GW9508 structure
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Common Name | GW9508 | ||
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CAS Number | 885101-89-3 | Molecular Weight | 347.407 | |
Density | 1.2±0.1 g/cm3 | Boiling Point | 538.4±45.0 °C at 760 mmHg | |
Molecular Formula | C22H21NO3 | Melting Point | N/A | |
MSDS | Chinese USA | Flash Point | 279.4±28.7 °C | |
Symbol |
GHS05, GHS07, GHS09 |
Signal Word | Danger |
Use of GW9508GW9508 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: GPR40GW9508 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). GW9508 produces a concentration-dependent increase in intracellular Ca2+ concentrations via GPR40 receptor activation and the GPR120 receptor. GW9508 is active as an agonist at both GPR40 and GPR120, it is approximately 100-fold selective for GPR40 with respect to GPR120. GW9508 produces a concentration-dependent increase (pEC50=6.14) in glucose-stimulated insulin secretion at high glucose levels (25 mM). GW9508 dose dependently stimulated insulin secretion in a glucose-sensitive manner in MIN6 cells. Furthermore, GW9508 is able to potentiate the KCl-mediated increase in insulin secretion in MIN6 cells. [1] GW9508 induced hyperpolarization and opening of KATP channels in rat β-cells. [2] GW9508 inhibits CCL17 and CCL5 expression in a pertussis toxin-sensitive manner. GW9508 further suppresses expression of IL-11, IL-24, and IL-33 induced in HaCaT cells by TNF-α and IFN-γ. GW9508 also inhibits CCL5 and CXCL10 production by normal human epidermal keratinocytes. [3] |
Name | 3-[4-[(3-phenoxyphenyl)methylamino]phenyl]propanoic acid |
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Synonym | More Synonyms |
Description | 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: GPR40GW9508 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). GW9508 produces a concentration-dependent increase in intracellular Ca2+ concentrations via GPR40 receptor activation and the GPR120 receptor. GW9508 is active as an agonist at both GPR40 and GPR120, it is approximately 100-fold selective for GPR40 with respect to GPR120. GW9508 produces a concentration-dependent increase (pEC50=6.14) in glucose-stimulated insulin secretion at high glucose levels (25 mM). GW9508 dose dependently stimulated insulin secretion in a glucose-sensitive manner in MIN6 cells. Furthermore, GW9508 is able to potentiate the KCl-mediated increase in insulin secretion in MIN6 cells. [1] GW9508 induced hyperpolarization and opening of KATP channels in rat β-cells. [2] GW9508 inhibits CCL17 and CCL5 expression in a pertussis toxin-sensitive manner. GW9508 further suppresses expression of IL-11, IL-24, and IL-33 induced in HaCaT cells by TNF-α and IFN-γ. GW9508 also inhibits CCL5 and CXCL10 production by normal human epidermal keratinocytes. [3] |
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Related Catalog | |
References |
Density | 1.2±0.1 g/cm3 |
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Boiling Point | 538.4±45.0 °C at 760 mmHg |
Molecular Formula | C22H21NO3 |
Molecular Weight | 347.407 |
Flash Point | 279.4±28.7 °C |
Exact Mass | 347.152130 |
PSA | 58.56000 |
LogP | 4.74 |
Vapour Pressure | 0.0±1.5 mmHg at 25°C |
Index of Refraction | 1.641 |
Storage condition | Store at RT |
Water Solubility | DMSO: >20mg/mL |
Symbol |
GHS05, GHS07, GHS09 |
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Signal Word | Danger |
Hazard Statements | H302-H315-H318-H335-H410 |
Precautionary Statements | P261-P273-P280-P305 + P351 + P338-P501 |
Personal Protective Equipment | dust mask type N95 (US);Eyeshields;Faceshields;Gloves |
Hazard Codes | Xn,N |
Risk Phrases | 22-37/38-41-50/53 |
Safety Phrases | 26-39-60-61 |
RIDADR | UN 3077 9 / PGIII |
~87% GW9508 CAS#:885101-89-3 |
Literature: PROMETIC BIOSCIENCES INC.; GAGNON, Lyne; GROUIX, Brigitte; GEERTS, Lilianne; LAURIN, Pierre; PENNEY, Christopher; ZACHARIE, Boulos Patent: WO2012/97427 A1, 2012 ; Location in patent: Page/Page column 41-42 ; |
~% GW9508 CAS#:885101-89-3 |
Literature: Bioorganic and Medicinal Chemistry Letters, , vol. 17, # 6 p. 1584 - 1589 |
Precursor 3 | |
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DownStream 0 |
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Benzenepropanoic acid, 4-[[(3-phenoxyphenyl)methyl]amino]- |
3-{4-[(3-Phenoxybenzyl)amino]phenyl}propanoic acid |
gw9508 |
GW-9508 |