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VU0119498

CAS No. 79183-37-2

VU0119498( —— )

Catalog No. M21591 CAS No. 79183-37-2

VU0119498 is a M1 muscarinic receptor agonist (EC50 = 3.1 μM) and pan mAChR M3 M5 positive allosteric modulator (PAM)and is a neuroprotective agent.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    VU0119498
  • Note
    Research use only, not for human use.
  • Brief Description
    VU0119498 is a M1 muscarinic receptor agonist (EC50 = 3.1 μM) and pan mAChR M3 M5 positive allosteric modulator (PAM)and is a neuroprotective agent.
  • Description
    VU0119498 is a M1 muscarinic receptor agonist (EC50 = 3.1 μM) and pan mAChR M3 M5 positive allosteric modulator (PAM)and is a neuroprotective agent.
  • In Vitro
    VU0119498 (0.01-30 μM; 150 s) potentiates Ach responses in M1, M3, and M5-expressing CHO cells, with EC50s of 6.04, 6.38, and 4.08 μM, respectively.VU0119498 (3-20 μM) augments ACh-mediated increasing in insulin secretion and intracellular calcium levels in MIN6-K8 cells.VU0119498 (20 μM; 90 min) enhances ACh-induced insulin release in mouse and human pancreatic islets.
  • In Vivo
    VU0119498 (0.1-2 mg/kg; a single i.p.) improves glucose tolerance and insulin secretion in mice in a β-cell M3R-dependent fashion.VU0119498 (0.5 mg/kg; a single i.p.) improves glucose tolerance and insulin secretion in obese, glucose-intolerant mice. Animal Model:Male WT mice (12 weeks)Dosage: 0.1, 0.5, 2 mg/kg Administration:A single i.p.Result:Caused a significant improvement in glucose tolerance at the dose of 0.5 mg/kg.Significantly augmented GSIS at the dose of 0.5 mg/kg.
  • Synonyms
    ——
  • Pathway
    Endocrinology/Hormones
  • Target
    AChR
  • Recptor
    mAChR
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    79183-37-2
  • Formula Weight
    316.15
  • Molecular Formula
    C15H10BrNO2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 50 mg/mL (158.15 mM)
  • SMILES
    Brc1ccc(CN2C(=O)C(=O)c3ccccc23)cc1
  • Chemical Name
    1-[(4-bromophenyl)methyl]indole-23-dione

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Lu Zhu Mario Rossiet al.Allosteric Modulation of β-Cell M 3 Muscarinic Acetylcholine Receptors Greatly Improves Glucose Homeostasis in Lean and Obese Mice.Proc Natl Acad Sci U S A. 2019 Sep 10;116(37):18684-18690.
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