| Bioactivity | 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[1][2][3][4]. | ||||||||||||
| 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)[4]. | ||||||||||||
| Name | Olodanrigan | ||||||||||||
| CAS | 1316755-16-4 | ||||||||||||
| Formula | C32H29NO5 | ||||||||||||
| Molar Mass | 507.58 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [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 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 |
Olodanrigan
CAS: 1316755-16-4 F: C32H29NO5 W: 507.58
Olodanrigan (EMA401) is a highly selective, orally active, peripherally restricted angiotensin II type 2 receptor (AT2R)
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