A GIRK1/2 and GIRK1/4 activator
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VU0810464

Item No. 43073

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-chloro-N-(1-cyclohexyl-3-methyl-1H-pyrazol-5-yl)-4-fluoro-benzeneacetamide
CAS Number
2126040-21-7
Molecular Formula
C18H21ClFN3O
Formula Weight
349.8
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Sparingly soluble: 1-10 mg/ml
SMILES
ClC1=CC(CC(NC2=CC(C)=NN2C3CCCCC3)=O)=CC=C1F
InChi Code
InChI=1S/C18H21ClFN3O/c1-12-9-17(23(22-12)14-5-3-2-4-6-14)21-18(24)11-13-7-8-16(20)15(19)10-13/h7-10,14H,2-6,11H2,1H3,(H,21,24)
InChi Key
HNJJARDABGKWSO-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $28

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    5 mg

    $104

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    10 mg

    $193

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    25 mg

    $345

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    Product Description

    VU0810464 is an activator of G protein-activated inward rectifier potassium channels (GIRKs), also known as Kir3.1 It induces GIRK1/2 and GIRK1/4 activity in a thallium flux assay using HEK293 cells expressing GIRK1 and GIRK2 or GIRK1 and GIRK4 (EC50s = 165 and 720 nM, respectively). VU0810464 (10 and 30 mg/kg, i.p.) reduces stress-induced hyperthermia in mice, but it does not affect the percentage of time spent or distance traveled in the open arms of the elevated plus maze in mice at 30 mg/kg.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wieting, J.M., Vadukoot, A.K., Sharma, S., 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. 8(9), 1873-1879 (2017).

    2. Vo, B.N., Abney, K.K., Anderson, A., et al. VU0810464, a non-urea G protein-gated inwardly rectifying K+ (Kir3/GIRK) channel activator, exhibits enhanced selectivity for neuronal Kir3 channels and reduces stress-induced hyperthermia in mice. Br. J. Pharmacol. 176(13), 2238-2249 (2019).