134362-79-1

134362-79-1 structure

Name: Ro 0437626
Chemical Name: N-[(2R)-1-[[(2S,3R,4S)-1-cyclohexyl-4-cyclopropyl-3,4-dihydroxybutan-2-yl]amino]-1-oxo-3-(1,3-thiazol-4-yl)propan-2-yl]-1H-benzimidazole-2-carboxamide
CAS Number: 134362-79-1
Molecular Formula: C₂₇H₃₅N₅O₄S
Molecular Weight: 525.66300
Catalog: Signaling Pathways Membrane Transporter/Ion Channel P2X Receptor
Create Date: 2018-06-22 13:45:04
Modify Date: 2024-01-06 18:24:55
Ro 0437626 is a selective purinergic (P2X1) receptor antagonist (IC50 = 3 μM), but shows low affinity for P2X2, P2X3 and P2X2/3 receptors (IC50 > 100 μM)[1].

Name	N-[(2R)-1-[[(2S,3R,4S)-1-cyclohexyl-4-cyclopropyl-3,4-dihydroxybutan-2-yl]amino]-1-oxo-3-(1,3-thiazol-4-yl)propan-2-yl]-1H-benzimidazole-2-carboxamide
Synonyms	Cortistatin 14

Description	Ro 0437626 is a selective purinergic (P2X1) receptor antagonist (IC50 = 3 μM), but shows low affinity for P2X2, P2X3 and P2X2/3 receptors (IC50 > 100 μM)[1].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Membrane Transporter/Ion Channel >> P2X Receptor
Target	IC50: 3 μM (P2X1 receptor)
In Vitro	Ro 0437626 reduces PMA-evoked Ca2+entry with 6.8 ± 4.7% of control[2].
In Vivo	Ro 0437626 (1 and 10 μmol/kg; i.v.) causes a reduction in postinfusion isovolumetric contractions[3]. Animal Model: Female rat (urethane-anaesthetized)[3] Dosage: 1 and 10 μmol/kg Administration: I.v. Result: Caused a reduction in postinfusion isovolumetric contractions.
References	[1]. Jaime-Figueroa S, et al. Discovery and synthesis of a novel and selective drug-like P2X(1) antagonist. Bioorg Med Chem Lett. 2005;15(13):3292-3295. [2]. Harper MT, et al. Phorbol ester-evoked Ca2+ signaling in human platelets is via autocrine activation of P(2X1) receptors, not a novel non-capacitative Ca2+ entry. J Thromb Haemost. 2010;8(7):1604-1613. [3]. King BF, et al. Investigation of the effects of P2 purinoceptor ligands on the micturition reflex in female urethane-anaesthetized rats. Br J Pharmacol. 2004;142(3):519-530.