2. Metabolic Enzyme/Protease
  3. Dopamine β-hydroxylase
  4. Etamicastat

Etamicastat  (Synonyms: BIA 5-453)

目录号: HY-14838
产品使用指南

摩尔计算器

Etamicastat (BIA 5-453) 是一种有效且可逆的多巴胺 β-羟化酶 (DBH) 抑制剂，IC50 值为 107 nM。可用于心血管疾病的研究。

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 Etamicastat hydrochloride 通常具有更好的水溶性和稳定性。

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Etamicastat Chemical Structure

Etamicastat Chemical Structure

CAS No. : 760173-05-5

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Etamicastat 的其他形式现货产品:

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Etamicastat 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Etamicastat (BIA 5-453) is a potent and reversible dopamine-β-hydroxylase (DBH) inhibitor with an IC50 value of 107 nM[1]. Etamicastat can be used in the research of cardiovascular diseases[2].

IC50 & Target

IC50: 107 nM (DBH)[1]
体外研究
(In Vitro)

Etamicastat blocks the hERG current amplitude with an IC50 value of 44 μg/mL (141 μM)[2].

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

Etamicastat 相关抗体:
体内研究
(In Vivo)

Etamicastat (100 mg/kg; administered intraperitoneally) leads to a significant reduction of noradrenaline levels in heart with concomitant increasing in dopamine levels[1].
Etamicastat (50 mg/kg; a single oral administration) exhibits moderate oral bioavailability (64%), Cmax (4.9 nM), and terminal elimination half-lives (T1/2=3.7 h) in male Wistar rats[1].

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

Animal Model: NMRi mice[1]
Dosage: 100 mg/kg
Administration: Administered intraperitoneally
Result: Led to a significant reduction of noradrenaline levels (36% control) in heart with concomitant increasing in dopamine levels (850% of control).
Animal Model: Male Wistar rats[1]
Dosage: 50 mg/kg (Pharmacokinetic Analysis)
Administration: Orally administered with at a dose volume of 10 mL/kg
Result: Oral bioavailability (64%), Cmax (4.9 nM), and (T1/2=3.7 h).
分子量

311.35

Formula

C14H15F2N3OS
CAS 号
中文名称

依他米司特
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

Etamicastat 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

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)
× = ×
C1   V1   C2   V2
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:

Etamicastat760173-05-5BIA 5-453依他米司特Dopamine β-hydroxylaseDopamine beta-hydroxylaseDopamine beta-monooxygenaseDopamine β-monooxygenaseCardiacriskDBHcardiovasculardiseasesInhibitorinhibitorinhibit

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