RO1138452

生物活性靶点体外研究体内研究 RO1138452 试剂级价格

RO1138452

CAS号:221529-58-4
英文名:4,5-DIHYDRO-N-[4-[[4-(1-METHYLETHOXY)PHENYL]METHYL]PHENYL]-1H-IMIDAZOL-2-AMINE
中文名:RO1138452
CBNumber:CB7455737
分子式:C19H23N3O
分子量:309.41
MOL File:221529-58-4.mol

RO1138452化学性质

沸点 :449.7±47.0 °C(Predicted)
密度 :1.13±0.1 g/cm3(Predicted)
储存条件 :under inert gas (nitrogen or Argon) at 2–8 °C
溶解度 :DMF: 30 mg/ml; DMF:PBS (pH 7.2)(1:10): 0.05 mg/ml; DMSO: 20 mg/ml; Ethanol: 20 mg/ml
形态 :A crystalline solid
酸度系数(pKa) :9.94±0.33(Predicted)
颜色 :Light yellow to brown

RO1138452性质、用途与生产工艺

生物活性 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，pKi 值为 9.3±0.1; 在重组 IP 受体系统中，pKi 值为 8.7±0.06。
靶点
Target Value
PGI2
(in human platelets) 9.3(pKi)
PGI2
(in a recombinant IP receptor system) 8.7(pKi)
体外研究

RO1138452 is IP receptor antagonist. The pIC ₅₀ 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 imidazoline ₂ (I ₂ ) (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.
体内研究

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).