V116517,1073616-61-1

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V116517

CAS No. : 1073616-61-1

MCE 国际站：V116517

产品活性：V116517 是一种有效的口服活性瞬时受体电位香草醛 (TRPV1) 拮抗剂。V116517 在表达天然 TRPV 的大鼠 DRG 神经元中显示出抑制辣椒素 (CAP) 和酸 (pH 5) 诱导电流的有效活性 (对于CAP，IC₅₀=423.2 nM；对于acid，IC₅₀=180.3 nM)。V116517 可用于疼痛的研究。

研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶点：TRP Channel

In Vitro: 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.

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. 
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.

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