2. GPCR/G Protein
  3. Angiotensin Receptor Endothelin Receptor
  4. BMS-248360

BMS-248360 是一种高效、有口服活性的血管紧张素 II 受体 (AT1) 和内皮素 A (ETA) 受体双拮抗剂，对 hAT1 和 hETA 受体作用的 Ki 值分别为 10 nM 和 1.9 nM。BMS-248360 具有抗高血压作用。

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BMS-248360 Chemical Structure

BMS-248360 Chemical Structure

CAS No. : 254737-87-6

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BMS-248360 相关抗体

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查看 Angiotensin Receptor 亚型特异性产品:

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AT1 Receptor AT2 Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BMS-248360 is a potent and orally active dual antagonist of both angiotensin II receptor (AT1) and endothelin A (ETA) receptor, with Kis of 10 nM and 1.9 nM for hAT1 and hETA receptor, respectively. BMS-248360 displays hypertensive effects[1].

IC50 & Target

Ki: 10 nM (hAT1), 1.9 nM (hETA receptor), 6.0 nM (rAT1), 1.9 nM(rETA receptor)[1]
体外研究
(In Vitro)

BMS-248360 shows activity against rat AT1 and rat ETA receptor, with Kis of 6.0 nM and 1.9 nM, respectively[1].
BMS-248360 shows no activity against AT2 and ETB receptor subtypes[1].

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

BMS-248360 相关抗体:
体内研究
(In Vivo)

BMS-248360 is found to be orally bioavailable in rats (%F=38) with excellent oral exposure (Cmax)=3.1 µM) and reasonable elimination profile (T1/2=5.5 hours)[1].
BMS-248360 (30 µmol/kg, 100 µmol/kg; p.o.) blocks the hypertensive effects of intravenously administered AII[1].

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

Animal Model: Male Rats[1]
Dosage: 30 µM/kg, 100 µM/kg
Administration: Oral administration
Result: Blocked the hypertensive effects of intravenously administered AII.
Animal Model: Male Rats[1]
Dosage: 10 µM/kg
Administration: Oral administration
Result: T1/2= 5.5 hours
分子量

659.84

Formula

C36H45N5O5S
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

BMS-248360 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • 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:

BMS-248360254737-87-6BMS248360BMS 248360Angiotensin ReceptorEndothelin ReceptorangiotensinAT1endothelinETAInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-114953
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