KR-33493
目录号 : GC19214
An inhibitor of FAF1
Cas No.:1021497-97-1
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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. | |
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.
| 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 | ||
| 分子式 | C20H18BrN3O3S | 分子量 | 460.34 |
| 溶解度 | DMSO : ≥ 31 mg/mL (67.34 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。