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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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D651112-1mg | 1mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $1,615.90 |
Synonyms | Dirlotapide [USAN:INN] | Slentrol [veterinary] (TN) | Q5280905 | BDBM50204367 | D03867 | DB11399 | dirlotapida | dirlotapidum | 5-((4'-trifluoromethyl-biphenyl-2-carbonyl)-amino)-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide | 6-carboxy-5'-uridy |
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Specifications & Purity | ≥99% |
Biochemical and Physiological Mechanisms | Dirlotapide (CP742033) is a gut-selective inhibitor of microsomal triglyceride transfer protein (MTP) that reliably produces weight loss in obese dogs. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Product Description | Dirlotapide (CP742033) is a gut-selective inhibitor of microsomal triglyceride transfer protein (MTP) that reliably produces weight loss in obese dogs. 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 . 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). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal administration 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. aladdin has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid |
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IUPAC Name | N-[(1S)-2-[benzyl(methyl)amino]-2-oxo-1-phenylethyl]-1-methyl-5-[[2-[4-(trifluoromethyl)phenyl]benzoyl]amino]indole-2-carboxamide |
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INCHI | InChI=1S/C40H33F3N4O3/c1-46(25-26-11-5-3-6-12-26)39(50)36(28-13-7-4-8-14-28)45-38(49)35-24-29-23-31(21-22-34(29)47(35)2)44-37(48)33-16-10-9-15-32(33)27-17-19-30(20-18-27)40(41,42)43/h3-24,36H,25H2,1-2H3,(H,44,48)(H,45,49)/t36-/m0/s1 |
InChi Key | TUOSYWCFRFNJBS-BHVANESWSA-N |
Canonical SMILES | CN1C2=C(C=C(C=C2)NC(=O)C3=CC=CC=C3C4=CC=C(C=C4)C(F)(F)F)C=C1C(=O)NC(C5=CC=CC=C5)C(=O)N(C)CC6=CC=CC=C6 |
Isomeric SMILES | CN1C2=C(C=C(C=C2)NC(=O)C3=CC=CC=C3C4=CC=C(C=C4)C(F)(F)F)C=C1C(=O)N[C@@H](C5=CC=CC=C5)C(=O)N(C)CC6=CC=CC=C6 |
Alternate CAS | 481658-94-0 |
PubChem CID | 9917862 |
MeSH Entry Terms | 5-((4'-trifluoromethyl-biphenyl-2-carbonyl)-amino)-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide;dirlotapide |
Molecular Weight | 674.71 |
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