An ago-PAM of GLP-1R
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VU0453379 (hydrochloride)

Item No. 41392

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-cyclopentyl-2,9-dihydro-9-methyl-N-[[(2S)-1-(1-methylethyl)-2-pyrrolidinyl]methyl]-1-oxo-1H-pyrido[3,4-b]indole-4-carboxamide, monohydrochloride
Molecular Formula
C26H34N4O2 • HCl
Formula Weight
471.0
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Sparingly soluble: 1-10 mg/ml
SMILES
O=C(C(C(C1=CC=CC=C12)=C3N2C)=CN(C4CCCC4)C3=O)NC[C@@H]5CCCN5C(C)C.Cl
InChi Code
InChI=1S/C26H34N4O2.ClH/c1-17(2)29-14-8-11-19(29)15-27-25(31)21-16-30(18-9-4-5-10-18)26(32)24-23(21)20-12-6-7-13-22(20)28(24)3;/h6-7,12-13,16-19H,4-5,8-11,14-15H2,1-3H3,(H,27,31);1H/t19-;/m0./s1
InChi Key
OCMGNMGYQPPMFF-FYZYNONXSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $61

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    5 mg

    $273

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    10 mg

    $424

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    Cayman Chemical
    Explore Obesity & Metabolic Disease Resources

    Discover high-quality research tools to investigate GLP-1 mechanisms and next-generation metabolic targets.

    OBESITY RESEARCH SOLUTIONS
    Product Description

    VU0453379 is an allosteric agonist and positive allosteric modulator (ago-PAM) of glucagon-like peptide 1 receptor (GLP-1R).1 It induces calcium mobilization in 9-3-H cells expressing human GLP-1R (EC50 = 1.3 µM) and enhances GLP-1-, exenatide-, or liraglutide-induced calcium mobilization in the same cells (EC50s = 1.8, 8.4, and 30 µM, respectively). VU0453379 (30 µM) potentiates exenatide-induced insulin secretion in primary mouse pancreatic islets. It reverses catalepsy induced by haloperidol (Item No. 12014) in a rat model of Parkinson’s disease motor symptoms when administered at a dose of 30 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Morris, L.C., Nance, K.D., Gentry, P.R., et al. Discovery of (S)-2-cyclopentyl-N-((1-isopropylpyrrolidin2-yl)-9-methyl-1-oxo-2,9-dihydro-1H-pyrrido[3,4-b]indole-4-carboxamide (VU0453379): A novel, CNS penetrant glucagon-like peptide 1 receptor (GLP-1R) positive allosteric modulator (PAM). J. Med. Chem. 57(23), 10192-10197 (2014).