| Description | Dirlotapide (CP742033) is an intestinal selective microsomal triglyceride transfer protein (MTP) inhibitor. It reduces body weight in diabetic dogs.Dirlotapide reduces food intake in a dose-dependent manner, possibly by increasing the release of peptide YY into the circulation. |
| In vivo | Dirlotapide（0.5 mg/kg；口服；犬）导致高比例体重减轻（每周3.3%）以及部分犬只出现厌食、呕吐和稀便。Dirlotapide通过减少食欲（约占体重减轻活性的90%）和增加粪便脂肪排泄（约占体重减轻活性的10%）来产生减重效果。[1] Dirlotapide（0.3 mg/kg；口服；每日一次；犬）与安慰剂处理的食物限制犬相比，粗脂肪消化率有小幅但显著下降（平均降低6.16 ± 2.22%，均值 ± 标准差）(P=0.018)，但粗蛋白、干物质或能量消化率无差异。Dirlotapide有效减少食欲和能量摄入，不影响除脂肪消化率外的营养物质消化率。[2] |
| Synonyms | CP742033, Slentrol |
| molecular weight | 674.71 |
| Molecular formula | C40H33F3N4O3 |
| CAS | 481658-94-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 67.47 mg/mL (100 mM), Sonication is recommended. H2O: <1 mg/mL (Insoluble) |
| References | 1. Wren JA, et al. Biologic activity of dirlotapide, a novel microsomal triglyceride transfer protein inhibitor, for weight loss in obese dogs. J Vet Pharmacol Ther. 2007 Aug;30 Suppl 1:33-42. 2. Kirk CA, et al. Influence of dirlotapide, a microsomal triglyceride transfer protein inhibitor, on the digestibility of a dry expanded diet in adult dogs. J Vet Pharmacol Ther. 2007 Aug;30 Suppl 1:66-72. |