EMPA
Modify Date: 2024-01-08 18:01:25
EMPA structure
|
Common Name | EMPA | ||
|---|---|---|---|---|
| CAS Number | 680590-49-2 | Molecular Weight | 454.54200 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C23H26N4O4S | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | N/A | |
| Symbol |
GHS07 |
Signal Word | Warning | |
Use of EMPAEMPA 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[1]. |
| Name | N-Ethyl-N2-(6-methoxy-3-pyridinyl)-N2-[(2-methylphenyl)sulfonyl]-N-(3-pyridinylmethyl)glycinamide |
|---|
| Description | 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[1]. |
|---|---|
| Related Catalog | |
| Target |
OX2 Receptor |
| In Vitro | 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[1]. 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[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 V1a receptors, respectively[1]. 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[1]. |
| 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. |
| References |
| Molecular Formula | C23H26N4O4S |
|---|---|
| Molecular Weight | 454.54200 |
| Exact Mass | 454.16700 |
| PSA | 101.08000 |
| LogP | 4.11840 |
| Storage condition | -20°C |
![[(6-methoxy-pyridin-3-yl)-(toluene-2-sulfonyl)-amino]-acetic acid structure](https://image.chemsrc.com/caspic/125/680591-44-0.png)
