1. Metabolic Enzyme/Protease
  2. Microsomal Triglyceride Transfer Protein (MTP)
  3. Dirlotapide

Dirlotapide  (Synonyms: CP742033; Slentrol)

Cat. No.: HY-U00070 Purity: ≥99.0%
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Dirlotapide (CP742033) is a gut-selective inhibitor of microsomal triglyceride transfer protein (MTP) that reliably produces weight loss in obese dogs.

For research use only. We do not sell to patients.

Dirlotapide Chemical Structure

Dirlotapide Chemical Structure

CAS No. : 481658-94-0

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Based on 1 publication(s) in Google Scholar

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Description

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

Cellular Effect
Cell Line Type Value Description References
HepG2 IC50
11.3 pM
Compound: 1
Inhibition of MTP in human HepG2 cells assessed as unbound drug level causing inhibition of apoB secretion after 40 hrs by ELISA
Inhibition of MTP in human HepG2 cells assessed as unbound drug level causing inhibition of apoB secretion after 40 hrs by ELISA
[PMID: 21684740]
HepG2 IC50
2.7 nM
Compound: 1
Inhibition of MTP in human HepG2 cells assessed as inhibition of apoB secretion after 40 hrs by ELISA
Inhibition of MTP in human HepG2 cells assessed as inhibition of apoB secretion after 40 hrs by ELISA
[PMID: 21684740]
HepG2 IC50
4 nM
Compound: dirlotapide
Inhibition of apoB secretion in human HepG2 cells after 40 hrs by ELISA
Inhibition of apoB secretion in human HepG2 cells after 40 hrs by ELISA
[PMID: 19181526]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

674.71

Formula

C40H33F3N4O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C(N1C)=CC2=C1C=CC(NC(C3=CC=CC=C3C4=CC=C(C(F)(F)F)C=C4)=O)=C2)N[C@@H](C5=CC=CC=C5)C(N(C)CC6=CC=CC=C6)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
Animal Administration
[2]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Dirlotapide
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HY-U00070
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