Dirlotapide (Synonyms: CP742033; Slentrol)

目錄號: HY-U00070 純度: ≥99.0%: FAQs
Data Sheet SDS COA 產(chǎn)品使用指南

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Dirlotapide (CP742033) 是一種選擇性的微粒體甘油三酯轉(zhuǎn)運蛋白 (MTP) 抑制劑，可以減輕糖尿病狗的體重。

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Dirlotapide Chemical Structure

CAS No. : 481658-94-0

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Dirlotapide 相關產(chǎn)品

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生物活性
實驗參考方法
純度 & 產(chǎn)品資料
參考文獻

生物活性

Dirlotapide (CP742033) is a gut-selective inhibitor of microsomal triglyceride transfer protein (MTP) that reliably produces weight loss in obese dogs.

細胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
HepG2	IC₅₀	11.3 pM 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 nM 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 nM 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]

體內(nèi)研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

674.71

Formula

C₄₀H₃₃F₃N₄O₃

CAS 號

481658-94-0

性狀

固體

顏色

White to off-white

中文名稱

地洛他派

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

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

純度 & 產(chǎn)品資料

純度: ≥99.0%

選擇批次：

Data Sheet (529 KB) SDS (251 KB)

COA (267 KB) HNMR (178 KB) LCMS (75 KB)

產(chǎn)品使用指南 (1538 KB)

參考文獻

[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]

Animal Administration ^[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 has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻	[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]

Animal Administration
^[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 has not independently confirmed the accuracy of these methods. They are for reference only.

參考文獻

[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 相關分類

Metabolic Disease

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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 Slentrol地洛他派CP 742033CP-742033Microsomal Triglyceride Transfer Protein (MTP)Inhibitorinhibitorinhibit

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Dirlotapide (Synonyms: CP742033; Slentrol)

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Dirlotapide (Synonyms: CP742033; Slentrol)

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Dirlotapide 相關產(chǎn)品

•同靶點產(chǎn)品:

•同靶點蛋白產(chǎn)品:

生物活性

實驗參考方法

純度 & 產(chǎn)品資料

參考文獻

Dirlotapide 相關分類

摩爾計算器

稀釋計算器

The molarity calculator equation

The dilution calculator equation

Keywords:

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