KP496
目录号 : GC31983
KP49是一个有选择性的LeukotrieneD4andThromboxaneA2受体的双重拮抗剂。
Cas No.:217799-03-6
Sample solution is provided at 25 µL, 10mM.
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KP496 is a selective, dual antagonist for Leukotriene D4 receptor and Thromboxane A2 receptor.
KP496 significantly inhibits acute (day 7) and chronic (day 21) lung inflammation. KP496 attenuates the number of lymphocytes on day 7 and those of macrophages, neutrophils, and eosinophils on days 7 and 21. KP496 and prednisolone significantly suppress the increase of hydroxyl-L-proline content in the lung. Compare to respective vehicle control group, the inhibition ratio of KP496 and prednisolone for increase of hydroxyl-L-proline content is about 74 and 63%, respectively[1]. The KP496 (100 mg/head) group and prednisolone (10 mg/kg) group exhibit significant inhibition of numbers of infiltrating total cells, eosinophils, monocytes/macrophages, and lymphocytes compare with the control group. Infiltration of all types of cells except neutrophils is decreased in the KP496 (30m g/head) group, though not to significant extents[2].
[1]. Kurokawa S, et al. Effect of inhaled KP-496, a novel dual antagonist of the cysteinyl leukotriene and thromboxane A2 receptors, on a bleomycin-induced pulmonary fibrosis model in mice. Pulm Pharmacol Ther. 2010 Oct;23(5):425-31. [2]. Ishimura M, et al. Effects of KP-496, a novel dual antagonist for cysteinyl leukotriene receptor 1 and thromboxane A2 receptor, on Sephadex-induced airway inflammation in rats. Biol Pharm Bull. 2009 Jun;32(6):1057-61.
Animal experiment: | Male mice (9 weeks old, 33 to 42g are used) BLM solution (15 mg/mL) is intravenously injected into mice (0.1 mL/10 g of body weight) on day 0. Mice are sacrificed on day 7 or 21. They are exposed to an aerosol of KP496 (KP-496) solution (0.5%) for 30 min using a pressure nebulizer 1 h before and 3 h after BLM-injection on day 0. From day 1 to the day before sacrificed, mice are exposed to KP496 (0.5%) for 30 min morning and evening[1]. |
References: [1]. Kurokawa S, et al. Effect of inhaled KP-496, a novel dual antagonist of the cysteinyl leukotriene and thromboxane A2 receptors, on a bleomycin-induced pulmonary fibrosis model in mice. Pulm Pharmacol Ther. 2010 Oct;23(5):425-31. | |
| Cas No. | 217799-03-6 | SDF | |
| Canonical SMILES | O=C(O)C1=CC=CC=C1S(=O)(N(CCCCNS(=O)(C2=CC=C(Cl)C=C2)=O)CC3=CC=CC(OCC4=NC(C(C)C)=CS4)=C3)=O | ||
| 分子式 | C31H34ClN3O7S3 | 分子量 | 692.27 |
| 溶解度 | DMSO : 100 mg/mL (144.45 mM; Need ultrasonic) | 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。 |
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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.4445 mL | 7.2226 mL | 14.4452 mL |
| 5 mM | 0.2889 mL | 1.4445 mL | 2.889 mL |
| 10 mM | 0.1445 mL | 0.7223 mL | 1.4445 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet