Molecular Formula | C17H12BrFN2O3 |
Molar Mass | 391.19 |
Density | 1.60 |
Melting Point | 184-186℃ (DEC.) |
Storage Condition | Store at RT |
In vitro study | Ponalrestat (ICI 128436; 1, 10, 100 μM; 6 hours) reduces PGF2αproduction in response to IL-1 in both cultured endometrial cells and endometrial explants. |
In vivo study | Ponalrestat (ICI 128436; 10, 50 mg/kg; orally; daily; 8 weeks) reduces sorbitol accumulation indicating efficacy of aldose reductase inhibition. Animal Model: Adult female Sprague-Dawley rats Dosage: 10, 50 mg/kg Administration: Orally; daily; 8 weeks Result: Reduced sorbitol accumulation. |
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. S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.556 ml | 12.782 ml | 25.563 ml |
5 mM | 0.511 ml | 2.556 ml | 5.113 ml |
10 mM | 0.256 ml | 1.278 ml | 2.556 ml |
5 mM | 0.051 ml | 0.256 ml | 0.511 ml |
overview | Polaris can be used as an intermediate in pharmaceutical synthesis. If you inhale Boris, please move the patient to fresh air; if you are in contact with the skin, you should remove the contaminated clothes, rinse the skin thoroughly with soapy water and water, and see a doctor if you feel uncomfortable; if you are in contact with the eyes, you should separate the eyelids, Rinse with flowing water or normal saline, and see a doctor immediately; if you eat, rinse your mouth immediately, prohibit vomiting, and see a doctor immediately. |
Biological activity | Ponalrestat (ICI 128436) is an orally active, selective and non-competitive aldose reductase (aldose reductase;AKR1B1;ALR) inhibitor. Ponalrestat can selectively inhibit ALR2,Ki is 7.7 nM, and the Ki value for ALR1 is 60 μM. Ponalrestat inhibits the conversion of glucose to sorbitol. |
target | Ki: 7.7 nM (ALR2) and 60 μM (ALR1) |
in vitro study | Ponalrestat (ICI 128436; 1, 10,100 μM; 6 hours) reduces PGF2αproduction in response to IL-1 in both cultured endometrial cells and endometrial explants. |
in vivo study | Ponalrestat (ICI 128436; 10, 50 mg/kg; orally; daily; 8 weeks) reduces sorbitol accumulation indicating efficacy of aldose reductase inhibition. Animal Model: Adult female Sprague-Dawley rats Dosage: 10, 50 mg/kg Administration: Orally; daily; 8 weeks Result: reduced sorbitol accumulation. |
Animal Model: | Adult female Sprague-Dawley rats |
Dosage: | 10, 50 mg/kg |
Administration: | Orally; daily; 8 weeks |
Result: | Reduced sorbitol accumulation. |