Home GPCR & G Protein Angiotensin Receptor antagonist Olodanrigan (EMA401) For research use only.

Olodanrigan (EMA401)

Synonyms: PD-126055, (S) PD-126055

Olodanrigan (EMA401, PD-126055, (S) PD-126055) is a highly selective, orally active, peripherally restricted antagonist of angiotensin II type 2 receptor (AT2R). Olodanrigan (EMA401) analgesic action appears to involve the inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons.

Olodanrigan (EMA401) Chemical Structure

Olodanrigan (EMA401) Chemical Structure

CAS No. 1316755-16-4

Purity & Quality Control

Batch: S032601 DMSO]100 mg/mL]false]Ethanol]100 mg/mL]false]Water]Insoluble]false Purity: 99.66%
99.66

Olodanrigan (EMA401) Related Products

Biological Activity

Description Olodanrigan (EMA401, PD-126055, (S) PD-126055) is a highly selective, orally active, peripherally restricted antagonist of angiotensin II type 2 receptor (AT2R). Olodanrigan (EMA401) analgesic action appears to involve the inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons.
Targets
AT2R [1]
In vitro
In vitro

EMA401 may act on paracrine/autocrine mechanisms at peripheral nerve terminals, or intracrine mechanisms, to reduce neuropathic pain signalling in AngII/NGF/TRPV1-convergent pathways.[1]
Cell Research Cell lines rat DRG neurons
Concentrations 10, 100 nM
Incubation Time 30 min
Method

48 h after plating, duplicate dishes were treated with AngII (10 nM), AngII + EMA401 (10 and 100 nM respectively), 100 nM EMA401, NGF (100 ng/ml) or vehicle treated (control 0), for 30 min at 37 ℃, then fixed with 4% PFA for 30 min for immunostaining.
In Vivo
In vivo

EMA401, a selective small molecule antagonist of the AT2R, 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).[2]
Animal Research Animal Models Adult male Sprague-Dawley (SD) rats with a unilateral chronic constriction injury (CCI) of the sciatic nerve
Dosages 1 mg/kg (i.v.); 10 mg/kg (p.o.)
Administration i.v.; p.o.

Chemical Information & Solubility

Molecular Weight 507.58 Formula

C32H29NO5
CAS No. 1316755-16-4 SDF --
Smiles COC1=C(C2=C(CN(C(C2)C(=O)O)C(=O)C(C3=CC=CC=C3)C4=CC=CC=C4)C=C1)OCC5=CC=CC=C5
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (197.01 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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