An inhibitor of GRK2/βARK1
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βARK1 Inhibitor

Item No. 21751

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[2-(5-nitro-2-furanyl)ethenyl]-2-furancarboxylic acid, methyl ester
CAS Number
24269-96-3
Molecular Formula
C12H9NO6
Formula Weight
263.2
Purity
≥95% (mixture of isomers)
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mLDMSO: 30 mg/mLDMSO:PBS (pH 7.2) (1:2): 0.3 mg/mLEthanol: slightly soluble
λmax
228, 298, 395 nm
SMILES
COC(C1=CC=C(/C=C/C2=CC=C([N+]([O-])=O)O2)O1)=O
InChi Code
InChI=1S/C12H9NO6/c1-17-12(14)10-6-4-8(18-10)2-3-9-5-7-11(19-9)13(15)16/h2-7H,1H3/b3-2+
InChi Key
YDJPHSNZGRVPCK-NSCUHMNNSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $157

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    10 mg

    $293

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    25 mg

    $680

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    βARK1 inhibitor is an inhibitor of G protein-coupled receptor kinase 2/β-adrenergic receptor kinase 1 (GRK2/βARK1; IC50 = 126 µM).1 It is selective for GRK2/βARK1 over PKA at concentrations up to 1 mM. βARK1 inhibitor decreases systolic blood pressure in ob/ob and nicotinamide plus streptozotocin-induced mouse models of type 2 diabetes when administered at a dose of 200 µg/kg.2 It also improves clonidine-induced relaxation of precontracted isolated aortic rings and improves glucose tolerance in the ob/ob mouse model. βARK1 inhibitor inhibits dopamine inhibition reversal (DIR) induced by serotonin (Item No. 14332) or neurotensin (Item No. 24717) in the rat ventral tegmental area in vitro.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Iino, M., Furugori, T., Mori, T., et al. Rational design and evaluation of new lead compound structures for selective betaARK1 inhibitors. J. Med. Chem. 45(11), 2150-2159 (2002).

    2. Taguchi, K., Matsumoto, T., Kamata, K., et al. Inhibitor of G protein-coupled receptor kinase 2 normalizes vascular endothelial function in type 2 diabetic mice by improving β-arrestin 2 translocation and ameliorating Akt/eNOS signal dysfunction. Endocrinology 153(7), 2985-2996 (2012).

    3. Nimitivai, S., McElvain, M.A., and Brodie, M.S. Reversal of dopamine D2 agonist-induced inhibition of ventral tegmental area neurons by Gq-linked neurotransmitters is dependent on protein kinase C, G protein-coupled receptor kinase, and dynamin. J. Pharmacol. Exp. Ther. 344(1), 253-263 (2013).