DP1 receptor agonist
货号：ajci12666
CAS：72814-32-5
分子式：C19H32N2O5
分子量：368.5
纯度：98%
存储：Store at -20°C
库存：现货
Background:
Target: DP1 receptor
IC50: 2.5 nM
Ki: 0.9 nM
BW 245C is a kind of prostaglandin analogue with stable chemical properties which functions as a potent inhibitor of platelet aggregation. BW 245C could selectively active the DP1 receptor, and inhibit [3H]-PGD2 binding to isolated human platelet membranes, with the Ki value of 0.9 nM [1].
In Vitro: BW 245C could inhibit the aggregation of human and rat platelets induced by ADP in a dose dependent manner, with the IC50 values of 8.7 nM and 9.9 nM, respectively [1]. Besides, in HEK293 cells stably expressing the hDP receptor, BW 245C could significantly increase cAMP production, with the EC50 value of 0.7 nM [2].
In Vivo: In spontaneously hypertensive rats, intravenous bolus injection with BW 245C at the dose of 250 μg/kg could reduce the systolic and diastolic blood pressure by 23% and 34%, respectively [1].
Clinical trial: In four healthy male volunteers, intravenous injection of BW 245C (1, 2 and 4 ng kg-1 min-1) exerted a progressive increase in heart rate and pulse pressure [3].
参考文献:
[1] Town H C, Casalsstenzel J, Schillinger E, et al. Pharmacological and cardiovascular properties of a hydantoin derivative, BW 245 C, with high affinity and selectivity for PGD2 receptors[J]. Prostaglandins, 1983, 25(1): 13-28.
[2] Boie Y, Sawyer N, Slipetz D, et al. MOLECULAR CLONING AND CHARACTERIZATION OF THE HUMAN PROSTANOID DP RECEPTOR[J]. Journal of Biological Chemistry, 1995, 270(32): 18910-18916.
[3] Orchard M A, Ritter J M, Shepherd G L, et al. Cardiovascular and platelet effects in man of BW 245C, a stable mimic of epoprostenol (PGI2)[J]. British journal of clinical pharmacology, 1983, 15(5): 509-511.
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