THIQ 产品活性：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 的一种活性分子过氧化物酶体，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。 产品来源： https://www.medchemexpress.cn/thiq.html 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 t1/2 is 0.6 hours in Sprague-Dawley rats (1 mg/kg, i.v. and 10 mg/kg, p.o.). 相关产品：Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Neuronal Signaling Compound Library | Anti-Obesity Compound Library | Targeted Diversity Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Activators Library | Bioactive Compound Library Max | α-MSH | Melanotan I | SHU 9119 | BMS-470539 dihydrochloride | Bremelanotide Acetate | Nonapeptide-1 acetate salt | JNJ-10229570 | Adrenocorticotropic Hormone (ACTH) (1-39), rat TFA | HS024 TFA | β-Melanocyte Stimulating Hormone (MSH), human TFA | Dersimelagon | MK-0493 | PF-00446687 | SNT-207707 | ACTH (1-17) (TFA) | Adrenocorticotropic Hormone (ACTH) (1-39), human(TFA) | MSG606 | SNT-207858 free base | [D-Trp8]-γ-MSH | Adrenocorticotropic Hormone (ACTH) (4-10), human | Agouti-related Protein (AGRP) (83-132) Amide (human) (TFA) | Fenoprofen | PF-07258669 | ACTH (11-24) | HS014 TFA | ML-00253764 hydrochloride | PG-931 | RO27-3225 TFA 品牌介绍: MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供最新最全的高品质小分子活性化合物；10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；设有专业的实验中心和严格的质控、验证体系；提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；产品的生物活性多经各国客户实验验证；Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果；专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；与世界各大制药公司及知名科研机构建立了长期的合作。