An HCA2 receptor agonist
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MK-1903

Item No. 34304

Technical Information
Formal Name
4,4aR,5,5aR-tetrahydro-1H-cyclopropa[4,5]cyclopenta[1,2-c]pyrazole-3-carboxylic acid
CAS Number
1268882-43-4
Molecular Formula
C8H8N2O2
Formula Weight
Purity
≥98%
Formulation
A solid
DMF: 25 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.3 mg/mlEthanol: 20 mg/ml
λmax
229, 258 nm
SMILES
OC(C1=NNC2=C1C[C@@]3([H])[C@]2([H])C3)=O
InChi Code
InChI=1S/C8H8N2O2/c11-8(12)7-5-2-3-1-4(3)6(5)9-10-7/h3-4H,1-2H2,(H,9,10)(H,11,12)/t3-,4-/m0/s1
InChi Key
CUTZNERBKDMLAP-IMJSIDKUSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    MK-1903 is an agonist of hydroxycarboxylic acid receptor 2 (HCA2), known previously as G protein-coupled receptor 109A (GPR109A).1 It reduces forskolin-induced cAMP production in a homogenous time-resolved fluorescence (HTRF) assay using CHO cells expressing the human receptor (EC50 = 12.9 nM). MK-1903 is selective for HCA2 over a panel of G protein-coupled receptors (GPCRs) and ion channels (IC50s = >10 µM for all). It reduces plasma free fatty acid levels in fasted rats when administered at doses ranging from 0.001 to 100 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Boatman, P.D., Lauring, B., Schrader, T.O., et al(1aR,5aR)1a,3,5,5a-Tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid (MK-1903): A potent GPR109a agonist that lowers free fatty acids in humans. J. Med. Chem. 55(8), 3644-3666 (2012).