基本属性 生物活性靶点体外研究体内研究 用途与合成方法 RO1138452 价格(试剂级) 供应商 相关产品
网站主页  化工产品目录 生物  细胞培养  添加剂  小分子化合物  RO1138452

RO1138452

RO1138452

中文名称:RO1138452
英文名称:4,5-DIHYDRO-N-[4-[[4-(1-METHYLETHOXY)PHENYL]METHYL]PHENYL]-1H-IMIDAZOL-2-AMINE
CAS号:221529-58-4
分子式:C19H23N3O
分子量:309.41
EINECS号:
Mol文件:221529-58-4.mol
RO1138452 结构式

RO1138452 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: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)

RO1138452 用途与合成方法

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。
TargetValue
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).

RO1138452 价格(试剂级)

更新日期 产品编号 产品名称 CAS号 包装 价格
2024-01-25 HY-108912 1 mg 457
2024-01-25 HY-108912 RO1138452 221529-58-4 5mg 1300

RO1138452供应商 更多

天津凯利奇生物科技有限公司
现货
联系电话: 15076683720
产品介绍:
英文名称:RO1138452 CAY10441
CAS:221529-58-4
纯度:>98%
包装信息:2g
备注:2g
库存量:2g
现货日期:2024/3/22 10:46:06
江苏艾康生物医药研发有限公司
联系电话:025-66099280 17798518460
产品介绍:
英文名称:RO1138452
CAS:221529-58-4
纯度:95%
包装信息:1g;5g;10g
上海一飞生物科技有限公司
联系电话:021-65675885 18964387627
产品介绍:
英文名称:CAY10441 Exclusive
CAS:221529-58-4
纯度:98%
包装信息:5mg;10mg;25mg
备注:试剂级
上海超岚化工科技中心
联系电话:QQ:65489617 15618227136
产品介绍:
英文名称:RO1138452 CAY10441
CAS:221529-58-4
纯度:98% HPLC
包装信息:5MG;10MG;50MG;100MG,1G,5G
北京普西唐生物科技有限公司
联系电话:010-60605840 18892239720
产品介绍:
英文名称:RO1138452
CAS:221529-58-4
纯度:98%(HPLC)
包装信息:25mg;100mg;5mg

"RO1138452"相关产品信息