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。
生物活性 | EMPA is a high-affinity, reversible and selectiveorexinOX2receptorantagonist. [3H]EMPA binds to human and rat OX2-HEK293 membranes with KDvalues of 1.1 and 1.4 nM respectively[1]. |
IC50& Target[1] | |
体外研究 (In Vitro) | EMPA competitively antagonizes orexin-A-and orexin-B-evoked accumulation of [3H]inositol phosphates (IP) at hOX2receptors with pA2values of 8.6 and 8.8 respectively[1]. EMPA displaces the [3H]EMPA binding from cell membranes containing human and rat OX2receptors, with Kivalues of 1.10±0.24 nM and 1.45±0.13 nM, respectively[1]. 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 V1areceptors, respectively[1]. In CHO(dHFr-) cells stably expressing hOX2receptors, EMPA inhibits orexin-A-or orexin-B-evoked [Ca2+]iresponse with IC50s of 8.8±1.7 nM and 7.9±1.7 nM, respectively[1].
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体内研究 (In Vivo) | 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[1]. 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[1].
Animal Model: | Male NMRI mice (20-30 g)[1] | 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)[1] | 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. |
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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 |
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溶解性数据 | In Vitro: DMSO : 50 mg/mL(110.00 mM;Need ultrasonic) 配制储备液 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 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-CDin 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 μL20% 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。 *以上所有助溶剂都可在本网站选购。
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