Olodanrigan (Synonyms: EMA401; PD-126055)
目录号: PL14759 纯度: ≥99%
CAS No. :1316755-16-4
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中文名称
Olodanrigan
中文别名
(3S)-2-(2,2-二苯基乙酰基)-1,2,3,4-四氢-6-甲氧基-5-苄氧基-3-异喹啉羧酸;EMA401
英文名称
Olodanrigan
英文别名
3-Isoquinolinecarboxylic acid, 2-(2,2-diphenylacetyl)-1,2,3,4-tetrahydro-6-methoxy-5-(phenylmethoxy)-, (3S)-;EMA 401;EMA-401;EMA401;Olodanrigan;Olodanrigan free acid;P0FN522VTO;Olodanrigan(EMA401);(S)-5-(benzyloxy)-2-(2,2-diphenylacetyl)-6-methoxy-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid;(3S)-2-(2,2-diphenylacetyl)-6-methoxy-5-phenylmethoxy-3,4-dihydro-1H-isoquinoline-3-carboxylic acid;EMA401; Olodanrigan;Olodanrigan [WHO-DD];GTPL8374;BCP23998;EX-
Cas No.
1316755-16-4
分子式
C32H29NO5
分子量
507.58
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Olodanrigan (EMA401) 是一个高选择性、口服活性、外周受限的血管紧张素 Ⅱ 类型 2 受体 (AT2R) 拮抗剂。可用于神经性疼痛的研究。Olodanrigan (EMA401) 的缓解疼痛作用似乎包括抑制增强的 AngII/AT2R 诱导的 p38 和 p42/p44 MAPK 激活,从而抑制 DRG 神经元的过度兴奋性和 DRG 神经元的萌发。
生物活性
Olodanrigan (EMA401) is a highly selective, orally active, peripherally restricted angiotensin II type 2 receptor (AT2R) antagonist. It is under development as a neuropathic pain therapeutic agent. Olodanrigan (EMA401) analgesic action appears to involve inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons.
性状
Solid
体内研究(In Vivo)
EMA401 (10?mg/kg; p.o.) 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). 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
ClinicalTrial
参考文献
[1]. Suguru Koyama,et al. An Electroencephalography Bioassay for Preclinical Testing of Analgesic Efficacy.
[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 adminis
溶解度数据
In Vitro: DMSO : ≥ 34 mg/mL (66.98 mM)H2O : 0.1 mg/mL (0.20 mM; Need ultrasonic)
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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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