KF 13218
目录号 : GC32653
KF13218是一种有效和持久的选择性血栓烷B2(TXB2)合成酶抑制剂，IC50值为5.3±1.3nM。
Cas No.:127654-03-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
KF 13218 is a potent, selective and long lasting thromboxane B2 (TXB2) synthase inhibitor with an IC50 value of 5.3±1.3 nM.
KF 13218 inhibits human and bovine platelet thromboxane synthase with IC50 values of 27±5.8 nM (mean±S.E.M.) and 36±6.9 nM, respectively. KF 13218 does not inhibit cyclooxygenase or 5-lipoxygenase up to a dose of 100 μM and does not antagonize thromboxane A2/prostaglandin H2 receptors. KF 13218 inhibits arachidonic acid-induced thromboxane B2 production by human intact platelets with an IC50 value of 5.3±1.3 nM. The IC50 value of KF 13218 for the intact platelets is about 5 times lower than that for the microsomal enzyme. The inhibition of thromboxane synthase in platelets by KF 13218 is sustained after removal of the extracellular compound[1].
After oral dosing in rat from 0.03 mg/kg to 3 mg/kg, KF 13218 dose-dependently inhibits the thromboxane B2 production in serum, and the inhibition is retained for 72 h. KF 13218, at a dose of 0.1 mg/kg p.o. prevents mortality induced by sodium arachidonate in rabbit[1].
[1]. Miki I, et al. A novel pyridobenzazepinone derivative with long lasting thromboxane synthase inhibition. Arzneimittelforschung. 1995 Oct;45(10):1066-70.
| Cas No. | 127654-03-9 | SDF | |
| Canonical SMILES | O=C(O)CCCC/C=C1C(C=NC=C2)=C2C(N(C)C3=CC=CC=C\13)=O | ||
| 分子式 | C20H20N2O3 | 分子量 | 336.38 |
| 溶解度 | Soluble in DMSO | 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 | 2.9728 mL | 14.8641 mL | 29.7283 mL |
| 5 mM | 0.5946 mL | 2.9728 mL | 5.9457 mL |
| 10 mM | 0.2973 mL | 1.4864 mL | 2.9728 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。
A novel pyridobenzazepinone derivative with long lasting thromboxane synthase inhibition
Arzneimittelforschung 1995 Oct;45(10):1066-70.PMID:8595060doi
A novel pyridobenzazepinone derivative (Z)-11-(5-carboxypentylidene)-6-methyl-5, 11-dihydropyrido +ad4,3-C] [1] benzazepin-5 (6H)-one (CAS 127654-03-9, KF 13218), inhibited human and bovine platelet thromboxane synthase with IC50 values of 27 +/- 5.8 nmol/l (mean +/- S.E.M.) and 36 +/- 6.9 nmol/l, respectively. The compound did not inhibit cyclooxygenase or 5-lipoxygenase up to a dose of 100 mumol/l and did not antagonize thromboxane A2/prostaglandin H2 receptors. KF13218 inhibited arachidonic acid-induced thromboxane B2 production by human intact platelets with an IC50 value of 5.3 +/- 1.3 nmol/l. The IC50 value of KF13218 for the intact platelets was about 5 times lower than that for the microsomal enzyme. The inhibition of thromboxane synthase in platelets by KF13218 was sustained after removal of the extracellular compound. After oral dosing in rat from 0.03 mg/kg to 3 mg/kg, KF13218 dose-dependently inhibited the thromboxane B2 production in serum, and the inhibition was retained for 72 h. KF13218, at a dose of 0.1 mg/kg p.o. prevented mortality induced by sodium arachidonate in rabbit. It is concluded that KF13218 is a potent, selective and long lasting thromboxane synthase inhibitor.