A GCGR antagonist
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Glucagon Receptor Antagonist 4

Item No. 22164

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[(1S)-1-[3,5-dimethyl-4-[4-(trifluoromethyl)-1H-pyrazol-1-yl]phenoxy]butyl]benzoyl]-β-alanine
CAS Number
1393124-08-7
Synonyms
  • GCGR Antagonist IV
Molecular Formula
C26H28F3N3O4
Formula Weight
503.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 50mg/mLDMSO: 50mg/mLDMSO:PBS (pH 7.2) (1:1): 0.5mg/mLEthanol: 0.5mg/mL
λmax
234 nm
SMILES
CC1=C(N2C=C(C(F)(F)F)C=N2)C(C)=CC(O[C@@H](CCC)C3=CC=C(C(NCCC(O)=O)=O)C=C3)=C1
InChi Code
InChI=1S/C26H28F3N3O4/c1-4-5-22(18-6-8-19(9-7-18)25(35)30-11-10-23(33)34)36-21-12-16(2)24(17(3)13-21)32-15-20(14-31-32)26(27,28)29/h6-9,12-15,22H,4-5,10-11H2,1-3H3,(H,30,35)(H,33,34)/t22-/m0/s1
InChi Key
IBDYYOQKQCCSDP-QFIPXVFZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    25 mg

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    Glucagon receptor antagonist 4 is an antagonist of the glucagon receptor (GCGR; Ki = 14 nM for the human recombinant receptor).1 It is greater than 230-fold selective for GCGR over the glucagon-like peptide 1 (GLP-1) receptor, as well as a panel of 69 receptors, ion channels, uptake sites, and enzymes at 10 µM. Glucagon receptor antagonist 4 prevents glucagon-induced increases in glucose levels in rat blood when administered at doses of 7.5 and 75 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Guzman-Perez, A., Pfefferkorn, J.A., Lee, E.C., et al. The design and synthesis of a potent glucagon receptor antagonist with favorable physicochemical and pharmacokinetic properties as a candidate for the treatment of type 2 diabetes mellitus. Bioorg. Med. Chem. Lett. 23(10), 3051-3058 (2013).