SKF-96148
Daltroban
CAS: 79094-20-5
Molecular Formula: C16H16ClNO4S
SKF-96148 - Names and Identifiers
SKF-96148 - Physico-chemical Properties
| Molecular Formula | C16H16ClNO4S |
| Molar Mass | 353.82 |
| Density | 1.378±0.06 g/cm3(Predicted) |
| Melting Point | 132.5-137.4 °C(lit.) |
| Boling Point | 555.3±60.0 °C(Predicted) |
| Physical and Chemical Properties | The chemical properties are white crystals obtained from aqueous ethanol with a melting point of 138~140 ℃. |
| Use | Uses for thromboxane A2 receptor specific potent antagonists, inhibit platelet aggregation, affect thrombosis, prevent sudden death and other effects. For the treatment of myocardial ischemia, hemorrhagic Shock, toxicity Shock, sudden cardiac death, acute renal failure, atherosclerosis. |
SKF-96148 - Risk and Safety
| Hazard Symbols | Xi - Irritant |
| Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36/37 - Wear suitable protective clothing and gloves. |
SKF-96148 - Upstream Downstream Industry
| Raw Materials | Ethanol Potassium carbonate Palladium chloride 4-Chlorobenzenesulfonyl chloride [4-(cyanomethyl)phenyl]acetic acid |
SKF-96148 - Uses and synthesis methods
biological activity
Daltroban (BM-13505) is a selective and specific thromboxane A2 (TXA2) receptor antagonist. Daltroban increase calcium in vascular smooth muscle cells. Daltroban has protective effect on reperfusion injury.
target
TXA 2
in vivo studies
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.
production method
4-Cyanomethylphenylacetic acid is dissolved in absolute ethanol, palladium chloride and concentrated hydrochloric acid are added, and hydrogen is passed at room temperature and 0.5MPa. The catalyst is filtered out, and the filtrate is distilled out of the solvent under reduced pressure. Add water, fully dissolve, filter, and the filtrate is a solution of compound (I). To the solution, add potassium carbonate, and then add p-chlorobenzenesulfonyl chloride at 80°C. After adding, stir at 80 ℃. Cool and acidify with 2mol/L hydrochloric acid to Ph 2. Filter solids, wash with water and dry. Then recrystallize with 66% ethanol to get Dachuban with a melting point of 138~140 ℃.
Last Update：2024-04-09 15:16:16
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Raw Materials for SKF-96148
Ethanol
Potassium carbonate
Palladium chloride
4-Chlorobenzenesulfonyl chloride
[4-(cyanomethyl)phenyl]acetic acid
Potassium carbonate
Palladium chloride
4-Chlorobenzenesulfonyl chloride
[4-(cyanomethyl)phenyl]acetic acid