CAS NO: | 72814-32-5 |
包装 | 价格(元) |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 368.5 |
Cas No. | 72814-32-5 |
Formula | C19H32N2O5 |
Solubility | ≤50mg/ml in ethanol;50mg/ml in DMSO;50mg/ml in dimethyl formamide |
Chemical Name | (4S)-(3-[(3R,S)-3-cyclohexyl-3-hydroxypropyl]-2,5-dioxo)-4-imidazolidineheptanoic acid |
Canonical SMILES | O=C(N1[H])[C@H](CCCCCCC(O)=O)N(CCC(O)C2CCCCC2)C1=O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
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].
References:
[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.