| 產(chǎn)品描述： | Olodanrigan (EMA401, PD-126055, (S) PD-126055) 是一種高度選擇性的、具有口服活性的外周限制性 angiotensin II type 2 receptor (AT2R) 拮抗劑。Olodanrigan 的鎮(zhèn)痛作用可能涉及抑制增強(qiáng) AngII/AT2R 誘導(dǎo)的 p38 和 p42/p44 MAPK 激活，從而抑制 DRG 神經(jīng)元過度興奮和 DRG 神經(jīng)元的萌芽 |
| 靶點(diǎn)： |
AT2R;RAAS |
| 體外研究： |
EMA401 may act on paracrine/autocrine mechanisms at peripheral nerve terminals, or intracrine mechanisms, to reduce neuropathic pain signalling in AngII/NGF/TRPV1-convergent pathways |
| 體內(nèi)研究： |
EMA401, a selective small molecule antagonist of the AT2R, results in a significant attenuation of theta power and increase in paw withdrawal latencies (PWL) in rats at day 14 after chronic constriction injury (CCI). |
| 細(xì)胞實驗： |
Cell lines: rat DRG neurons Concentrations: 10, 100 nM Incubation Time: 30 min Method: 48 h after plating, duplicate dishes were treated with AngII (10 nM), AngII + EMA401 (10 and 100 nM respectively), 100 nM EMA401, NGF (100 ng/ml) or vehicle treated (control 0), for 30 min at 37 ℃, then fixed with 4% PFA for 30 min for immunostaining. |
| 動物實驗： |
Animal Models: Adult male Sprague-Dawley (SD) rats with a unilateral chronic constriction injury (CCI) of the sciatic nerve Dosages: 1 mg/kg (i.v.); 10 mg/kg (p.o.) Administration: i.v.; p.o. |
| 參考文獻(xiàn)： |
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. Smith MT, et al.Small molecule angiotensin II type 2 receptor (AT?R) antagonists as novel analgesics for neuropathic pain: comparative pharmacokinetics, radioligand binding, and efficacy in rats. Pain Med. 2013 May;14(5):692-705. |
| 溶解性： |
DMSO: ≥ 34 mg/mL |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.97 ml |
9.851 ml |
19.701 ml |
| 5 mM |
0.394 ml |
1.97 ml |
3.94 ml |
| 10 mM |
0.197 ml |
0.985 ml |
1.97 ml |
| 50 mM |
0.039 ml |
0.197 ml |
0.394 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學(xué)品經(jīng)營許可證（不帶存儲）
營業(yè)執(zhí)照(三證合一)
北京