A GCGR antagonist
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GRA Ex-25

Item No. 29727

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[[[trans-4-(1,1-dimethylethyl)cyclohexyl][[[4-(trifluoromethoxy)phenyl]amino]carbonyl]amino]methyl]benzoyl]-β-alanine
CAS Number
307983-31-9
Molecular Formula
C29H36F3N3O5
Formula Weight
563.6
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 25 mg/mlDMSO:PBS (pH 7.2) (1:8): 0.1 mg/mlEthanol: 10 mg/ml
λmax
241 nm
SMILES
FC(F)(F)OC1=CC=C(NC(N(CC2=CC=C(C(NCCC(O)=O)=O)C=C2)[C@@H]3CC[C@@H](C(C)(C)C)CC3)=O)C=C1
InChi Code
InChI=1S/C29H36F3N3O5/c1-28(2,3)21-8-12-23(13-9-21)35(27(39)34-22-10-14-24(15-11-22)40-29(30,31)32)18-19-4-6-20(7-5-19)26(38)33-17-16-25(36)37/h4-7,10-11,14-15,21,23H,8-9,12-13,16-18H2,1-3H3,(H,33,38)(H,34,39)(H,36,37)/t21-,23-
InChi Key
BZXMLCVDKDXRQY-AFARHQOCSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $153

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    10 mg

    $268

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    25 mg

    $587

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    GRA Ex-25 is a glucagon receptor (GCGR) antagonist (IC50s = 55 and 56 nM for the human and rat receptors, respectively).1 It inhibits adenylate cyclase activity induced by glucagon (Item No. 24204) with a Ki value of 254 nM.2 GRA Ex-25 (3 mg/kg, i.v.) reduces glucagon-induced increases in blood glucose levels in rats.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lau, J., Behrens, C., Sidelmann, U.G., et al. New β-alanine derivatives are orally available glucagon receptor antagonists. J. Med. Chem. 50(1), 113-128 (2007).

    2. Kurukulasuriya, R., Sorensen, B.K., Link, J.T., et al. Biaryl amide glucagon receptor antagonists. Bioorg. Med. Chem. Lett. 14(9), 2047-2050 (2004).