AMG7703 是一种FFA2(GPR43) 的选择性变构激动剂，FFA2 是短链脂肪酸 (SCFA)、醋酸盐 (acetate) 和丙酸 (methylacetic) 的受体。AMG7703可用于炎症和代谢的研究。
| 生物活性 | AMG7703 is a selective and allosteric agonists ofFFA2(GPR43), the receptor for short-chain fatty acids (SCFAs), acetate, and propionate. AMG7703 can be used to research for in inflammatory and metabolic[1]. |
体外研究
(In Vitro) | AMG7703 (phenylacetamide 1) (30 μM) shows selectivity on FFA2 (GPR43) over FFA1 (GPR40) and FFA3 (GPR41) with in Chinese hamster ovary cells[1].
AMG7703 (0.041, 0.123, 0.37, 1.11 μM) acts as an FFA2 allosteric agonist, activates Gαicoupled signaling pathway[1].
AMG7703 (1, 3, 10, 30 μM) results in Gαi-dependent inhibition of lipolysis in adipocytes (3T3L1)[1].
AMG7703 (0.041, 0.123, 0.37, 1.11 μM) exhibits allosteric activity and inhibits Gαi-coupled cAMP with IC50values of 0.7 μM (hFFA2) and 0.96 μM (mFFA2), respectively; as for Gαq-coupled aequorin inhibition, with EC50s of 0.45 μM (hFFA2) and 1.27 μM (mFFA2), respectively[1].
AMG7703 (0-1 μM) shows the positive cooperating effect of acetate and stimulates calcium mobilization in a concentration-dependent manner in CHO cell stably expressing hFFA2 and aequorin[1].
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(339.21 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 3.3921 mL | 16.9607 mL | 33.9213 mL | | 5 mM | 0.6784 mL | 3.3921 mL | 6.7843 mL | | 10 mM | 0.3392 mL | 1.6961 mL | 3.3921 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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