化合物SB-649868 T5498

Product Introduction
Bioactivity


英文名: SB-649868

描述: SB-649868 (GSK649868) 是一种有效的选择性口服活性食欲素拮抗剂，对 OX1 和 OX2 受体的 pKi 分别为 9.4 和 9.5。

体外活性: SB-649868 antagonizes orexin-A-induced inositol 1 phosphate (IP1) accumulation with the following pKB value (OX1=9.67;?OX2=9.64).?SB-649868 displaces the [3H]ACT-078573 receptor binding with the following pKi values: OX1=9.27;?OX2=8.91.?Increasing concentrations of SB-649868 (0.3 nM-30 nM) induces a rightward shift of the orexin-A CRCs with a depression of the agonist efficacy suggesting a clear non-surmountable behavior.?The calculated apparent pKb values are 9.67 0.03 and 9.64 0.07 for OX1 and OX2

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 100 mg/mL (209.40 mM)


关键字: Inhibitor | HCRT Receptor | Orexin Receptor (OX Receptor) | Hypocretin Receptor | inhibit | GSK 649868 | SB-649868 | SB649868 | SB 649868 | GSK-649868

相关产品: Seltorexant | TCS 1102 | PF3274167 | Orexin B, rat, mouse Acetate | TCS-OX2-29 | Almorexant | MK-1064 | IPSU | OXA (17-33) acetate | SB-408124

相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | ReFRAME Related Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | GPCR Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途