Teglicar

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Teglicar

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

250694-07-6

包装与价格：

包装	价格(元)
1mg	电议
5mg	电议
10mg	电议
50mg	电议
100mg	电议

产品名称

替格列卡

产品介绍

Teglicar 是一种选择性、可逆性的肉碱棕榈酰转移酶1(L-CPT1)肝脏亚型抑制剂，具有口服活性，其IC₅₀值为 0.68 μM,K_i值为 0.36 μM。Teglicar 具有潜在的抗高血糖特性。Teglicar 可用于糖尿病和神经退行性疾病的研究，包括亨廷顿病(HD)。

生物活性

Teglicar is a selective and reversible orally active liver isoform ofcarnitine palmitoyl-transferase 1 (L-CPT1)inhibitor with anIC₅₀value of 0.68 μM and aK_ivalue of 0.36 μM. Teglicar has a potential antihyperglycemic propert. Teglicar can be used for the research of diabetes and neurodegenerative disease including Huntington's disease (HD)^[1]^[2].

IC₅₀& Target

IC50: 0.68 μM (L-CPT1); Ki: 0.36 μM (L-CPT1)^[1]

体外研究
(In Vitro)

Teglicar has L-CPT1 inhibitory activity with anIC₅₀value of 0.68 μM and aK_ivalue of 0.36 μM^[1].
Teglicar (10 μM; 2 h) induces a concentration-dependent reduction of ketone bodies and glucose production^[1].

体内研究
(In Vivo)

Teglicar (oral, 80 mg/kg, once a day, for 30 days or infusion, 5.3 mg/kg/h, for 3 h) reduces the endogenous glucose production (262%) without affecting peripheral glucose utilization in SD rats^[1].
Teglicar (gavage, 50 mg/kg, single or long-term 100 mg/kg/day for 30 days) not affects heart 2-[³H]deoxyglucose uptake in C57BL6/J mice^[1].
Teglicar (gavage, 50 mg/kg, twice a day, for 45 days) reduces postabsorptive glycemia (238%), water consumption (231%), and fructosamine (230%) in db/db mice^[1].
Teglicar (30 mg/kg, twice a day, for 26 days) normalized glycemia (219%) and insulinemia (253%) and increases HTGC but not affects liver and peripheral insulin sensitivity in high-fat diet C57BL/6J mice^[1].
Teglicar (oral, 50 μM, was added to the surface of fly food, 1, 8, 12, and 15 days) ameliorates the neurodegenerative phenotype in a drosophila Huntington's Disease Model by acting on the expression of carnitine-related genes^[2].

Animal Model:	SD rats^[1]
Dosage:	80 mg/kg, 5.3 mg/kg
Administration:	oral, 80 mg/kg, once a day, for 30 days or infusion, 5.3 mg/kg/h, for 3 h
Result:	Reduced basal insulin levels, showed a higher triglyceride and low glycogen content in the liver, without any change in liver weight. Showed a rapid drop in glycemia, suppressed EGP (EGP2) diminished by 62% and not affected peripheral glucose utilization (GU).

Animal Model:	C57BL6/J mice^[1]
Dosage:	50 mg/kg, 100 mg/kg
Administration:	gavage, 50 mg/kg, single or long-term 100 mg/kg/day for 30 days.
Result:	Did not modify etomoxir-induced M-CPT1 inhibition and failed to determine significant changes in 2-DG heart uptake, heart weights, and triglyceride content.

Animal Model:	db/db mice^[1]
Dosage:	50 mg/kg
Administration:	gavage, 50 mg/kg, twice a day, for 45 days
Result:	Induced a significant reduction of postabsorptive serum glucose, reduced serum fructosamine and average daily water consumption, increased Serum FFAs, but did not change insulin levels, triglycerides, alanine aminotransferase, also induced a significant reduction of glucose AUC during ITT. Did not induce any variation in the content of PPAR-α and its target gene product MCAD and peroxisomal b-oxidation in liver and heart of db/db mice.

Animal Model:	High-fat diet C57BL/6J mice^[1]
Dosage:	30 mg/kg
Administration:	30 mg/kg, twice a day, for 26 days
Result:	Did not affect food intake, did not change body weight and serum FFAs and triglycerides and did not affect glucose intolerant.

分子量

399.61

性状

Solid

Formula

C₂₂H₄₅N₃O₃

CAS 号

250694-07-6

中文名称

替格列卡

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

溶解性数据

In Vitro:

DMSO : 19 mg/mL(47.55 mM;Need ultrasonic)

H₂O : 10 mg/mL(25.02 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.5024 mL	12.5122 mL	25.0244 mL
5 mM	0.5005 mL	2.5024 mL	5.0049 mL
10 mM	0.2502 mL	1.2512 mL	2.5024 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.
请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline
Solubility: ≥ 3.33 mg/mL (8.33 mM); Clear solution
此方案可获得 ≥ 3.33 mg/mL (8.33 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 33.3 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
2.
请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline)
Solubility: ≥ 1.9 mg/mL (4.75 mM); Clear solution
此方案可获得 ≥ 1.9 mg/mL (4.75 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 19.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

*以上所有助溶剂都可在本网站选购。