THIQ
- CAS号:312637-48-2
- 英文名:THIQ
- 中文名:THIQ
- CBNumber:CB52459564
- 分子式:C33H41ClN6O2
- 分子量:589.17
- MOL File:312637-48-2.mol
- 密度 :1.33±0.1 g/cm3(Predicted)
- 储存条件 :Store at -20°C
- 溶解度 :DMSO : 250 mg/mL (424.33 mM; Need ultrasonic)
- 形态 :Powder
- 酸度系数(pKa) :13.82±0.20(Predicted)
- 颜色 :White to off-white
THIQ性质、用途与生产工艺
- 生物活性 THIQ 是 MC4R 的第一选择激动剂，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。
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体外研究
THIQ maintains low potency at human MC1R, MC3R and MC5R with IC 50 s of 2067, 761, 326 nM and EC 50 s of 2850, 2487, 737 nM, resepectively. THIQ maintains low potency at rat MC3R and MC5R with IC 50 s 1883 and 1575 nM, and EC 50 s 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. -
体内研究
THIQ (0.3-10 mg/kg; i.v.) dose-dependently increases erections (ED 50 =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.).
- 更新日期：2024/11/08
- 产品编号：HY-10624
- 产品名称：THIQ
- CAS编号：
- 包装：1 mg
- 价格：491元
- 更新日期：2024/11/08
- 产品编号：HY-10624
- 产品名称：THIQ THIQ
- CAS编号：312637-48-2
- 包装：5mg
- 价格：1000元
- 公司名称：TOCRIS-US
- 联系电话：--
- 电子邮件：customerservice@tocris.co.uk
- 国家：英国
- 产品数：5726
- 优势度：77
