V116517

Research use only, not for human use.

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.

V-116517, a TRPV1 antagonist, is used potentially for the treatment of severe pain due to osteoarthritis and chronic pain due postherpetic neuralgia (PHN).

V116517?is highly selective for TRPV1 and did not show potency up to 10 μM in both TRPV3 and TRPV4 assays. V116517?has fast-off kinetics for antagonism of both mode activations of TRPV1.

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.?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).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).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.Animal Model:Male Sprague-Dawley rats (6 weeks, 180-280 g) bearing acute inflammatory CFA model Dosage:0.3, 1, 3, 10, 30 mg/kg Administration:Oral administration Result:Dose-dependently reversed inflammatory thermal hyperalgesia.

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Others

Other Targets

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1073616-61-1

442.82

C19H18ClF3N4O3

>98% (HPLC)

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(-20℃)

With Ice Pack

≥ 2 years