CAS NO: | 212481-66-8 |
包装 | 价格(元) |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
生物活性 | ABT-546 (A-216546) is a potent, highly selective and activeendothelinETAreceptorantagonist with aKiof 0.46 nM for [125I]endothelin-1 binding to clonedhuman endothelinETA. ABT-546 is >25,000-fold more selective for theETAreceptorthan for theETBreceptor. ABT-546 blocks endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis withIC50of 0.59 nM and 3 nM, respectively[1]. | ||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | ABT-546 (A-216546) effectively inhibits specific I endothelin-1 binding to endothelin ETAreceptor in membranes prepared from rat pituitary MMQ cells with an IC50value of 0.56 nM. ABT-546 is much less effective in inhibiting specific [125I]endothelin-3 binding to endothelin ETBrceptor in membranes prepared from porcine cerebellum with an IC50value of 16,700 nM. In membranes prepared from CHO cells stably transfected with the human endothelin ETAand ETBreceptors, ABT-546 again effectively inhibits specific [125I]endothelin-1 binding to endothelin ETAreceptor with an IC50value of 0.49 nM, but is less effective in inhibiting specific [125I]endothelin-3 binding to endothelin ETBreceptor with an IC50value of 15,400 nM[1]. | ||||||||
体内研究 (In Vivo) | ABT-546 (A-216546; 0-100 mg/kg; oral administration; for 1 hour or 4 hours; male Sprague-Dawley rats) treatment dose-dependently blocks endothelin-1-induced pressor response in conscious rats[1].
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分子量 | 532.71 | ||||||||
Formula | C30H48N2O6 | ||||||||
CAS 号 | 212481-66-8 | ||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |