ASP7663|1190217-35-6|-陌孚医药/Medlife

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ASP7663

目录号: PL12444 纯度: ≥99%

CAS No. :1190217-35-6

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中文名称	ASP7663
中文别名	ASP 7663
英文名称	ASP7663
英文别名	ASP 7663;(2E)-2-[7-Fluoro-1,2-dihydro-1-(2-methylpropyl)-2-oxo-3H-indol-3-ylidene]acetic acid;(E)-[7-Fluoro-1-(2-methylpropyl)-2-oxo-1,2-dihydro-3H-indol-3-ylidene]acetic acid;ASP7663;GTPL10274;BDBM50318498;ASP7663, >=98% (HPLC);2-(7-fluoro-1-isobutyl-2-oxoindolin-3-ylidene)acetic acid;(2E)-2-[7-fluoro-1-(2-methylpropyl)-2-oxoindol-3-ylidene]acetic acid;CID 44232532
Cas No.	1190217-35-6
分子式	C₁₄H₁₄FNO₃
分子量	263.26
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	ASP7663 是具有口服活性的、选择性的 TRPA1 激动剂。ASP7663 具有抗便秘和抗腹痛的活性。
生物活性	ASP7663 is an orally active and selective TRPA1 agonist. ASP7663 exerts both anti-constipation and anti-abdominal pain actions.
性状	Solid
体外研究(In Vitro)	ASP7663 concentration dependently increases intracellular Ca concentration in human, rat, and mouse TRPA1 expressed in HEK293 cells in a similar manner, with respective EC50 values (95% confidence interval [CI]) of 0.51 (0.40–0.66), 0.54 (0.41–0.72), and 0.50 (0.41–0.63) μmol/L. ASP7663 concentration-dependently stimulates 5-HT release from QGP-1 cells, a lineage of TRPA1-expressing EC cells, with an EC50 value of 72.5 (52.6–99.9) μmol/L. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	ASP7663 significantly improves the loperamide-induced delay in colonic transit in mice. ASP7663 (orally, 0.3 and 1 mg/kg) significantly shortens the prolonged bead expulsion time caused by loperamide. ASP7663 (orally, 1 and 3 mg/kg) exhibits inhibitory effects on colorectal distension in rat. has not independently confirmed the accuracy of these methods. They are for reference only.
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
参考文献	[1]. Ryosuke Kojima, et al. Effects of Novel TRPA1 Receptor Agonist ASP7663 in Models of Drug-Induced Constipation and Visceral Pain. Eur J Pharmacol. 2014 Jan 15;723:288-93. [2]. Yao Lu, et al. Transient Receptor Potential Ankyrin 1 Activation Within the Cardiac Myocyte Limits Ischemia-reperfusion Injury in Rodents. Anesthesiology. 2016 Dec;125(6):1171-1180.

溶解度数据	In Vitro: DMSO : 50 mg/mL (189.93 mM; Need ultrasonic)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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