MTP-IN-1是微粒体甘油三酯转移蛋白(microsomaltriglyceridetransferprotein(MTP))抑制剂，IC50值为0.77±0.29nM。
PF-02575799 is a microsomal triglyceride transfer protein (MTP) inhibitor with an IC50 of 0.77±0.29 nM.
PF-02575799 is compound 13 from the reference[1].
PF-02575799 produces appreciable triglyceride effects at its minimally effective dose (10 mg/kg). PF-02575799 significant increase alanine transaminase at 100 mg/kg[1].
[1]. Robinson RP, et al. Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide. Bioorg Med Chem Lett. 2011 Jul 15;21(14):4150-4.
Animal experiment: | Rats[1]Spray-dried dispersions formulated PF-02575799 is tested in a seven-day rat model. Food intake, body weight, liver TG, as well as serum alanine transaminase (ALT) are measured. In the definitive study, dose effect relationships are examined (PF-02575799 1, 3, 10, 30 and 100 mg/kg q.d.) and systemic exposures are measured[1]. |
参考文献: [1]. Robinson RP, et al. Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide. Bioorg Med Chem Lett. 2011 Jul 15;21(14):4150-4. | |
动态评分
0.0