2. GPCR/G Protein
  3. Endothelin Receptor
  4. ABT-546

ABT-546 (A-216546) 是一种有效的，高选择性和活性的内皮素 ETA 受体拮抗剂，对 [125I]-内皮素-1 与克隆的人 ETA 结合的 Ki 为 0.46 nM。ABT-546 对 ETA 的选择性比对 ETB 受体的选择性高 25,000 倍以上。ABT-546 阻断内皮素-1 诱导的花生四烯酸释放和磷脂酰肌醇水解，IC50 分别为 0.59 nM 和 3 nM。

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ABT-546 Chemical Structure

ABT-546 Chemical Structure

CAS No. : 212481-66-8

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ABT-546 相关抗体

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ABT-546 (A-216546) is a potent, highly selective and active endothelin ETA receptor antagonist with a Ki of 0.46 nM for [125I]endothelin-1 binding to cloned human endothelin ETA. ABT-546 is >25,000-fold more selective for the ETA receptor than for the ETB receptor. ABT-546 blocks endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis with IC50 of 0.59 nM and 3 nM, respectively[1].

IC50 & Target[1]

ETA

0.46 nM (Ki)

体外研究
(In Vitro)

ABT-546 (A-216546) effectively inhibits specific I endothelin-1 binding to endothelin ETA receptor in membranes prepared from rat pituitary MMQ cells with an IC50 value of 0.56 nM. ABT-546 is much less effective in inhibiting specific [125I]endothelin-3 binding to endothelin ETB rceptor in membranes prepared from porcine cerebellum with an IC50 value of 16,700 nM. In membranes prepared from CHO cells stably transfected with the human endothelin ETA and ETB receptors, ABT-546 again effectively inhibits specific [125I]endothelin-1 binding to endothelin ETA receptor with an IC50 value of 0.49 nM, but is less effective in inhibiting specific [125I]endothelin-3 binding to endothelin ETB receptor with an IC50 value of 15,400 nM[1].
In isolated vessels, ABT-546 inhibits endothelin ETA receptor-mediated endothelin-1-induced vasoconstriction, and endothelin ETB receptor-mediated sarafotoxin 6c-induces vasoconstriction with pA2 of 8.29 and 4.57, respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

ABT-546 相关抗体:
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats (250-350 g) induced with endothelin-1[1]
Dosage: 0.1 mg/kg, 1 mg/kg, 10 mg/kg, 30 mg/kg, 100 mg/kg
Administration: Oral administration; for 1 hour or 4 hours
Result: Exhibited a dose-dependent inhibition of the peak pressor response to endothelin-1, and statistically significant inhibition was achieved at doses of 3 to 100 mg/kg.
分子量

532.71

Formula

C30H48N2O6
CAS 号
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.
纯度 & 产品资料
参考文献

ABT-546 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ABT-546212481-66-8A-216546ABT546ABT 546A216546A 216546Endothelin ReceptorETAendothelin-1-mediatedphosphatidylinositolarachidonicacidreleasevasoconstrictionpressorInhibitorinhibitorinhibit

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产品名称：
ABT-546
目录号：
HY-135283
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