A positive allosteric modulator of GLP-1R
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LSN3318839

Item No. 41245

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[1-[(1R)-1-(2,6-dichloro-3-cyclopropylphenyl)ethyl]-1H-imidazo[4,5-c]pyridin-6-yl]-αR-methyl-benzeneacetic acid
CAS Number
2764704-18-7
Molecular Formula
C26H23Cl2N3O2
Formula Weight
480.4
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
ClC(C(C1CC1)=CC=C2Cl)=C2[C@@H](C)N3C=NC4=CN=C(C=C43)C5=C(C=CC=C5)[C@@H](C)C(O)=O
InChi Code
InChI=1S/C26H23Cl2N3O2/c1-14(26(32)33)17-5-3-4-6-19(17)21-11-23-22(12-29-21)30-13-31(23)15(2)24-20(27)10-9-18(25(24)28)16-7-8-16/h3-6,9-16H,7-8H2,1-2H3,(H,32,33)/t14-,15-/m1/s1
InChi Key
JPJWHCNGSBCZMI-HUUCEWRRSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    500 µg

    $148

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    1 mg

    $281

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    LSN3318839 is a positive allosteric modulator (PAM) of glucagon-like peptide 1 receptor (GLP-1R).1 It potentiates increases in cAMP accumulation induced by the GLP-1R full agonist GLP-1 (9-36), but not the GLP-1R partial agonist GLP-1 (7-36), in INS-1 832/3 cells. LSN3318839 (1 and 3 µM) increases insulin levels in the presence, but not absence, of GLP-1 (9-36) in INS-1 832/3 cells under high-glucose conditions. It reduces blood glucose levels in glucose-dependent insulinotropic polypeptide receptor (GIPR) knockout mice in an oral glucose tolerance test when administered at a dose of 30 mg/kg and has an additive effect on reducing blood glucose levels in GIPR knockout mice when administered at 10 or 30 mg/kg in combination with the dipeptidyl peptidase 4 (DPP-4) inhibitor sitagliptin.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Willard, F.S., Wainscott, D.B., Showalter, A.D., et al. Discovery of an orally efficacious positive allosteric modulator of the glucagon-like peptide-1 receptor. J. Med. Chem. 64(6), 3439-3448 (2021).