SQ 29,548
(Synonyms: 1S-[1Α,2Β(5Z),3Β,4Α]]-7-[3-[2-(苯氨基甲酰基)肼基甲基]-7-氧代双环[2.2.1]庚-2-基]-5-庚烯酸) 目录号 : GC15213A selective TP receptor antagonist
Cas No.:98672-91-4
Sample solution is provided at 25 µL, 10mM.
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SQ 29,548 is a novel and selective thromboxane antagonist [1]. Thromboxane belongs to a family of lipids involved in clot formation (thrombosis). Thromboxane is a vasoconstrictor and a potent hypertensive agent which facilitates platelet aggregation [2].
In vitro: In guinea-pig trachea and rat aorta, SQ 29,548 competitively antagonized the activity of 9,11-azo PGH2 with pA2 values of 7.8 and 8.4, respectively. SQ 29,548 competitively antagonized contractions of guinea-pig tracheal spirals induced by 11,9-epoxymethano PGH2 with the pA2 value of 9.1. The SQ 29,548 competitively antagonized tracheal induced by 11,9-epoxymethano PGH2 and PGD2 with the pA2 values of 8.2 and 8.3, respectively. SQ 29,548 partially antagonized the contractions of guinea-pig tracheal spirals caused by PGE2. SQ 29,548 significantly inhibited the aorta contracting activity of 11,9-epoxymethano PGH2 (pA2 = 9.1) and thromboxane A2 released from perfused guinea-pig lungs upon arachidonic acid challenge [1].
In vivo: In anesthetized dogs, SQ 29,548 (0.2 mg/kg/h) completely inhibited the vasoconstrictor response of the left circumflex coronary artery (LCX) caused by U-46619. SQ 28,585 showed no effects on infarct size as compared with vehicle controls [3]. In sham MI rats, treatment with SQ-29,548 significantly blunted this loss of CK activity and amino-nitrogen concentration from the ischemic myocardium. SQ-29,548 significantly prevented the extension of ischemic damage in the myocardium and improved survival following acute coronary artery ligation [4].
References:
[1] Ogletree M L, Harris D N, Greenberg R, et al. Pharmacological actions of SQ 29,548, a novel selective thromboxane antagonist[J]. Journal of Pharmacology and Experimental Therapeutics, 1985, 234(2): 435-441.
[2] Abe T, Takeuchi K, Takahashi N, et al. Rat kidney thromboxane receptor: molecular cloning, signal transduction, and intrarenal expression localization[J]. Journal of Clinical Investigation, 1995, 96(2): 657.
[3] Grover G J, Schumacher W A. Effect of the thromboxane receptor antagonist SQ 29,548 on myocardial infarct size in dogs[J]. Journal of cardiovascular pharmacology, 1988, 11(1): 29-35.
[4] Hock C E, Brezinski M E, Lefer A M. Anti-ischemic actions of a new thromboxane receptor antagonist, SQ-29,548, in acute myocardial ischemia[J]. European journal of pharmacology, 1986, 122(2): 213-219.
| Cas No. | 98672-91-4 | SDF | |
| 别名 | 1S-[1Α,2Β(5Z),3Β,4Α]]-7-[3-[2-(苯氨基甲酰基)肼基甲基]-7-氧代双环[2.2.1]庚-2-基]-5-庚烯酸 | ||
| 化学名 | [1S-[1α,2α(Z),3α,4α]]-7-[3-[[2-[(phenylamino)carbonyl]hydrazino]methyl]-7-oxabicyclo[2.2.1]hept-2-yl]-5-heptenoic acid | ||
| Canonical SMILES | OC(=O)CCC/C=C\CC1C2CCC(O2)C1CNNC(=O)Nc1ccccc1 | ||
| 分子式 | C21H29N3O4 | 分子量 | 387.5 |
| 溶解度 | ≤0.9mg/ml in ethanol;5mg/ml in DMSO;0.14mg/ml in dimethyl formamide | 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 | 2.5806 mL | 12.9032 mL | 25.8065 mL |
| 5 mM | 0.5161 mL | 2.5806 mL | 5.1613 mL |
| 10 mM | 0.2581 mL | 1.2903 mL | 2.5806 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