Home GPCR & G Protein Angiotensin Receptor antagonist Olodanrigan (EMA401)

Olodanrigan (EMA401)

Catalog No.S0326 Synonyms: PD-126055, (S) PD-126055

For research use only.

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

CAS No. 1316755-16-4

Purity & Quality Control

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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

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]
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]

Protocol (from reference)

Cell Research:

[1]
  • 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.
Animal Research:

[2]
  • 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

Molecular Weight 507.58
Formula

C32H29NO5
CAS No. 1316755-16-4
Storage 3 years -20°C powder
2 years -80°C in solvent
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

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