V116517

• Description :

  V116517 is a potent, orally active transient receptor potential vanilloid (TRPV1) antagonist. V116517 shows potent activity in inhibiting both capsaicin (CAP) - and acid (pH 5) -induced currents in rat DRG neurons expressing native TRPV (IC50=423.2 nM for CAP; IC50=180.3 nM for acid) . V116517 can be used for the research of pain[1].

• UNSPSC :

  12352005

• Target :

  TRP Channel

• Type :

  Reference compound

• Related Pathways :

  Membrane Transporter/Ion Channel; Neuronal Signaling

• Applications :

  COVID-19-immunoregulation

• Field of Research :

  Inflammation/Immunology; Neurological Disease

• Assay Protocol :

  https://www.medchemexpress.com/v116517.html

• Solubility :

  10 mM in DMSO

• Smiles :

  O=C(N1CC=C(C2=NC=C([C@H](O)CO)C=C2Cl)CC1)NC3=NC=C(C(F)(F)F)C=C3

• Molecular Formula :

  C19H18ClF3N4O3

• Molecular Weight :

  442.82

• References & Citations :

  [1]Laykea Tafesse, et al. Structure-activity relationship studies and discovery of a potent transient receptor potential vanilloid (TRPV1) antagonist 4-[3-chloro-5-[ (1S) -1,2-dihydroxyethyl]-2-pyridyl]-N-[5- (trifluoromethyl) -2-pyridyl]-3,6-dihydro-2H-pyridine-1-carboxamide (V116517) as a clinical candidate for pain management. J Med Chem. 2014 Aug 14;57 (15) :6781-94.

• Shipping Conditions :

  Room temperature

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 2

• Isoform :

  TRPV1

• CAS Number :

  [1073616-61-1]