Ro 0437626

Modify Date: 2024-01-06 18:24:55

Ro 0437626 Structure
Ro 0437626 structure
Common Name Ro 0437626
CAS Number 134362-79-1 Molecular Weight 525.66300
Density N/A Boiling Point N/A
Molecular Formula C27H35N5O4S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Ro 0437626


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].

 Names

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
Synonym More Synonyms

 Ro 0437626 Biological Activity

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
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.

 Chemical & Physical Properties

Molecular Formula C27H35N5O4S
Molecular Weight 525.66300
Exact Mass 525.24100
PSA 168.47000
LogP 3.72930

 Synonyms

Cortistatin 14