RO1138452
中文名称 | RO1138452 |
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中文同义词 | 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 |
英文名称 | 4,5-DIHYDRO-N-[4-[[4-(1-METHYLETHOXY)PHENYL]METHYL]PHENYL]-1H-IMIDAZOL-2-AMINE |
英文同义词 | 4,5-DIHYDRO-N-[4-[[4-(1-METHYLETHOXY)PHENYL]METHYL]PHENYL]-1H-IMIDAZOL-2-AMINE;RO1138452;CAY10441 Exclusive;N-(4-(4-Isopropoxybenzyl)phenyl)-4,5-dihydro-1H-imidazol-2-amine;CAY10441;CAY10441 RO1138452;RO1138452 CAY10441;RO 1138452;RO-1138452;RO1138452;CAY 10441;CAY-10441;CAY10441 |
CAS号 | 221529-58-4 |
分子式 | C19H23N3O |
分子量 | 309.41 |
EINECS号 | |
相关类别 | API |
Mol文件 | 221529-58-4.mol |
结构式 |
RO1138452 性质
沸点 | 449.7±47.0 °C(Predicted) |
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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:30mg/mL; DMF:PBS (pH 7.2)(1:10):0.05 mg/ml; DMSO:20mg/mL;乙醇:20mg/mL |
形态 | 结晶固体 |
酸度系数(pKa) | 9.94±0.33(Predicted) |
颜色 | 浅黄至棕色 |
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).
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-108912 | RO1138452 | 1 mg | 457元 | |
2024/08/19 | HY-108912 | RO1138452 RO1138452 | 221529-58-4 | 5mg | 1300元 |