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Ro 0437626

Names

[ CAS No. ]:
134362-79-1

[ Name ]:
Ro 0437626

[Synonym ]:
Cortistatin 14

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]:

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.

Chemical & Physical Properties

[ Molecular Formula ]:
C27H35N5O4S

[ Molecular Weight ]:
525.66300

[ Exact Mass ]:
525.24100

[ PSA ]:
168.47000

[ LogP ]:
3.72930

Related Compounds