SML3969
EMA401 sodium salt
≥98% (HPLC)
别名:
(3S)-2-(2,2-Diphenylacetyl)-1,2,3,4-tetrahydro-6-methoxy-5-(phenylmethoxy)-3-iIsoquinolinecarboxylic acid, sodium salt, (3S)-EMA400 sodium salt, (3S)-PD-126,055 sodium salt, (3S)-PD-126055 sodium salt, Olodanrigan sodium salt
生化/生理作用
Orally available, selective, high-affinity type-2 angiotensin II receptor (AT2R) antagonist with in vivo pain relief efficacy.
EMA401, the (3S)-enantiomer of EMA400 (PD-126,055), is a selective, high-affinity type-2 angiotensin II receptor (AT2R) antagonist (IC50 = 39.5 nM/>39 μM against 50 pM CGP 42112A for binding human AT2R/AT1R; IC50 = 39.5 nM/408 μM against 40 nM Ang II for binding rat AT2R/AT1R). EMA401, but not the AT1R antagonist losartan, is shown to inhibit capsaicin (200 nM) responses in cultured neurons of human and rat DRG (IC50 = 10 nM). EMA401 is orally available (F = 33.2%, t1/2 = 5.7 h, Cmax = 885 ng/mL post 10 mg/kg oral dosage in rats) and exhibits in vivo pain relief efficacy among adult male SD rats with a unilateral chronic constriction injury (CCI) of the sciatic nerve (ED50 = 10 μg/kg via i.p. using the racemate EMA400).
EMA401, the (3S)-enantiomer of EMA400 (PD-126,055), is a selective, high-affinity type-2 angiotensin II receptor (AT2R) antagonist (IC50 = 39.5 nM/>39 μM against 50 pM CGP 42112A for binding human AT2R/AT1R; IC50 = 39.5 nM/408 μM against 40 nM Ang II for binding rat AT2R/AT1R). EMA401, but not the AT1R antagonist losartan, is shown to inhibit capsaicin (200 nM) responses in cultured neurons of human and rat DRG (IC50 = 10 nM). EMA401 is orally available (F = 33.2%, t1/2 = 5.7 h, Cmax = 885 ng/mL post 10 mg/kg oral dosage in rats) and exhibits in vivo pain relief efficacy among adult male SD rats with a unilateral chronic constriction injury (CCI) of the sciatic nerve (ED50 = 10 μg/kg via i.p. using the racemate EMA400).
免责声明
Hygroscopic
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
此项目有
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
U Anand et al.
European journal of pain (London, England), 17(7), 1012-1026 (2012-12-21)
The angiotensin II (AngII) receptor subtype 2 (AT2 R) is expressed in sensory neurons and may play a role in nociception and neuronal regeneration. We used immunostaining with characterized antibodies to study the localization of AT2 R in cultured human
Maree T Smith et al.
Pain medicine (Malden, Mass.), 14(5), 692-705 (2013-03-16)
Neuropathic pain is an area of unmet clinical need. The objective of this study was to define the pharmacokinetics, oral bioavailability, and efficacy in rats of small molecule antagonists of the angiotensin II type 2 receptor (AT₂R) for the relief
Uma Anand et al.
Molecular pain, 11, 38-38 (2015-06-27)
The clinical efficacy of the Angiotensin II (AngII) receptor AT2R antagonist EMA401, a novel peripherally-restricted analgesic, was reported recently in post-herpetic neuralgia. While previous studies have shown that AT2R is expressed by nociceptors in human DRG (hDRG), and that EMA401
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