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V116517

CAT: 0804-HY-12914Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-12914Size:1 Each
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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].
CAS Number
1073616-61-1
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

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