KR-33493 |
رقم الكتالوجGC19214 |
KR-33493 هو مثبط قوي لموت الخلايا بوساطة Fas (FAF1)
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Cas No.: 1021497-97-1
Sample solution is provided at 25 µL, 10mM.
KR-33493 is a potent inhibitor of Fas-mediated cell death (FAF1).
Body weight changes of both sexes are not related to KR-33493 in all doses. In rats administrated KR-33493 for 4 weeks, no test article-related changes in any treated groups of either sex are found in hematology, serum biochemistry, and urinalysis. In dogs administrated KR-33493 for 2 weeks, red blood cell count (RBC) value in males is significantly higher at the 1000 mg/kg/day dose than that of the control group (i.e., 6.96±0.323 vs. 6.12±0.418). However, the change of RBC is recovered after the end of the administration period. The dose-normalized AUClast is not significantly different between the groups, suggesting that KR-33493 is governed by linear kinetics[1].
References:
[1]. Jeong JW, et al. Subacute toxicity evaluation of KR-33493, FAF1 inhibitor for a new anti-parkinson's disease agent, after oral administration in rats and dogs. Regul Toxicol Pharmacol. 2016 Nov;81:387-396.
Animal experiment: | A total of 93 male and 93 female specific pathogen-free rats (6 weeks of age), and 16 male and 16 female beagle dogs (8 months of age) are used in this study. In a toxicokinetic study, rat blood samples (approximately 0.6 mL) are collected into tubes containing heparin from the lateral tail vein at 0, 0.5, 1, 2, 4, 8, 12, and 24 h after dosing with KR-33493 at doses of 50, 150, and 500 mg/kg/day on Day 1 and Week 4. Dog blood samples (approximately 0.6 mL) are collected into tubes containing EDTA-2K from the cephalic vein at 0, 0.5, 1, 2, 4, 6, 8, and 24 h after dosing at KR-33493 doses of 50, 250, and 1000 mg/kg/day on Day 1 and Week 2. The plasma is separated by centrifugation (approximately 132,000 g, 3 min, 4°C) and stored at approximately -80°C until analysis. The KR-33493 concentration in plasma is quantified[1]. |
References: [1]. Jeong JW, et al. Subacute toxicity evaluation of KR-33493, FAF1 inhibitor for a new anti-parkinson's disease agent, after oral administration in rats and dogs. Regul Toxicol Pharmacol. 2016 Nov;81:387-396. |
Cas No. | 1021497-97-1 | SDF | |
Canonical SMILES | OC(C1=NN(CCC2=CC=CC=C2)C=C1NC(CSC3=CC=C(Br)C=C3)=O)=O | ||
Formula | C20H18BrN3O3S | M.Wt | 460.34 |
الذوبان | DMSO : ≥ 31 mg/mL (67.34 mM) | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
1 mM | 2.1723 mL | 10.8615 mL | 21.7231 mL |
5 mM | 0.4345 mL | 2.1723 mL | 4.3446 mL |
10 mM | 0.2172 mL | 1.0862 mL | 2.1723 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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