RO1138452
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- CAS号:
- 221529-58-4
- 英文名:
- 4,5-DIHYDRO-N-[4-[[4-(1-METHYLETHOXY)PHENYL]METHYL]PHENYL]-1H-IMIDAZOL-2-AMINE
- 英文别名:
- CAY10441;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]-;RO-1138452,Inhibitor,RO1138452,CAY 10441,inhibit,CAY-10441,Prostaglandin Receptor,RO 1138452
- 中文名:
- RO1138452
- 中文别名:
- 化合物RO1138452;RO1138452游离态;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
- CBNumber:
- CB7455737
- 分子式:
- C19H23N3O
- 分子量:
- 309.41
- MOL File:
- 221529-58-4.mol
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RO1138452化学性质
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沸点:
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449.7±47.0 °C(Predicted)
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密度:
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1.13±0.1 g/cm3(Predicted)
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储存条件:
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under inert gas (nitrogen or Argon) at 2–8 °C
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溶解度:
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DMF: 30 mg/ml; DMF:PBS (pH 7.2)(1:10): 0.05 mg/ml; DMSO: 20 mg/ml; Ethanol: 20 mg/ml
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形态:
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A crystalline solid
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酸度系数(pKa):
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9.94±0.33(Predicted)
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RO1138452性质、用途与生产工艺
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。
| Target | Value |
PGI2
(in human platelets)
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9.3(pKi)
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PGI2
(in a recombinant IP receptor system)
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8.7(pKi)
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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).
RO1138452
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上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-108912 | RO1138452 | | 1 mg | 457元 |
| 2024/04/30 | HY-108912 | RO1138452
RO1138452 | 221529-58-4 | 5mg | 1300元 |
221529-58-4, RO1138452 相关搜索:
- API
- 合成有机化合物配体
- N-(4-(4-异丙基氧基苄基)苯基)-4,5-二氢-1H-咪唑-2-胺
- N-[4-(4-异丙氧基苄基)苯基]-4,5-二氢-1H-咪唑-2-胺
- 化合物RO1138452
- RO1138452游离态
- 221529-58-4
- RO-1138452,Inhibitor,RO1138452,CAY 10441,inhibit,CAY-10441,Prostaglandin Receptor,RO 1138452
- 1H-Imidazol-2-amine, 4,5-dihydro-N-[4-[[4-(1-methylethoxy)phenyl]methyl]phenyl]-
- RO 1138452;RO-1138452;RO1138452;CAY 10441;CAY-10441;CAY10441
- RO1138452 CAY10441
- CAY10441 RO1138452
- CAY10441
- N-(4-(4-Isopropoxybenzyl)phenyl)-4,5-dihydro-1H-imidazol-2-amine
- CAY10441 Exclusive
- RO1138452
- 4,5-DIHYDRO-N-[4-[[4-(1-METHYLETHOXY)PHENYL]METHYL]PHENYL]-1H-IMIDAZOL-2-AMINE