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RO1138452

CAS No. : 221529-58-4

MCE 站：RO1138452

产品活性：RO1138452 是一种有效的选择性前列环素 IP (prostacyclin) 受体拮抗剂。RO1138452 对 IP 受体具有高的亲和力。在人血小板中，pK_i 值为 9.3±0.1; 在重组 IP 受体系统中，pK_i 值为 8.7±0.06。

研究领域：GPCR/G Protein

作用靶点：Prostaglandin Receptor

In Vitro: RO1138452 is IP receptor antagonist. The pIC₅₀ values of RO1138452 in attenuating cAMP accumulation is 7.0±0.07. Functional antagonism of RO1138452 is studied by measuring inhibition of carbaprostacyclin-induced cAMP accumulation in CHO-K1 cells stably expressing the human IP receptor. The antagonist affinity (pK_i) of RO1138452 is 9.0±0.06. Selectivity profiles for RO1138452 are determined via a panel of receptor binding and enzyme assays. RO1138452 displays affinity at imidazoline₂ (I₂) (8.3) and platelet activating factor (PAF) (7.9) receptors. RO1138452 (10 pM-10 μM) added to cells concurrently with a fixed concentration of Taprostene (1 μM) prevents, in a concentration-dependent manner, the inhibition of CXCL9 and CXCL10 release, with p[A]₅₀ (molar) values of -8.73±0.11 and -8.47±0.16 (p>0.05), respectively.

In Vivo: RO1138452 is a potent and selective antagonist for both human and rat IP receptors and that is possesses analgesic and anti-inflammatory potential. RO1138452 (1-10?mg/kg, i.v.) significantly reduces acetic acid-induced abdominal constrictions. RO1138452 (3-100?mg/kg, p.o.) significantly reduces carrageenan-induced mechanical hyperalgesia and edema formation. One?hour after administration of RO1138452 (5?mg/kg, i.v.) to rats, the total plasma concentration is 0.189 ?μg/mL, whereas the free plasma concentrations is calculated to be 0.009?μg/mL (28 nM).

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