CGS 15435
目录号 : GC31981
CGS15435是一种有效的血栓烷(TxA2)合成酶抑制剂，IC50为1nM，比作用于环氧合酶，PGI2合成酶和脂氧合酶的选择性高100000倍。
Cas No.:95853-92-2
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
Kinase experiment: | Thromboxane synthetase, cyclooxygenase, prostacyclin synthetase, and lipoxygenase enzymes are prepared. For the individual enzyme assays. [1-14C]Arachidonic acid (AA) is incubated with partially purified enzyme obtained from human platelets (thromboxane synthetase), sheep seminal vesicles (cyclooxygenase), bovine aorta (prostacyclin synthetase), and guinea-pig leukocytes (lipoxygenase). At the end of the incubation period, the products are extracted into ethyl acetate, the extracts are evaporated to dryness, the residues are redissolved in acetone, and these solutions are spotted on thin layer chromatography plates. The plates are developed in the appropriate solvents, scanned and radioactive spots corresponding to those of TxB2, PGE2, 6-keto PGFu, and 5-HETE, are scraped off and counted by a radiospectrometer. The IC50 values are determined by employing a range of concentrations of test compounds over the linear range of the assay and analyzed graphically. All determinations are done in duplicate and repeated once[1]. |
Animal experiment: | Rabbits[1]Adult male New Zealand rabbits (2.3-3.5 kg) are anesthetized with sodium pentobarbital (30 mg/kg i.v.). The animals are tracheotomized and the left femoral artery and vein are cannulated for the recording of mean arterial blood pressure (MABP) and the injection of either vehicle or drug, respectively. The animals are allowed to stabilize for at least 15 rain prior to drug or vehicle administration. CGS 15435 and DAZ are dissolved in 2 mL of 0.5 M Tris buffer (pH 8.4) and injected i.v. over a 15 s period. CGS 15435 (8.6 μmol/kg; 3.1 mg/kg) is administered at 15 min (n=4) or 24 h (n=6) prior to AA. |
References: [1]. Olson RW, et al. CGS 15435A, a thromboxane synthetase inhibitor with an extended duration of action: a comparison with dazoxiben. Eur J Pharmacol. 1987 Jan 20;133(3):265-73. | |
CGS 15435, a potent thromboxane (TxA2) synthetase inhibitor with an IC50 of 1 nM, has a selectivity for Tx synthetase 100000-fold greater than that for cyclooxygenase, PGI2 synthetase and lipoxygenase enzymes.
CGS 15435 is a highly specific Tx synthetase inhibitor. CGS 15435 is only weakly effective as an inhibitor of PGE2 (Cyclooxygenase, IC50=1200 μM), prostacyclin (PGI2 synthetase, IC50=90 μM) or 5-Lipoxygenase (IC50=60 μM) product formation[1].
CGS 15435 has a long duration of action, since the increases in the plasma levels of TxB2 are prevented even at 24 h after CGS 15435 administration. CGS 15435 significantly inhibits TxB2 formation 4, 6, 12 and 24 h after dosing. Administration of CGS 15435 0.25 or 24 h prior to Arachidonic acid (AA) produced no increase in TxB2 in the surviving animals (4/4 and 5/6, respectively). The final TxB2 levels in the CGS15435A (0.25 and 24 h pretreatment) groups are significantly lower (P<0.05) than those seen in the AA or the Dazoxiben (2 h pretreatment) groups[1].
[1]. Olson RW, et al. CGS 15435A, a thromboxane synthetase inhibitor with an extended duration of action: a comparison with dazoxiben. Eur J Pharmacol. 1987 Jan 20;133(3):265-73.
| Cas No. | 95853-92-2 | SDF | |
| Canonical SMILES | O=C(O)CCCCCC1=C(C2=CC=CN=C2)N(C)C3=C1C=C(Cl)C=C3 | ||
| 分子式 | C20H21ClN2O2 | 分子量 | 356.85 |
| 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 | 2.8023 mL | 14.0115 mL | 28.023 mL |
| 5 mM | 0.5605 mL | 2.8023 mL | 5.6046 mL |
| 10 mM | 0.2802 mL | 1.4011 mL | 2.8023 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。