V116517

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

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.

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.

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.

———

Others

Other Targets

———

———

———

1073616-61-1

442.82

C19H18ClF3N4O3

>98% (HPLC)

———

———

———

(-20℃)

With Ice Pack

≥ 2 years