1. GPCR/G Protein Metabolic Enzyme/Protease
  2. Angiotensin Receptor Neprilysin
  3. TD-0212

TD-0212 (compound 35) 是一种具有口服活性的、血管紧张素II型1受体 AT1 和脑啡肽酶 (NEP)的双抑制剂,其对 AT1pKi 值为 8.9, 对 NEP 的pIC50值为9.2。

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 TD-0212 TFA 通常具有更好的水溶性和稳定性。

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TD-0212 Chemical Structure

TD-0212 Chemical Structure

CAS No. : 1073549-10-6

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TD-0212 的其他形式现货产品:

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查看 Angiotensin Receptor 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TD-0212 (compound 35) is an orally active dual pharmacology angiotensin II type 1 receptor (AT1) antagonist and neprilysin (NEP) inhibitor, with a pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP[1].

IC50 & Target

pKi: 8.9 (AT1)
pIC50: 9.2 (NEP)[1].

体外研究
(In Vitro)

TD-0212 (compound 35) provides the enhanced activity of dual AT1/NEP inhibition with a potentially lower risk of angioedema relative to dual ACE/NEP inhibition[1].

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

体内研究
(In Vivo)

TD-0212 (compound 35) produces blood pressure reductions similar to omapatrilat and combinations of AT1 receptor antagonists and NEP inhibitors in models of renin-dependent and –independent hypertension[1].

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

分子量

527.65

Formula

C28H34FN3O4S

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
  • 摩尔计算器

  • 稀释计算器

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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.

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产品名称:
TD-0212
目录号:
HY-114412
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