EMPA

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

EMPA 是食欲素 OX2 受体（人和大鼠 OX2-HEK293 膜，KD 值分别为 1.1 和 1.4 nM）的选择性、高亲和力和可逆拮抗剂。EMPA 取代含有人和大鼠 OX2 受体的细胞膜上的 EMPA 结合，Ki值分别为1.10±0.24 nM和1.45±0.13 nM。

EMPA is a selective, high-affinity and reversible antagonist of orexin OX2 receptor(human and rat OX2-HEK293 membranes with KD values of 1.1 and 1.4 nM respectively)EMPA displaces the 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 competitively antagonizes orexin-A-and orexin-B-evoked accumulation of inositol phosphates (IP) at hOX2 receptors with pA2 values of 8.6 and 8.8 respectively.?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.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 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 (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.

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Others

Other Targets

OX2 Receptor

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680590-49-2

454.54

C23H26N4O4S

>98% (HPLC)

DMSO:230 mg/mL (506 mM; Need ultrasonic)

CCN(Cc1cccnc1)C(=O)CN(c1ccc(OC)nc1)S(=O)(=O)c1ccccc1C

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(-20℃)

With Ice Pack

≥ 2 years