Laropiprant sodium 是一种有效的具有选择性的 DP 受体拮抗剂 (DP receptor)，Ki值为 0.57 nM，对 TP 受体的Ki值为 2.95 nM。
| 生物活性 | Laropiprant sodium is a potent and selectiveDPreceptorantagonist withKivalues of 0.57 nM and 2.95 nM forDPreceptor and TP Receptor, respectively[1][2][3]. |
| IC50& Target[2] | |
体外研究
(In Vitro) | Laropiprant sodium (0.01-1000 μM; 10 mins; HEK293 cells) is an Inverse Agonist of DP1 cAMP Signaling and reduces DP1 cAMP signaling below basal levels[1].
Laropiprant sodium (1 μM; 0-24 h; HEK293 cells) is a pharmacochaperone in promoting DP1 cell surface expression[1].
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体内研究
(In Vivo) | Laropiprant sodium (0-100 mg/kg; p.o. and i.v.; male Sprague-Dawley rats) exhibits good pharmacokinetic profiles[3].
| Animal Model: | Male Sprague-Dawley rats[3] | | Dosage: | 1, 5, 25 and 100 mg/kg | | Administration: | Oral administration and intravenous injection | | Result: | 1.19| Dose (mg/kg) | AUC0-∞(μM·hr) | Clp(ml/min/kg) | Vdss(L/kg) | T1/2(hr) | | 1 | 22.7 | 1.9 | 0.7 | 7.4 | | 5 | 96.0 | 2.1 | 0.9 | 7.6 |
1.19| Dose (mg/kg) | AUC0-∞(μM·hr) | Cmax(μM) | Tmax(hr) | F% | | 5 | 52.6 | 15.6 | 1.2 |
| | Clinical Trial | | | 分子量 | | | Formula | | | CAS 号 | | | 运输条件 | Room temperature in continental US; may vary elsewhere. | | 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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