达尔卓潘

生物活性靶点体内研究达尔卓潘试剂级价格

达尔卓潘

CAS号:79094-20-5
英文名:Daltroban
中文名:达尔卓潘
CBNumber:CB3384707
分子式:C16H16ClNO4S
分子量:353.82
MOL File:79094-20-5.mol

达尔卓潘化学性质

熔点 :132.5-137.4 °C(lit.)
沸点 :555.3±60.0 °C(Predicted)
密度 :1.378±0.06 g/cm3(Predicted)
储存条件 :Store at -20°C
溶解度 :DMSO: 22 mg/mL, soluble
形态 :A solid
酸度系数(pKa) :4.33±0.10(Predicted)
颜色 :white
InChI :InChI=1S/C16H16ClNO4S/c17-14-5-7-15(8-6-14)23(21,22)18-10-9-12-1-3-13(4-2-12)11-16(19)20/h1-8,18H,9-11H2,(H,19,20)
InChIKey :IULOBWFWYDMECP-UHFFFAOYSA-N
SMILES :C1(CC(O)=O)=CC=C(CCNS(C2=CC=C(Cl)C=C2)(=O)=O)C=C1
CAS 数据库 :79094-20-5(CAS DataBase Reference)

安全信息

危险品标志 :Xi
危险类别码 :36/37/38
安全说明 :26-36/37
WGK Germany :3

达尔卓潘性质、用途与生产工艺

生物活性 Daltroban (BM-13505) 是一种选择性和特异性血栓素 A2 (TXA2) 受体拮抗剂。Daltroban 增加血管平滑肌细胞内钙。Daltroban 对再灌注损伤有保护作用。
靶点

TXA ₂

体内研究

Daltroban (BM-13505) (1 mg/kg; i.v.; per hour) exerts protective effect in reperfusion injury following acute myocardial ischemia in cats.
In comparison with vehicle (physiological saline)-treated cats, Daltroban (20 mg/kg per hour i.v.) reduces the ischaemia-induced rise in the ST segment and prevented the development of a Q-wave in the ECG during reperfusion. Daltroban protects the myocardium from ischaemic injury and that this effect involves prevention of ischaemia-induced leukocytosis.

Animal Model:	Adult male cats (2.8 to 4.6 kg; anesthetized cat model)
Dosage:	1 mg/kg
Administration:	i.v.; 30 minutes before reperfusion at a rate of 1 mg/kg followed by 1 mg/kg/hour
Result:	Significantly reduced the area of ischemic tissue as a percent of total left ventricular mass and total area at risk, without altering basic hemodynamics and thereby not influencing myocardial oxygen demand.

化学性质从含水乙醇得白色结晶，熔点138～140℃。
用途为血栓素A2受体的特异性强效拮抗剂，有抑制血小板聚集，影响血栓形成，防止猝死等作用。用于治疗心肌缺血、出血性休克、内毒性休克、心肺性猝死、急性肾衰竭、动脉粥样硬化等。
生产方法 4-氰甲基苯乙酸溶于无水乙醇，加入氯化钯和浓盐酸，在室温和0.5MPa通氢。滤除催化剂，滤液减压蒸出溶剂。加入水，充分溶解，过滤，滤液为化合物(I)的溶液。往该溶液中，加入碳酸钾，再在80℃加入对氯苯磺酰氯。加毕，在80℃搅拌。冷却，用2mol/L盐酸酸化至Ph值2。滤集固体，水洗，干燥。再用66%乙醇重结晶，得达曲班，熔点138～140℃。