A GCGR antagonist
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MK-0893

Item No. 28923

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[(1S)-1-[3-(3,5-dichlorophenyl)-5-(6-methoxy-2-naphthalenyl)-1H-pyrazol-1-yl]ethyl]benzoyl]-β-alanine
CAS Number
870823-12-4
Molecular Formula
C32H27Cl2N3O4
Formula Weight
588.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/mlEthanol: Soluble: ≥ 10 mg/ml
SMILES
O=C(NCCC(O)=O)C1=CC=C([C@H](C)N2C(C3=CC=C(C=C(OC)C=C4)C4=C3)=CC(C5=CC(Cl)=CC(Cl)=C5)=N2)C=C1
InChi Code
InChI=1S/C32H27Cl2N3O4/c1-19(20-3-5-21(6-4-20)32(40)35-12-11-31(38)39)37-30(18-29(36-37)25-14-26(33)17-27(34)15-25)24-8-7-23-16-28(41-2)10-9-22(23)13-24/h3-10,13-19H,11-12H2,1-2H3,(H,35,40)(H,38,39)/t19-/m0/s1
InChi Key
DNTVJEMGHBIUMW-IBGZPJMESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $79

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    5 mg

    $356

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    10 mg

    $553

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    25 mg

    $889

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    Cayman Chemical
    Explore Obesity & Metabolic Disease Resources

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    OBESITY RESEARCH SOLUTIONS
    Product Description

    MK-0893 is an allosteric antagonist of the glucagon receptor (GCGR; IC50 = 15.7 nM).1,2 It is selective for GCGR over glucose-dependent insulinotropic polypeptide receptor (GIPR), glucagon-like peptide 1 receptor (GLP-1R), pituitary adenylate cyclase-activating peptide (PACAP) type 1 (PAC1) receptor, vasoactive intestinal polypeptide receptor 1 (VPAC1), and VPAC2 (IC50s = 1,020, >10,000, 9,200, 11,580, and 12,800 nM, respectively).2 MK-0893 (1 and 3 mg/kg) reduces glucagon-induced increases in blood glucose levels in rhesus monkeys.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jazayeri, A., Doré, A.S., Lamb, D., et al. Extra-helical binding site of a glucagon receptor antagonist. Nature 533(7602), 274-277 (2016).

    2. Xiong, Y., Guo, J., Candelore, M.R., et al. Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. J. Med. Chem. 55(13), 6137-6148 (2012).