EMPA|cas:680590-49-2|西域试剂

EMPA,99.69%

产品编号：Bellancom-108682| CAS NO：680590-49-2| 分子式：C₂₃H₂₆N₄O₄S| 分子量：454.54

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-108682	￥600.00	杭州北京（现货）
Bellancom-108682	￥1500.00	杭州北京（现货）
Bellancom-108682	￥2500.00	杭州北京（现货）
Bellancom-108682	￥5500.00	杭州北京（现货）
Bellancom-108682	￥9500.00	杭州北京（现货）

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EMPA

产品介绍

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，K_D 值分别为 1.1 和 1.4 nM。

生物活性

EMPA is a high-affinity, reversible and selective orexin OX₂ receptor antagonist. [³H]EMPA binds to human and rat OX₂-HEK293 membranes with K_D values of 1.1 and 1.4 nM respectively.

体外研究

EMPA competitively antagonizes orexin-A-and orexin-B-evoked accumulation of [³H]inositol phosphates (IP) at hOX₂ receptors with pA₂ values of 8.6 and 8.8 respectively.
EMPA displaces the [³H]EMPA binding from cell membranes containing human and rat OX₂ receptors, with K_i values of 1.10±0.24 nM and 1.45±0.13 nM, respectively.
EMPA shows an IC₅₀=5.75 µM, K_i=2.63 µM, and IC₅₀=12.8 µM, K_i=5.8 µM in the binding assay at human and mouse V_1a receptors, respectively.
In CHO(dHFr^-) cells stably expressing hOX₂ receptors, EMPA inhibits orexin-A-or orexin-B-evoked [Ca²⁺]_i response with IC₅₀s of 8.8±1.7 nM and 7.9±1.7 nM, respectively.

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

体内研究

EMPA (1-300 mg/kg; i.p.) dose-dependently reverses this [Ala¹¹,D-Leu¹⁵]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.

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

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 [Ala¹¹,D-Leu¹⁵]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.

体内研究

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

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 [Ala¹¹,D-Leu¹⁵]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.

性状

Solid

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。
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: ≥ 2.5 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。
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: ≥ 2.5 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。