Dirlotapide
Based on 1 Customer Validation
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.
- Purity: 99.86%
- CAS No.: 481658-94-0
- Formula: C40H33F3N4O3
- Molecular Weight:674.71
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
- Protocol
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Hepatocyte | IC50 |
1.5 nM
Compound: 3
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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 pM
Compound: 1
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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
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[PMID: 21684740] |
| HepG2 | IC50 |
2.7 nM
Compound: 1
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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 nM
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 nM
Compound: dirlotapide
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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] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 481658-94-0
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Appearance Solid
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Molecular Weight 674.71
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Formula C40H33F3N4O3
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Color White to off-white
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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
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Synonyms
CP742033; Slentrol
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Protocol
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (271 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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. [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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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