VU0810464(VU 0810464
Modify Date: 2024-04-11 09:53:19
VU0810464(VU 0810464 structure
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Common Name | VU0810464(VU 0810464 | ||
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| CAS Number | 2126040-21-7 | Molecular Weight | 349.834 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C18H21ClFN3O | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of VU0810464(VU 0810464VU0810464 (VU 0810464, VU464) is a selective neuronal GIRK channels activator, displays nanomolar potency for GIRK1/2 (EC50=163 nM) and improved brain penetration; exhibits comparable efficacy and potency compared with ML297, but VU0810464 is more selective for neuronal GIRK channels (GIRK1/4 EC50>500 nM); displays >3-fold more potent on GIRK1/2-expressing HEK293 cells compared to GIRK1/4-expressing cells, as measured using a Tl+ flux assay; reduced stress-induced hyperthermia in a GIRK-dependent manner in mice, ML297, but not VU0810464, decreased anxiety-related behavior as assessed with the elevated plus maze test. |
| Name | VU0810464 |
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| Description | VU0810464 (VU 0810464, VU464) is a selective neuronal GIRK channels activator, displays nanomolar potency for GIRK1/2 (EC50=163 nM) and improved brain penetration; exhibits comparable efficacy and potency compared with ML297, but VU0810464 is more selective for neuronal GIRK channels (GIRK1/4 EC50>500 nM); displays >3-fold more potent on GIRK1/2-expressing HEK293 cells compared to GIRK1/4-expressing cells, as measured using a Tl+ flux assay; reduced stress-induced hyperthermia in a GIRK-dependent manner in mice, ML297, but not VU0810464, decreased anxiety-related behavior as assessed with the elevated plus maze test. |
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| Related Catalog | |
| Target |
EC50: 165 nM (GIRK 1/2); 720 nM (GIRK1/4 )[1][2] |
| In Vitro | VU0810464 (0, 0.1, 0.3, 1, 3, 10, 30 μM) produces a concentration‐dependent response curves of currents in SAN and HPC cells, in addition, VU0810464 is 9‐fold higher potency for Kir3 channel activation in neurons as compared to SAN cells[2]. |
| In Vivo | VU0810464 (intraperitoneal injection; 30 mg/kg, 10 mg/kg; 30mg/kg; pre-treated 30 mins) produces a dose-dependent reduction of SIH response in Male C57BL/6J mice. To test if VU0810464 plays it role through Kir3 channel activation, VU0810464 (10 mg/kg) suppresses the SIH response in wild‐ type mice, but has no impact on Kcnj3−/− mice[2]. VU0810464 (intraperitoneal injection ; 30 mg/kg; 15, 30, 45, or 60 min post‐injection) displays a favourable distribution to the brain (Kp,uu = 0.83), has a improvement over ML297 (Kp,uu= 0.32). Clearance of VU0810464 is rapid,brain and plasma half-lives is 20 min in a PK study[2]. Animal Model: Male C57BL/6J mice, Kcnj3−/− siblings female and male C57BL/6J mice Dosage: 10 mg/kg; 30mg/kg Administration: Intraperitoneal injection Result: Reduced stress‐induced hyperthermia (SIH), a physiological test ofanxiolytic efficacy in wild mice, but had no impact in and Kcnj3 (Girk1) −/− mice. |
| References |
| Molecular Formula | C18H21ClFN3O |
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| Molecular Weight | 349.834 |
| Storage condition | -20°C |