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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.86%
- CAS 番号: 481658-94-0
- 分子式: C40H33F3N4O3
- 分子量:674.71
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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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
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[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
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[PMID: 21684740] |
| HepG2 | IC50 |
2.9 nM
Compound: 3
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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
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[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
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[PMID: 19181526] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 481658-94-0
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性状 Solid
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分子量 674.71
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分子式 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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別名
CP742033; Slentrol
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
プロトコル
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.
純度とドキュメンテーション
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データシート (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)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Dirlotapide 関連分類
HY-U00070 関連分類
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