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

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Olodanrigan (EMA401) Angiotensin Receptor antagonist

Cat.No.S0326

Olodanrigan (EMA401, PD-126055, (S) PD-126055) is a highly selective, orally active, peripherally restricted antagonist of angiotensin II type 2 receptor (AT2R). Its 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) Angiotensin Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 507.58

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (197.01 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 507.58 Formula

C32H29NO5

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1316755-16-4 -- Storage of Stock Solutions

Synonyms PD-126055, (S) PD-126055 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

Mechanism of Action

Targets/IC50/Ki
AT2R
In vitro

Olodanrigan (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.
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).
References

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