Dirlotapide - CAS 481658-94-0
Catalog number: 481658-94-0
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C40H33F3N4O3
Molecular Weight:
674.71
COA:
Inquire
Targets:
Others
Description:
Dirlotapide is a drug used to treat obesity in dogs works as a gut-selective microsomal triglyceride transfer protein (MTTP or MTP) inhibitor.
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Purity:
≥95%
Appearance:
Solid powder
Synonyms:
Slentrol; 5-((4'-Trifluoromethyl-biphenyl-2-carbonyl)amino)-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide;
Solubility:
Soluble in DMSO
Storage:
Store at -20 °C
MSDS:
Inquire
Application:
MTTP Inhibitor
Quality Standard:
Enterprise standard
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly.
Quantity:
Milligrams-Grams
InChIKey:
TUOSYWCFRFNJBS-BHVANESWSA-N
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
Canonical SMILES:
CN(Cc1ccccc1)C(=O)[C@@H](NC(=O)c2cc3cc(NC(=O)c4ccccc4c5ccc(cc5)C(F)(F)F)ccc3n2C)c6ccccc6
1.An evaluation of dirlotapide to reduce body weight of client-owned dogs in two placebo-controlled clinical studies in Europe.
Gossellin J1, McKelvie J, Sherington J, Wren JA, Eagleson JS, Rowan TG, Sunderland SJ. J Vet Pharmacol Ther. 2007 Aug;30 Suppl 1:73-80.
The clinical efficacy for weight loss and safety of dirlotapide in dogs were evaluated in two multi-centre studies with parallel designs. Overweight, adult dogs (n = 245) of various breeds were randomized to treatment with dirlotapide or placebo in a 2:1 ratio. Dirlotapide was administered orally once daily to dogs at an initial dose of 0.05 mg/kg/day commencing on day 0 and doubled after 14 days. Every 28 days, dogs were examined, weighed, body condition scores (BCS) were recorded, and dose was adjusted to meet weight loss targets. Each study comprised three consecutive phases: weight-loss (up to day 196); weight-stabilization (84 days); and post-treatment (28 days). pre-treatment feeding and exercise regimens were continued during treatment. Dirlotapide-treated dogs showed mean weight loss of 15.9% (study A) and 14.0% (study B) by the end of weight loss phase (up to day 196). Percentage weekly weight losses for dirlotapide were significantly greater than for placebo (P < or = 0.
2.Influence of dirlotapide, a microsomal triglyceride transfer protein inhibitor, on the digestibility of a dry expanded diet in adult dogs.
Kirk CA1, Boucher JF, Sunderland SJ, Wren JA. J Vet Pharmacol Ther. 2007 Aug;30 Suppl 1:66-72.
The objectives of this study were to evaluate the effects of dirlotapide, a microsomal triglyceride transfer protein inhibitor, on apparent nutrient digestibility of an expanded dry dog food, on defecation frequency and fecal consistency. Eighteen beagles were randomized to either placebo (n = 6) or dirlotapide (n = 12). Testing was divided into a 21-day adaptation phase (days -21 to -1) and a 35-day treatment (digestibility testing) phase (days 0-35). During the treatment phase, dogs were administered oral dirlotapide (0.3 mg/kg) or placebo (0.06 mL/kg) once daily. For digestibility testing, feces were collected over two periods for 7 days each starting on days -9 and 28. All dogs were fed a commercial adult dog food throughout the study. Food intake was adjusted to maintain body weight during adaptation, followed by pair-feeding placebo dogs the amount of food ingested by the dirlotapide dogs during the treatment period. Dogs in both groups had reduced food intake and lost similar amounts of body weight during treatment.
3.Evaluation of dirlotapide for sustained weight loss in overweight Labrador retrievers.
Gossellin J1, Peachey S, Sherington J, Rowan TG, Sunderland SJ. J Vet Pharmacol Ther. 2007 Aug;30 Suppl 1:55-65.
The effects of dirlotapide on body weight (BW) reduction were investigated in overweight Labradors in two parallel-design studies. Study A involved 42 dogs randomized to 0.0, 0.025, 0.05, 0.1, 0.2 or 0.4 mg dirlotapide/kg/day orally for 4 weeks. Study B involved 72 dogs randomized to nine treatments: placebo (24 weeks); dirlotapide (24 weeks) followed by placebo (28 weeks); or dirlotapide (52 weeks); on diets containing 5%, 10% or 15% fat. Dirlotapide dose (initially 0.1 mg/kg) was adjusted monthly during 24-week weight-loss and subsequent 28-week weight-stabilization phases. Food was offered above maintenance energy requirements (MERx 1.1-1.2) based on initial BW. Body composition (body fat, lean tissue and bone mineral content) was monitored using dual-energy X-ray absorptiometry. After treatment, dogs that had received dirlotapide for 52 weeks were fed 90% of quantity consumed at week 52. In study A, BW and food intake decreased asymptotically with dose: mean weekly weight loss exceeded 1% at 0.
4.Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide.
Robinson RP1, Bartlett JA, Bertinato P, Bessire AJ, Cosgrove J, Foley PM, Manion TB, Minich ML, Ramos B, Reese MR, Schmahai TJ, Swick AG, Tess DA, Vaz A, Wolford A. Bioorg Med Chem Lett. 2011 Jul 15;21(14):4150-4. doi: 10.1016/j.bmcl.2011.05.099. Epub 2011 Jun 2.
Analogues related to dirlotapide (1), a gut-selective inhibitor of microsomal triglyceride transfer protein (MTP) were prepared with the goal of further reducing the potential for unwanted liver MTP inhibition and associated side-effects. Compounds were designed to decrease active metabolite load: reducing MTP activity of likely human metabolites and increasing metabolite clearance to reduce exposure. Introduction of 4'-alkyl and 4'-alkoxy substituents afforded compounds exhibiting improved therapeutic index in rats with respect to liver triglyceride accumulation and enzyme elevation. Likely human metabolites of select compounds were prepared and characterized for their potential to inhibit MTP in vivo. Based on preclinical efficacy and safety data and its potential for producing short-lived, weakly active metabolites, compound 13 (PF-02575799) advanced into phase 1 clinical studies.
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