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Chemical Structure| 1316755-16-4 同义名 : EMA401; PD-126055; (S)PD-126055; (S)-EMA400
CAS号 : 1316755-16-4
货号 : A513856
分子式 : C32H29NO5
纯度 : 99%+
分子量 : 507.58
MDL号 : MFCD28502251
存储条件：

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 The renin-angiotensin system has physiological roles outside the cardiovascular system, including in the central and peripheral nervous systems. The angiotensin II type 2 receptor (AT2R) is a new target for neuropathic pain. EMA401, a highly selective AT2R antagonist, is under development as a novel neuropathic pain therapeutic agent[2]. In rats, single administration of 10 mg/kg EMA401 (p.o.) resulted in a significant attenuation of theta power (0.71 ± 0.13 relative to CCI) and increase in PWL (1.26 ± 0.11 relative to CCI; n = 6 rats at d14[3]. EMA401 (100 mg twice daily) provides superior relief of postherpetic neuralgia compared with placebo at the end of 28 days of treatment. EMA401 was well tolerated by patients[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.97mL

0.39mL

0.20mL

9.85mL

1.97mL

0.99mL

19.70mL

3.94mL

1.97mL
参考文献

[1]Anand U et al. Mechanisms underlying clinical efficacy of Angiotensin II type 2 receptor (AT2R) antagonist EMA401 in neuropathic pain: clinical tissue and in vitro studies. Mol Pain. 2015 Jun 26;11:38.

[2]Rice ASC, Dworkin RH, McCarthy TD, et al. EMA401, an orally administered highly selective angiotensin II type 2 receptor antagonist, as a novel treatment for postherpetic neuralgia: a randomised, double-blind, placebo-controlled phase 2 clinical trial. Lancet. 2014;383(9929):1637‐1647

[3]An Electroencephalography Bioassay for Preclinical Testing of Analgesic Efficacy