EMA401 (EMA401) 是一种高选择性、口服活性、外周受限的血管紧张素 II 2 型受体 (AT2R) 拮抗剂。
| Cas No. | 1316755-16-4 |
| 别名 | EMA401; PD-126055 |
| Canonical SMILES | O=C([C@H]1N(C(C(C2=CC=CC=C2)C3=CC=CC=C3)=O)CC4=C(C(OCC5=CC=CC=C5)=C(OC)C=C4)C1)O |
| 分子式 | C32H29NO5 |
| 分子量 | 507.58 |
| 溶解度 | DMSO : ≥ 34 mg/mL (66.98 mM) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | EMA401, a highly selective AT2R antagonist, inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons.target: AT2RIn vivo: AngII induces p38, p42/p44 mitogen activated protein kinase (MAPK) activation, neurite outgrowth in adult rat DRG neurons, and sensitization of adult rat and human DRG neurons that is blocked by EMA401. Inhibits capsaicin responses in cultured hDRG neurons. References:
[1]. Rice AS 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 May 10;383(9929):1637-47.
[2]. 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.
[3]. Rice AS 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 May 10;383(9929):1637-47. |
