1. GPCR/G Protein
    Neuronal Signaling
  2. Adrenergic Receptor
  3. Metipranolol

Metipranolol (Synonyms: 美替洛尔)

目录号: HY-121567 纯度: 98.36%
产品使用指南

Metipranolol 是一种非选择性的具有口服活性的 β-肾上腺素能受体 (β-adrenergic receptor) 拮抗剂。Metipranolol 可用于高血压和青光眼的研究。

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Metipranolol Chemical Structure

Metipranolol Chemical Structure

CAS No. : 22664-55-7

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Description

Metipranolol is a nonselective and orally active β-adrenergic receptor antagonist. Metipranolol can be used for hypertension and glaucoma research[1][2].

IC50 & Target[2]

β1 adrenoceptor

8.3 (pA2)

β2 adrenoceptor

8.4 (pA2)

In Vitro

In vitro β1- and β2-adrenoceptor antagonism is evaluated using the guinea pig atrium and the rat uterus, respectively. The respective pA2 values are 8.3 and 8.4[2].
Metipranolol significantly reduces iron/ascorbate-induced lipid peroxidation in rat brain homogenates with an IC50 value of 6.9 μM . Metipranolol also concentration-dependently inhibits sodium nitroprusside-stimulated lipid peroxidation in rat brain homogenates, displaying an IC50 value of 25.1 μM[3].

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

In Vivo

At postnatal day 35 (P35), rd10 mice given daily subcutaneous injections of 40 mg/kg of Metipranolol has reduction in markers of nitrosative stress, fewer TUNEL-positive cells, increased outer nuclear layer thickness, and substantially more staining for rhodopsin. At P50, Metipranolol-treated rd10 mice has decreased 3-nitrotyrosine staining in the retina, increased immunostaining for cone arrestin, a marker for cone photoreceptors, and significantly higher scotopic and photopic b-wave amplitudes at the highest stimulus intensity. At P65, cone density is significantly higher in Metipranolol-treated versus vehicle-injected rd10 mice[1].

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

Molecular Weight

309.40

Formula

C₁₇H₂₇NO₄

CAS No.

22664-55-7

中文名称

美替洛尔

SMILES

CC(OC1=C(C=C(C(C)=C1C)OCC(CNC(C)C)O)C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (808.02 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2321 mL 16.1603 mL 32.3206 mL
5 mM 0.6464 mL 3.2321 mL 6.4641 mL
10 mM 0.3232 mL 1.6160 mL 3.2321 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (6.72 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.72 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (6.72 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.72 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (6.72 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.72 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
References
  • 摩尔计算器

  • 稀释计算器

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Keywords:

MetipranololAdrenergic ReceptorBeta ReceptorNitrosativestresshypertensionglaucomaantioxidantlipidperoxidationInhibitorinhibitorinhibit

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