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Merck
CN

SML3969

Sigma-Aldrich

EMA401 sodium salt

≥98% (HPLC)

Synonym(s):

(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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About This Item

Empirical Formula (Hill Notation):
C32H28NNaO5
CAS Number:
1316755-17-5
Molecular Weight:
529.56
MDL number:
MFCD30502664
UNSPSC Code:
12352200

Key Documents

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Quality Level

100

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).

Disclaimer

Hygroscopic

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number
0000373719
0000356332
0000356331
0000335678
0000335678

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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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