产品
编 号：F424664
分子式：C23H26N4O4S
分子量：454.54
分子式：C23H26N4O4S
分子量：454.54
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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25mg
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50mg
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结构图
CAS No: 680590-49-2
产品详情
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 KD values of 1.1 and 1.4 nM respectively.
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.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 hyperlocomotionwithout 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 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 [Ca2+]i response with IC50s of 8.8±1.7 nM and 7.9±1.7 nM, respectively.
EMPA is a high-affinity, reversible and selective orexin OX2 receptor antagonist. [3H]EMPA binds to human and rat OX2-HEK293 membranes with KD values of 1.1 and 1.4 nM respectively.
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.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 hyperlocomotionwithout 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 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 [Ca2+]i response with IC50s of 8.8±1.7 nM and 7.9±1.7 nM, respectively.
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