VU0810464
- Product Name
- VU0810464
- CAS No.
- 2126040-21-7
- Chemical Name
- VU0810464
- Synonyms
- VU0810464;VU0810464, 10 mM in DMSO;2-(3-Chloro-4-fluorophenyl)-N-(1-cyclohexyl-3-methyl-1H-pyrazol-5-yl)acetamide;Benzeneacetamide, 3-chloro-N-(1-cyclohexyl-3-methyl-1H-pyrazol-5-yl)-4-fluoro-;3-?Chloro-?N-?(1-?cyclohexyl-?3-?methyl-?1H-?pyrazol-?5-?yl)?-?4-?fluoro-benzeneacetamide;cells,KcsA,VU-0810464,Potassium Channel,neuronal GIRK,HPC,VU0810464,VU 0810464,SAN,inhibit,Inhibitor
- CBNumber
- CB65839814
- Molecular Formula
- C18H21ClFN3O
- Formula Weight
- 349.83
- MOL File
- 2126040-21-7.mol
VU0810464 Property
- Boiling point:
- 549.1±50.0 °C(Predicted)
- Density
- 1.31±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- DMSO: ≥ 250 mg/mL (714.63 mM)
- pka
- 13.35±0.70(Predicted)
- form
- Solid
- color
- White to off-white
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- CS-0093112
- Product name
- VU0810464
- Purity
- 99.72%
- Packaging
- 5mg
- Price
- $350
- Updated
- 2021/12/16
- Product number
- CS-0093112
- Product name
- VU0810464
- Purity
- 99.72%
- Packaging
- 10mg
- Price
- $550
- Updated
- 2021/12/16
- Product number
- CS-0093112
- Product name
- VU0810464
- Purity
- 99.72%
- Packaging
- 50mg
- Price
- $1950
- Updated
- 2021/12/16
- Product number
- A1219204
- Product name
- 2-(3-Chloro-4-fluorophenyl)-N-(1-cyclohexyl-3-methyl-1H-pyrazol-5-yl)acetamide
- Purity
- 98%
- Packaging
- 100mg
- Price
- $438
- Updated
- 2021/12/16
- Product number
- CSN25285
- Product name
- VU0810464
- Packaging
- 1mg
- Price
- $29
- Updated
- 2021/12/16
VU0810464 Chemical Properties,Usage,Production
Uses
VU0810464 is a potent and selective non-ureaG protein-gated inwardly-rectifying potassium channels (GIRK, Kir3) activator. VU0810464 displays nanomolar potency for neuronal (EC50=165 nM) and GIRK1/4 (EC50=720 nM) channels with improved brain penetration[1][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 of anxiolytic efficacy in wild mice, but had no impact in and Kcnj3 (Girk1) ?/? mice. |
References
[1] Vo BN, et al. VU0810464, a non-urea G protein-gated inwardly rectifying K+?(Kir?3/GIRK) channel activator, exhibits enhanced selectivity for neuronal Kir?3 channels and reduces stress-induced hyperthermia in mice.Br J Pharmacol.?2019 Jul;176(13):2238-2249. DOI:10.1111/bph.14671
[2] Wieting JM,et al. Discovery and Characterization of 1H-Pyrazol-5-yl-2-phenylacetamides as Novel, Non-Urea-Containing GIRK1/2 Potassium Channel Activators.ACS Chem Neurosci.?2017?Sep 20;8(9):1873-1879. DOI:10.1021/acschemneuro.7b00217
VU0810464 Preparation Products And Raw materials
Raw materials
Preparation Products
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