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Purity: ≥98%
GW9508 (GW-9508) is a novel, potent and selective agonist for FFA1 (fatty acid receptor GPR40) with pEC50 of 7.32, and is 100-fold selective against GPR120, it stimulates insulin secretion in a glucose-sensitive manner. GW9508 is a GPR40/120 agonist and is different from the reported GPR40/120 agonist GW1100. When tested with HEK-293 (human embryonic kidney) cells expressing GPR40 or GRP120, GW9508 treatment increased intracellular Ca2+ concentration via activating GPR40/120 in a dose-dependent manner.
| ln Vitro |
In HEK-293 cells expressing GPR40 (pEC50 of 7.32) or GPR120 (pEC50 of 5.46), GW9508 increases intracellular Ca2+ mobilization, but not in the parent HEK-293 cell line [1]. GW9508 concentration-dependently enhances glucose-stimulated insulin secretion at high glucose levels (25 mM) (pEC50 of 6.14). Insulin secretion was raised 1.52-fold when 20 μM GW9508 was used in conjunction with 25 mM glucose as opposed to 25 mM glucose alone. As the quantity of glucose increases, GW9508 (10 μM) can considerably increase the amount of insulin secreted in MIN6 cells [1]. CCL17 and CCL5 expression in pertussis toxin-sensitive cells is inhibited by GW9508. Through RNA interference, GPR40 can be reduced, so GW9508's inhibitory impact can be removed. In HaCaT cells, GW9508 additionally suppressed the expression of IL-11, IL-24, and IL-33 that were triggered by TNF-α and IFN-γ. GW9508 also prevents normal human epidermal keratinocytes from producing CCL5 and CXCL10[2].
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| ln Vivo |
Topical application of 200 (μM) GW9508 to the skin prevented ear swelling and contact hypersensitivity in repeated hapten application models (BALB/c and C57BL/6 mice) via downregulating CCL5 and CXCL10, respectively [2].
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| References |
[1]. Briscoe CP, et al. Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules. Br J Pharmacol. 2006 Jul;148(5):619-28.
[2]. Fujita T, et al. A GPR40 agonist GW9508 suppresses CCL5, CCL17, and CXCL10 induction in keratinocytes and attenuates cutaneous immune inflammation. J Invest Dermatol, 2011, 131(8), 1660-1667. [3]. Zhao YF, et al. Activation of ATP-sensitive potassium channels in rat pancreatic beta-cells by linoleic acid through both intracellular metabolites and membrane receptor signalling pathway. J Endocrinol, 2008, 198(3), 533-540. [4]. Suski M, et al. Anti-atherosclerotic action of GW9508 - Free fatty acid receptors activator - In apoE-knockout mice. Pharmacol Rep. 2019 Aug;71(4):551-555. |
| Molecular Formula |
C22H21NO3
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| Molecular Weight |
347.41
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| CAS # |
885101-89-3
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| Related CAS # |
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| SMILES |
O(C1C([H])=C([H])C([H])=C([H])C=1[H])C1=C([H])C([H])=C([H])C(=C1[H])C([H])([H])N([H])C1C([H])=C([H])C(=C([H])C=1[H])C([H])([H])C([H])([H])C(=O)O[H]
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| InChi Key |
DGENZVKCTGIDRZ-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
3-(4-((3-phenoxybenzyl)amino)phenyl)propanoic acid
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8784 mL | 14.3922 mL | 28.7844 mL | |
| 5 mM | 0.5757 mL | 2.8784 mL | 5.7569 mL | |
| 10 mM | 0.2878 mL | 1.4392 mL | 2.8784 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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