Olodanrigan (EMA401) - 98%, high purity , Angiotensin II type 2 (AT-2) receptor antagonist, CAS No.1316755-16-4, Angiotensin II type 2 (AT-2) receptor antagonist
Olodanrigan (EMA401) - 98%, high purity , Angiotensin II type 2 (AT-2) receptor antagonist, CAS No.1316755-16-4, Angiotensin II type 2 (AT-2) receptor antagonist
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/AT
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
ANTAGONIST
Mechanism of action
Angiotensin II type 2 (AT-2) receptor antagonist
Product Description
Information
Olodanrigan (EMA401) 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.
1.Chakrabarty A, Blacklock A, Svojanovsky S, Smith PG. (2008) Estrogen elicits dorsal root ganglion axon sprouting via a renin-angiotensin system.. Endocrinology, 149 (7):(3452-60). [PMID:18388195]
2.Patil J, Schwab A, Nussberger J, Schaffner T, Saavedra JM, Imboden H. (2010) Intraneuronal angiotensinergic system in rat and human dorsal root ganglia.. Regul Pept, 162 (1-3):(90-8). [PMID:20346377]
3.Smith MT, Wyse BD, Edwards SR. (2013) Small molecule angiotensin II type 2 receptor (AT₂R) antagonists as novel analgesics for neuropathic pain: comparative pharmacokinetics, radioligand binding, and efficacy in rats.. Pain Med, 14 (5):(692-705). [PMID:23489258]
4.Rice AS, Dworkin RH, McCarthy TD, Anand P, Bountra C, McCloud PI, Hill J, Cutter G, Kitson G, Desem N et al.. (2014) EMA401, an orally administered highly selective angiotensin II type 2 receptor antagonist, as a novel treatment for postherpetic neuralgia: a randomised, double-blind, placebo-controlled phase 2 clinical trial.. Lancet, 383 (9929):(1637-47). [PMID:24507377]
5.McCarthy T. (2014) Development of EMA401 as an orally-administered, highly-selective angiotensin II type 2 receptor antagonist for the treatment of neuropathic pain.. J Peripher Nerv Syst, 19 Suppl 2 (3):(S13-4). [PMID:25269730]
6.Murgasova R, Carreras ET, Suetterlin-Hachmann M, da Silva Torrao LR, Kittelmann M, Alexandra V, Fredenhagen A. (2020) Non-clinical characterization of the disposition of EMA401, a novel small molecule angiotensin II type 2 receptor (AT2R) antagonist.. Biopharm Drug Dispos, 41 (4-5):(166-183). [PMID:32190910]
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C2331761