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THIQ

CAS No. : 312637-48-2

MCE 站：THIQ

产品活性：THIQ 是 MC4R 的选择激动剂，对 hMC4R (IC₅₀=1.2 nM; EC₅₀=2.1 nM) 和 rMC4R(IC₅₀=0.6 nM; EC₅₀=2.9 nM) 具有较高的亲和力和效价。THIQ 对 MC1R、MC3R 和 MC5R 有较低效价，在引起啮齿动物勃起活动中起作用。THIQ 作为 MC4R 的一种药物过氧化物酶体，挽救了一些细胞内保留的 MC4R 突变体的细胞表面表达和信号传导。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Melanocortin Receptor

In Vitro: THIQ maintains low potency at human MC1R, MC3R and MC5R with IC₅₀s of 2067, 761, 326 nM and EC₅₀s of 2850, 2487, 737 nM, resepectively. THIQ maintains low potency at rat MC3R and MC5R with IC₅₀s 1883 and 1575 nM, and EC₅₀s of 1325 and >3000 nM, respectively.
THIQ (10 μM; 24 hours) decreases the signal intensity of WT MC4R by approximately 50% whereas increases that of three mutants (N62S, C84R, and C271Y) in HEK293 cells.

In Vivo: THIQ (0.3-10 mg/kg; i.v.) dose-dependently increases erections (ED₅₀=0.87 mg/kg) in sexually mature male Sprague Dawley rats. The maximal increase in the number of erections (60%) is detected at 5 mg/kg but was not significantly different from that produced by 1 mg/kg. THIQ (20 mg/kg; p.o.) also produces statistically significant increases in erectile responses with a mean increase of 31±4%.
THIQ treatment shows the t_1/2 is 0.6 hours in Sprague-Dawley rats (1 mg/kg, i.v. and 10 mg/kg, p.o.).

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