79094-20-5
中文名称
达尔卓潘
英文名称
Daltroban
CAS
79094-20-5
分子式
C16H16ClNO4S
MDL 编号
MFCD00868295
分子量
353.82
MOL 文件
79094-20-5.mol
更新日期
2024/08/28 21:53:41
79094-20-5 结构式
基本信息
中文别名
2-[4-[2-(4-氯苯基)磺酰胺基乙基]苯基]乙酸达尔卓潘
达替氯铵
达曲班
4-[2-(4-氯苯磺酰氨基)乙基]苯乙酸
英文别名
2-[4-[2-(4-chlorophenyl)sulfonylaminoethyl]phenyl]acetic acid4-[2-[(4-CHLOROPHENYLSULFONYL)AMINO]ETHYL]BENZENEACETIC ACID
BM-13505
DALTROBAN
SKF-96148
DatelliptiumChloride
4-[2-[(4-Chlorophenylsulfonyl)amino]ethyl]benzeneacetic acid, BM-13505, SKF-96148
4-[2-(4-Chlorobenzene-sulfonamido)ethyl]benzeneacetic acid
所属类别
药物: 血液系统用药物理化学性质
外观性状从含水乙醇得白色结晶,熔点138~140℃。
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-20°C储存
溶解度DMSO: 22 mg/mL, soluble
酸度系数(pKa)4.33±0.10(Predicted)
形态固体
颜色white
颜色白色
InChIInChI=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)
InChIKeyIULOBWFWYDMECP-UHFFFAOYSA-N
SMILESC1(CC(O)=O)=CC=C(CCNS(C2=CC=C(Cl)C=C2)(=O)=O)C=C1
制备方法
方法一
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℃。常见问题列表
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. |