中文名 | RO1138452 |
英文名 | 4,5-DIHYDRO-N-[4-[[4-(1-METHYLETHOXY)PHENYL]METHYL]PHENYL]-1H-IMIDAZOL-2-AMINE |
别名 | RO1138452游离态 化合物RO1138452 N-[4-(4-异丙氧基苄基)苯基]-4,5-二氢-1H-咪唑-2-胺 N-(4-(4-异丙基氧基苄基)苯基)-4,5-二氢-1H-咪唑-2-胺 |
英文别名 | CAY10441 RO1138452 CAY 10441 CAY-10441 RO 1138452 RO-1138452 CAY10441 RO1138452 RO1138452 CAY10441 CAY10441 Exclusive N-(4-(4-Isopropoxybenzyl)phenyl)-4,5-dihydro-1H-imidazol-2-amine 4,5-DIHYDRO-N-[4-[[4-(1-METHYLETHOXY)PHENYL]METHYL]PHENYL]-1H-IMIDAZOL-2-AMINE |
CAS | 221529-58-4 |
化学式 | C19H23N3O |
分子量 | 309.41 |
密度 | 1.13±0.1 g/cm3(Predicted) |
沸点 | 449.7±47.0 °C(Predicted) |
酸度系数 | 9.94±0.33(Predicted) |
存储条件 | under inert gas (nitrogen or Argon) at 2–8 °C |
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). |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.232 ml | 16.16 ml | 32.32 ml |
5 mM | 0.646 ml | 3.232 ml | 6.464 ml |
10 mM | 0.323 ml | 1.616 ml | 3.232 ml |
5 mM | 0.065 ml | 0.323 ml | 0.646 ml |