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SQ 29,548
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SQ 29,548图片
CAS NO:98672-91-4
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
SQ 29,548 是一种高亲和力放射性配体,是一种选择性血栓素-前列腺素 (TP) 受体拮抗剂。
Cas No.98672-91-4
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 SMILESOC(=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℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.