1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. TRP Channel
  3. V116517

V116517 

Cat. No.: HY-12914
Handling Instructions

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.

For research use only. We do not sell to patients.

V116517 Chemical Structure

V116517 Chemical Structure

CAS No. : 1073616-61-1

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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].

IC50 & Target[1]

TRPV1

 

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

442.82

Formula

C₁₉H₁₈ClF₃N₄O₃

CAS No.
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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V116517
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HY-12914
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