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
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关于此项目
经验公式（希尔记法）:
C32H28NNaO5
化学文摘社编号:
分子量:
529.56
UNSPSC Code:
12352200
MDL number:
NACRES:
NA.21
Assay:
≥98% (HPLC)
Form:
powder
Storage condition:
desiccated
Quality Segment
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Biochem/physiol Actions
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).
Disclaimer
Hygroscopic
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable