THIQ is the first selective agonist of themelanocortin-4 receptor (MC4R), with high affinity and potency for hMC4R (IC₅₀=1.2 nM,EC₅₀=2.1 nM) and rMC4R (IC₅₀=0.6 nM,EC₅₀=2.9 nM). THIQ maintains low potency atMC1R,MC3RandMC5R. THIQ plays a role in eliciting erectile activity in rodents. THIQ acts as a pharmacoperone of theMC4Rrescuing the cell surface expression and signaling of some intracellularly retainedMC4Rmutants^[1][2].

THIQ maintains low potency athumanMC1R, MC3R and MC5R with IC₅₀s of 2067, 761, 326 nM and EC₅₀s of 2850, 2487, 737 nM, resepectively. THIQ maintains low potency atratMC3R and MC5R with IC₅₀s 1883 and 1575 nM, and EC₅₀s of 1325 and >3000 nM, respectively^[1].
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^[2].

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%^[1].
THIQ treatment shows the t_1/2is 0.6 hours in Sprague-Dawley rats (1 mg/kg, i.v. and 10 mg/kg, p.o.)^[1].

589.17

Solid

C₃₃H₄₁ClN₆O₂

312637-48-2

Room temperature in continental US; may vary elsewhere.

DMSO : 250 mg/mL(424.33 mM;Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 2.08 mg/mL (3.53 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (3.53 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 2.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.08 mg/mL (3.53 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (3.53 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。