V116517_product_DataBase

Bioactivity	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].
Invitro	V116517 is highly selective for TRPV1 and did not show potency up to 10 μM in both TRPV3 and TRPV4 assays[1]. V116517 has fast-off kinetics for antagonism of both mode activations of TRPV1[1].
In Vivo	V116517 shows dose-dependent reversal of thermal hyperalgesia with an ED50 of 2 mg/kg (PO) in complete Freund’s adjuvant (CFA) inflammatory pain model[1]. V116517 exhibits high oral bioavailability (rat 74%, dog 100%, monkey 107%) and Cmax (rat 1380, dog 1120, monkey 459 ng/mL) following oral administration (rat 3, dog 3, monkey 3 mg/kg)[1].V116517 exhibits terminal elimination half-lives (rat 3.3, dog 3.6 and, monkey 18 h) due to high plasma clearance (0.24, 0.28, and 0.36 L/h/kg respectively) combined with large volumes of distribution (0.68, 1.2, and 6.0 L/kg respectively) following intravenous administration (rat 1, dog 1 and, monkey 1 mg/kg)[1].V116517 (rat 3 mg/kg; oral administration) is primarily restricted in periphery.The ratio of brain-to-plasma concentration is 0.09 at 3 h[1]. Animal Model:
Name	V116517
CAS	1073616-61-1
Formula	C19H18ClF3N4O3
Molar Mass	442.82
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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

PeptideDB

V116517

CAS: 1073616-61-1 F: C19H18ClF3N4O3 W: 442.82