Revefenacin

Revefenacin
  • Name: Revefenacin
  • Catalog No.: CPDD1221
  • CAS No.: 864750-70-9
  • Molecular Weight: 597.76
  • Chemical Formula: C35H43N5O4
  • For scientific research only, not for patients.

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    Pack Size Availability Price (USD)
    10mg In stock 200
    100mg In stock 800
    1g In stock 3400
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    Chemical Name:

    1-(2-(3-((4-carbamoylpiperidin-1-yl)methyl)-N-methylbenzamido)ethyl)piperidin-4-yl [1,1'-biphenyl]-2-ylcarbamate

    SMILES Code: 

    O=C(OC1CCN(CCN(C)C(C2=CC=C(CN3CCC(C(N)=O)CC3)C=C2)=O)CC1)NC4=CC=CC=C4C5=CC=CC=C5

    InChi Code:

    InChI=1S/C35H43N5O4/c1-38(34(42)29-13-11-26(12-14-29)25-40-19-15-28(16-20-40)33(36)41)23-24-39-21-17-30(18-22-39)44-35(43)37-32-10-6-5-9-31(32)27-7-3-2-4-8-27/h2-14,28,30H,15-25H2,1H3,(H2,36,41)(H,37,43)

    InChi Key:

    FYDWDCIFZSGNBU-UHFFFAOYSA-N

    Keyword:

    Revefenacin, TD-4208, GSK-1160724, TD4208, TD 4208, GSK1160724, GSK 1160724, 864750-70-9

    Solubility: Soluble in DMSO

    Storage: 0 - 4°C for short term (days to weeks), or -20°C for long term (months).

    Description: 

    In Vitro:The Kis of revefenacin are 0.42, 0.32, 0.18, 0.56, and 6.7 nM at human M1, M2, M3, M4 and M5 receptors, respectively. In a functional assay, revefenacin is shown to be a functional antagonist with inhibition constants similar to binding Ki's. Revefenacin also inhibits agonist-induced contraction of guinea pig isolated tracheal ring preparation with an affinity of 0.1 nM, similar to the measured M3 biding Ki[1]. In Vivo:In anesthetized dogs, revefenacin, along with tiotropium and glycopyrronium, produce sustained inhibition of acetylcholine-induced bronchoconstriction for up to 24 hours. In anesthetized rats, inhaled revefenacin exhibits dose-dependent 24-hour bronchoprotection against methacholine-induced bronchoconstriction. The estimated 24-hour potency is 45.0 µg/mL and the bronchoprotective potencies are maintained after 7 days of once-daily dosing[2].

    Target: mAChR




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