Olodanrigan | Angiotensin II type 2 receptor antagonist

CAS:
 1316755-16-4
Catalog Number:
 10-4957
Olodanrigan supplier | CAS 1316755-16-4 | Focus Biomolecules

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5mg$75.00
25mg$235.00

Olodanrigan (EMA401; CAS 1316755-16-4) is a potent (IC50 = 39.5 nM) and selective (>10,000-fold selectivity AT2R/AT1R) antagonist of the angiotensin II type 2 receptor.1 It produced dose-dependent relief of hindpaw sensitivity in a rat model of neuropathic pain1 and showed efficacy in a human trial against postherpetic neuralgia2.  Olodanrigan prevented paclitaxel-associated acute pain syndrome in mice.3 It blocked visceral hypersensitivity and colonic hyperpermeability in a rat model of irritable bowel syndrome.4 It was also able to inhibit proliferation of AT2R-expressing glioblastoma spheroids and blocked their invasiveness and angiogenic capability.5

References/Citations:

  1. Smith et al. (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., 14 692
  2. Rice et al. (2014), EMA401, an orally administered highly selective angiotensin II type 2 receptor antagonist, as a novel treatment for postherpetic neuralgia: a randomized, double-blind, placebo-controlled phase 2 clinical trial; Lancet, 383 1637
  3. Zanata et al. (2021), Blockade of bradykinin receptors or angiotensin II type 2 receptor prevents paclitaxel-associated acute pain syndrome in mice; Eur. J. Pain., 25 189
  4. Nozu et al. (2021), EMA401, an angiotensin II type 2 receptor antagonist blocks visceral hypersensitivity and colonic hyperpermeability in rat model of irritable bowel syndrome; J. Pharmacol. Sci., 146 121
  5. Perryman et al. (2022), Inhibition of the angiotensin II type 2 receptor AT2R is a novel therapeutic strategy for glioblastoma; Proc. Natl. Acad. Sci. USA, 119 e2116289119
CAS:
1316755-16-4
Catalog Number:
10-4957
Activity:
Angiotensin II type 2 receptor antagonist
Chemical Names:
(S)-Benzyloxy-2-diphenylacetyl-6-methoxy-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid
Alternate Name:
EMA401
Molecular Weight:
507.59
Molecular Formula:

C32H29NO5

Solubility:
Soluble in DMSO (at least 35 mg/ml)
Physical Properties:
Off-white solid
Purity:

>98% HPLC
NMR (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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