A partial agonist of GPR109A/HCA2 receptors
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LUF6283

Item No. 15423

Technical Information
Formal Name
5-butyl-1H-pyrazole-3-carboxylic acid
CAS Number
92933-48-7
Molecular Formula
C8H12N2O2
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMSO: 16 mg/mlEthanol: 16 mg/ml
λmax
218 nm
SMILES
O=C(O)C1=NNC(CCCC)=C1
InChi Code
InChI=1S/C8H12N2O2/c1-2-3-4-6-5-7(8(11)12)10-9-6/h5H,2-4H2,1H3,(H,9,10)(H,11,12)
InChi Key
ZJTXSGLJNBAMJS-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    LUF6283 is a partial agonist of GPR109A/HCA2 G protein-coupled receptors (Ki = 0.55 μM in a radioligand binding assay).1 It stimulates [35S]-GTPγS binding and increases phosphorylation of ERK in HEK293T cells expressing GPR109A/HCA2 receptors (EC50s = 3.1 and 0.32 μM, respectively). In vivo, LUF6283 (400 mg/kg per day) reduces plasma levels of VLDL and hepatic expression of apolipoprotein B in mice.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Li, Z., Blad, C.C., van der Sluis, R.J., et alEffects of pyrazole partial agonists on HCA2-mediated flushing and VLDL-triglyceride levels in mice. Br. J. Pharmacol. 167(4), 818-825 (2012).