-18)26-20-6-2-1-3-7-20/h1-10,12-13,15,23H,11,14,16H2,(H,24,25)
2

Introduction

GW9508 is a potent and selective agonist for FFA1 (GPR40) with pEC50 of 7.32, 100-fold selective against GPR120, stimulates insulin secretion in a glucose-sensitive manner. IC50 value: 7.32 (pEC50) [1] Target: GPR40 GW9508 is shown to be at least 100-fold selective against 220 other GPCRs, 60 kinases, 63 proteases, seven integrins and 20 nuclear receptors including PPARα, δ and γ (pEC50 4.0, 4 and 4.9, respectively).

Background Information

GW9508 is a selective FFA1/GPR40 agonist (pEC50 values are 7.32, < 4.3 and < 4.3 for FFA1, FFA2 and FFA3 receptors respectively). GPR40 was formerly an orphan G protein-coupled receptor whose endogenous ligands have now been identified as free fatty acids (FFAs). GW9508 showed greater than 500-fold selectivity for GPR40 over GPR41 and GPR43 and possessed a good in vitro and in vivo profile with excellent bioavailability. GW9508 inhibited CCL17 and CCL5 expression in a pertussis toxin-sensitive manner. GW9508 also inhibited CCL5 and CXCL10 production by normal human epidermal keratinocytes. Administration of GW9508 topically to the skin in the challenging phase suppressed ear swelling in a repeated hapten application model and contact hypersensitivity with downregulation of CCL5 and CXCL10, respectively. GW9508 dose dependently potentiated glucose-stimulated insulin secretion in MIN6 cells, but not in primary rat or mouse islets. Furthermore, GW9508 was able to potentiate the KCl-mediated increase in insulin secretion in MIN6 cells. ......by AbMole BioScience
GW 9508 is a cell-permeable aminophenylpropanoate that acts as a potent and selective agonist for the G-protein coupled receptor (GPCR) GRP40/FFA1 receptor (EC50 ?50 nM) with reduced activity towards family members GRP120 (EC50 ?3.5 μM), GRP41/GRP43 (EC50 >50 μM), as well as a panel of eight other free fatty acid (FFA) and prostaglandin receptors.
......by AdooQ BioScience, LLC
Description ......by Apexbio Technology LLC
GW9508 is a potent and selective agonist for FFA1 (GPR40) with pEC50 of 7.32, 100-fold selective against GPR120, stimulates insulin secretion in a glucose-sensitive manner. ......by BOC Sciences
GW 9508 is a potent and selective agonist for the free fatty acid receptor FFA1 (GPR40) with pEC₅₀ of 7.32; 100-fold selective against GPR120. Inactive against a range of other GPCRs, kinases, proteases, integrins and PPARs. Potentiates glucose-stimulated insulin secretion in MIN6 cells (pEC₅₀ = 6.14). ......by BioVision, Inc.,
GW9508 is a GPR40 agonist. GW9508 suppresses CCL5, CCL17, and CXCL10 induction in keratinocytes and attenuates cutaneous immune inflammation. GW9508 also inhibits insulin secretion by activating ATP-sensitive potassium channels in rat pancreatic β-cells. ......by MedKoo Biosciences, Inc.
GW9508 is a potent and selective agonist for FFA1 (GPR40) with pEC50 of 7.32, 100-fold selective against GPR120, stimulates insulin secretion in a glucose-sensitive manner. ......by Selleck Chemicals LLC
GW9508 is a potent and selective agonist for FFA1 (GPR40) with pEC50 of 7.32, 100-fold selective against GPR120, stimulates insulin secretion in a glucose-sensitive manner. ......by Target Molecule Corp.
Potent and selective agonist for the free fatty acid receptor FFA1 (GPR40) (pEC50 values are 7.32, < 4.3 and < 4.3 for FFA1, FFA2 and FFA3 receptors respectively). Inactive against a range of other GPCRs, kinases, proteases, integrins and PPARs. Potentiates glucose-stimulated insulin secretion in MIN6 cells (pEC50 = 6.14). ......by Tocris Bioscience Inc.
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

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Physical and Chemical Properties

Appearance:White to off-white solid EBNumber:EB000015605

Storage condition

Storage condition:Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). Stock solution storage:0 - 4 C for short term (days to weeks), or -20 C for long term (months). Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. by MedKoo Biosciences, Inc.

Solubility

DMSO 69 mg/ml; Water <1 mg/ml by MedChemexpress Co., Ltd.
Soluble in DMSO, not in water by MedKoo Biosciences, Inc.
(25°C) * In vitro DMSO 69 mg/mL (198.61 mM); Ethanol69 mg/mL (198.61 mM); Water<1 mg/mL (<1 mM) by Selleck Chemicals LLC
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Mechanism and Indication

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

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
GW9508 - Not Found
GW9508 - No Development Reported
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Safety Data of GW9508

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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
AbMole BioScience 10mg/USD90(In stock) USA
Abcam 100mg/USD455() USA
AdooQ BioScience, LLC USA
Aladdin 10mg/RMB899();250mg/RMB6999() China
Apexbio Technology LLC 5mg/USD30(In stock);10mg/USD55(In stock) USA
Ark Pharm, Inc. USA
Axon Medchem BV 10mg/USD102(In stock) Netherlands
BOC Sciences
BioVision, Inc., 10mg/USD135() USA
Biochempartner Co., Ltd China
CHEMSCENE, LLC 10mg/USD68();50mg/USD288() USA
Cayman Chemical Company 5mg/USD30() USA
EMD Millipore 10mg/USD209() USA
Lancrix Chemicals. 10mg/USD78() China
MedChemexpress Co., Ltd. 10mg/USD68();50mg/USD288() USA
MedKoo Biosciences, Inc. USA
Santa Cruz Biotechnology, Inc. 10mg/USD125() USA
Selleck Chemicals LLC 10mg/USD147(In stock);10mM/1mLIn DMSO/USD190(In stock);50mg/USD470(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 10mg/USD68();50mg/USD288() China
Sigma-Aldrich, Inc. 5mg/USD114() USA
Target Molecule Corp. 5mg/USD28();10mg/USD55();25mg/USD108();50mg/USD198();100mg/USD368() USA
Tocris Bioscience Inc. 10mg/USD145() USA
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Related Products

Other Forms of 885101-89-3

Name CAS No Formula MW

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
AMG 837 865231-46-5 C26H21F3O3 438.44
TUG-770 1402601-82-4 C19H14FNO2 307.32
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

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References

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More Information

GW9508

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