T 3364366 是一种可逆的、缓慢结合的噻吩并嘧啶酮 delta-5 去饱和酶 (D5D) 抑制剂,在 HepG2 和 RLN-10 细胞中的 IC50 分别为 1.9 nM 和 2.1 nM。
Cas No. | 1356354-09-0 |
Canonical SMILES | CC(NCCSC1=NC2=CSC=C2C(N1C3=CC=C(C=C3)OCC(F)(F)F)=O)=O |
分子式 | C18H16F3N3O3S2 |
分子量 | 443.46 |
溶解度 | Soluble in DMSO |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | Potent and reversible fatty acid desaturase 1 (FADS1; Δ5 desaturase) inhibitor (IC50 values are 1.9 nM and 2.1 nM in human and rat hepatocyte cell lines, respectively). Exhibits >300 fold selectivity for FADS1 over FADS2 (Δ6 desaturase). Inhibits arachidonic acid production in rat and human hepatocyte cell lines. Orally bioavailable. Miyahisa et al (2016) T-3364366 targets the desaturase domain of delta-5 desaturase with nanomolar potency and a multihour residence time. ACS Med.Chem.Lett. 7 868 PMID:27660693 |