CP742033

Names

[ Name ]:
CP742033

[Synonym ]:
578H0RMP25
N-((1S)-2-(Benzylmethylamino)-2-oxo-1-phenylethyl)-1-methyl-5-(((4'-(trifluoromethyl)biphenyl-2-yl)carbonyl)amino)-1H-indole-2-carboxamide
N-{(1S)-2-[Benzyl(methyl)amino]-2-oxo-1-phenylethyl}-1-methyl-5-({[4'-(trifluoromethyl)-2-biphenylyl]carbonyl}amino)-1H-indole-2-carboxamide
N-{(1S)-2-[benzyl(methyl)amino]-2-oxo-1-phenylethyl}-1-methyl-5-({[4'-(trifluoromethyl)biphenyl-2-yl]carbonyl}amino)-1H-indole-2-carboxamide
1H-Indole-2-carboxamide, 1-methyl-N-((1S)-2-(methyl(phenylmethyl)amino)-2-oxo-1-phenylethyl)-5-(((4'-(trifluoromethyl)(1,1'-biphenyl)-2-yl)carbonyl)amino)-
Slentrol
1H-Indole-2-carboxamide, 1-methyl-N-[(1S)-2-[methyl(phenylmethyl)amino]-2-oxo-1-phenylethyl]-5-[[[4'-(trifluoromethyl)[1,1'-biphenyl]-2-yl]carbonyl]amino]-
Dirlotapide

Biological Activity

[Description]:

CP742033 is a gut-selective inhibitor of microsomal triglyceride transfer protein (MTP) that reliably produces weight loss in obese dogs.

[Related Catalog]:

Signaling Pathways >> Others >> Others

Research Areas >> Metabolic Disease

[In Vivo]

Dogs receiving 0.3 mg dirlotapide/kg once daily have a small but significant (P=0.018) decrease (6.16 ± 2.22%, mean ± SD) in crude fat digestibility compared with the placebo-treated food-restricted dogs, but no difference in crude protein, dry matter, or energy digestibility is observed. Dirlotapide effectively reduces appetite and energy intake without affecting nutrient digestibility, except for a minimal decrease in fat digestibility[1]. Dirlotapide (0.5 mg/kg) results in a high rate of weight loss (3.3% weekly) and anorexia, emesis, and loose stools for some dogs. Dirlotapide produces weight loss by both reducing appetite (about 90% of the weight loss activity) and by increasing fecal fat excretion (about 10% of the weight loss activity)[2].

[Animal admin]

Dirlotapide in the commercial formulation of a 5-mg/mL oil solution, is administered at an initial rate of 0.5 mg/kg adjusted individually based on the weight loss change in the previous 2 weeks. Dogs assigned to placebo receive the oil vehicle (identical in appearance to the dirlotapide solution) at a rate of 0.1 mL/kg and 0.075 mL/kg during the weight loss and weight management phases, respectively. The dose volume is administered directly into the dog's mouth with a dosing syringe approximately 30 min before feeding.

[References]

[1]. 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.

[2]. 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.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
821.2±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C₄₀H₃₃F₃N₄O₃

[ Molecular Weight ]:
674.710

[ Flash Point ]:
450.5±34.3 °C

[ Exact Mass ]:
674.250488

[ LogP ]:
6.95

[ Vapour Pressure ]:
0.0±3.0 mmHg at 25°C

[ Index of Refraction ]:
1.614

Related Compounds

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