79094-20-5
中文名稱
達(dá)爾卓潘
英文名稱
Daltroban
CAS
79094-20-5
分子式
C16H16ClNO4S
MDL 編號(hào)
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 結(jié)構(gòu)式
基本信息
中文別名
2-[4-[2-(4-氯苯基)磺酰胺基乙基]苯基]乙酸達(dá)爾卓潘
達(dá)替氯銨
達(dá)曲班
4-[2-(4-氯苯磺酰氨基)乙基]苯乙酸
英文別名
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
所屬類別
藥物: 血液系統(tǒng)用藥物理化學(xué)性質(zhì)
外觀性狀從含水乙醇得白色結(jié)晶，熔點(diǎn)138～140℃。
熔點(diǎn)132.5-137.4 °C(lit.)
沸點(diǎn)555.3±60.0 °C(Predicted)
密度1.378±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO: 22 mg/mL, soluble
酸度系數(shù)(pKa)4.33±0.10(Predicted)
形態(tài)固體
顏色white
顏色白色
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
CAS 數(shù)據(jù)庫(kù)79094-20-5(CAS DataBase Reference)
安全數(shù)據(jù)
警示詞警告
危險(xiǎn)性描述H315-H319-H335
危險(xiǎn)品標(biāo)志Xi
危險(xiǎn)類別碼R36/37/38
安全說(shuō)明S26-S36/37
WGK Germany3
應(yīng)用領(lǐng)域
用途一
為血栓素A2受體的特異性強(qiáng)效拮抗劑，有抑制血小板聚集，影響血栓形成，防止猝死等作用。用于治療心肌缺血、出血性休克、內(nèi)毒性休克、心肺性猝死、急性腎衰竭、動(dòng)脈粥樣硬化等。制備方法
方法一
4-氰甲基苯乙酸溶于無(wú)水乙醇，加入氯化鈀和濃鹽酸，在室溫和0.5MPa通氫。濾除催化劑，濾液減壓蒸出溶劑。加入水，充分溶解，過(guò)濾，濾液為化合物(I)的溶液。往該溶液中，加入碳酸鉀，再在80℃加入對(duì)氯苯磺酰氯。加畢，在80℃攪拌。冷卻，用2mol/L鹽酸酸化至Ph值2。濾集固體，水洗，干燥。再用66%乙醇重結(jié)晶，得達(dá)曲班，熔點(diǎn)138～140℃。常見(jiàn)問(wèn)題列表
生物活性
Daltroban (BM-13505) 是一種選擇性和特異性血栓素 A2 (TXA2) 受體拮抗劑。Daltroban 增加血管平滑肌細(xì)胞內(nèi)鈣。Daltroban 對(duì)再灌注損傷有保護(hù)作用。靶點(diǎn)
|
TXA 2
|
體內(nèi)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. |