产品说明书
RO1138452
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同义名 : | CAY10441 |
| CAS号 : | 221529-58-4 | |
| 货号 : | A682702 | |
| 分子式 : | C19H23N3O | |
| 纯度 : | 97% | |
| 分子量 : | 309.405 | |
| MDL号 : | MFCD08062147 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(339.36 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO 无水乙醇: 50 mg/mL(161.6 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Prostacyclin (PGI2), a member of the eicosanoid family of lipid mediators, is a major product of arachidonic acid metabolism formed in the vascular endothelium and other tissues. PGI2 mediates its effects primarily through a membrane‐associated G protein‐coupled receptor termed the IP (prostacyclin) receptor[2]. RO1138452 is a potent and selective IP receptor antagonist, which displays high affinity for IP receptors. In human platelets, pKi is 9.3 ± 0.1; in a recombinant IP receptor system, pKi is 8.7 ± 0.06[2]. Functional antagonism of RO1138452 was studied by measuring inhibition of carbaprostacyclin-induced cAMP accumulation in CHO-K1 cells stably expressing the human IP receptor. The antagonist affinities (pKi) of RO1138452 was 9.0 ± 0.06. Selectivity profiles for RO1138452 was determined via a panel of receptor binding and enzyme assays. RO1138452 displayed affinity at imidazoline2 (I2) (8.3) and 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[3]. RO1138452 (1 - 10 mg/kg, i.v.) significantly reduced acetic acid-induced abdominal constrictions. RO1138452 (3-100 mg/kg, p.o.) significantly reduced 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)[2]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.23mL 0.65mL 0.32mL |
16.16mL 3.23mL 1.62mL |
32.32mL 6.46mL 3.23mL |
| 参考文献 |
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