EMPA
目录号 : KM4592 CAS No. : 680590-49-2 纯度 : 98%

EMPA 是一种高亲和力的,可逆的选择性 orexin OX2 受体拮抗剂。[3H] EMPA 与人和大鼠 OX2-HEK293 膜结合,KD 值分别为 1.1 和 1.4 nM。

规格 价格 是否有货 数量
1mg
In-stock
5mg
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10mg
In-stock
50mg 询价 In-stock
100mg 询价 In-stock

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生物活性

EMPA is a high-affinity, reversible and selective orexin OX2 receptor antagonist. [H]EMPA binds to human and rat OX2-HEK293 membranes with KD values of 1.1 and 1.4 nM respectively.

体外研究

EMPA competitively antagonizes orexin-A-and orexin-B-evoked accumulation of [H]inositol phosphates (IP) at hOX2 receptors with pA2 values of 8.6 and 8.8 respectively.
EMPA displaces the [H]EMPA binding from cell membranes containing human and rat OX2 receptors, with Ki values of 1.10±0.24 nM and 1.45±0.13 nM, respectively.
EMPA shows an IC50=5.75 µM, Ki=2.63 µM, and IC50=12.8 µM, Ki=5.8 µM in the binding assay at human and mouse V1a receptors, respectively.
In CHO(dHFr) cells stably expressing hOX2 receptors, EMPA inhibits orexin-A-or orexin-B-evoked [Ca]i response with IC50s of 8.8±1.7 nM and 7.9±1.7 nM, respectively.

体内研究

EMPA (1-300 mg/kg; i.p.) dose-dependently reverses this [Ala,D-Leu]orexin-B-induced hyperlocomotion without itself significantly affecting locomotor activity (LMA) in male NMRI mice.
EMPA (3-30 mg/kg; i.p.) induces a significant and dose-dependent reduction in the baseline LMA in france and male Wistar rats. EMPA (3-30 mg/kg; i.p.) demonstrates a clear dose-dependent inhibition of spontaneous activity as compared with vehicle-treated animals.

Animal Model: Male NMRI mice (20-30 g)
Dosage: 1, 3, 10, 30, 100, 300 mg/kg
Administration: Injected i.p. at a volume of 10 mL/kg
Result: Dose-dependently reversed this [Ala,D-Leu]orexin-B-induced hyperlocomotion without itself significantly affecting LMA.
Animal Model: France and Male Wistar rats (196-237 g)
Dosage: 3, 10, 30 mg/kg
Administration: Injected i.p. at a volume of 5 mL/kg
Result: Induced a significant and dose-dependent reduction in the baseline LMA.
Demonstrated a clear dose-dependent inhibition of spontaneous activity as compared with vehicle-treated animals.
分子式
C27H34N4O4S
分子量
454.54
CAS号
680590-49-2
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (110.00 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2000 mL 11.0001 mL 22.0003 mL
5 mM 0.4400 mL 2.2000 mL 4.4001 mL
10 mM 0.2200 mL 1.1000 mL 2.2000 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。-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: ≥ 2.5 mg/mL (5.50 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.50 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 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。

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.50 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 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。

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.50 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
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