Dirlotapide (Synonyms: CP742033; Slentrol)

Name: Dirlotapide
Brand: MedChemExpress
SKU: HY-U00070
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Cat. No.: HY-U00070 Pureza: 99.86%: Ficha de datos
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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.

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Dirlotapide Estructura química

No. CAS : 481658-94-0

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Descripciòn

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
Hepatocyte	IC₅₀	1.5 1 Compound: 3	Inhibition of MTP assessed as inhibition of apoB secretion from canine hepatocytes Inhibition of MTP assessed as inhibition of apoB secretion from canine hepatocytes	[PMID: 17276061]
HepG2	IC₅₀	11.3 4 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 1 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	2.7 1 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 1 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]
HepG2	IC₅₀	2.9 1 Compound: 3	Inhibition of MTP assessed as inhibition of apoB secretion from human HepG2 cells Inhibition of MTP assessed as inhibition of apoB secretion from human HepG2 cells	[PMID: 17276061]
HepG2	IC₅₀	4 1 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]
HepG2	IC₅₀	11.3 4 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	11.3 4 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 1 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	2.9 1 Compound: 3	Inhibition of MTP assessed as inhibition of apoB secretion from human HepG2 cells Inhibition of MTP assessed as inhibition of apoB secretion from human HepG2 cells	[PMID: 17276061]
HepG2	IC₅₀	4 1 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]
Hepatocyte	IC₅₀	1.5 1 Compound: 3	Inhibition of MTP assessed as inhibition of apoB secretion from canine hepatocytes Inhibition of MTP assessed as inhibition of apoB secretion from canine hepatocytes	[PMID: 17276061]

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.

Peso molecular

674.71

Fòrmula

C₄₀H₃₃F₃N₄O₃

No. CAS

481658-94-0

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

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Pureza y Documentación

Purity: 99.86%

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Ficha de datos (271 KB) SDS (252 KB)

COA (251 KB) HNMR (144 KB) CNMR (180 KB) LCMS (103 KB)

Instrucciones de manejo (2659 KB)

Referencias

[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. [Content Brief]

[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. [Content Brief]

Administraciòn de animales
^[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 no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.

Referencias

[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. [Content Brief]

[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. [Content Brief]

Dirlotapide Related Classifications

Metabolic Disease

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Dirlotapide481658-94-0CP742033 SlentrolCP 742033CP-742033Microsomal Triglyceride Transfer Protein (MTP)Inhibitorinhibitorinhibit

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Dirlotapide (Synonyms: CP742033; Slentrol)

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Dirlotapide Related Classifications

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