221529-58-4
基本信息
RO1138452游離態(tài)
N-[4-(4-異丙氧基芐基)苯基]-4,5-二氫-1H-咪唑-2-胺
RO1138452
CAY10441 RO1138452
RO1138452 CAY10441
CAY10441 Exclusive
RO 1138452
RO-1138452
RO1138452
CAY 10441
CAY-10441
CAY10441
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
1H-Imidazol-2-amine, 4,5-dihydro-N-[4-[[4-(1-methylethoxy)phenyl]methyl]phenyl]-
物理化學(xué)性質(zhì)
常見問(wèn)題列表
Target | Value |
PGI2
(in human platelets) | 9.3(pKi) |
PGI2
(in a recombinant IP receptor system) | 8.7(pKi) |
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.
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).