Teglicar 替格列卡|cas:250694-07-6|西域试剂

Teglicar 替格列卡,98.0%

产品编号：Bellancom-16482| CAS NO：250694-07-6| 分子式：C₂₂H₄₅N₃O₃| 分子量：399.61

Teglicar 是选择性和可逆性的肉毒碱棕榈酰转移酶 1 (L-CPT1) 肝异构体抑制剂，可减少酮生成和葡萄糖生成，降低糖异生，改善葡萄糖稳态。Teglicar 具有潜在的抗高血糖特性。

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-16482	￥5500.00	杭州北京（现货）
Bellancom-16482	￥9800.00	杭州北京（现货）
Bellancom-16482	￥15000.00	杭州北京（现货）

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Teglicar 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 of carnitine palmitoyl-transferase 1 (L-CPT1) inhibitor with an IC₅₀ value of 0.68 μM and a K_i value 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).

体外研究

Teglicar has L-CPT1 inhibitory activity with an IC₅₀ value of 0.68 μM and a K_i value of 0.36 μM.
Teglicar (10 μM; 2 h) induces a concentration-dependent reduction of ketone bodies and glucose production.

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

体内研究

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.
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.
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.
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.
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.

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

Animal Model:	SD rats
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
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
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
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.

体内研究

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

Animal Model:	SD rats
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
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
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
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.

性状

Solid

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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-CD in 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 μL 20% 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西域网站选购。

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

参考文献

. Roberto Conti, et al. Selective reversible inhibition of liver carnitine palmitoyl-transferase 1 by teglicar reduces gluconeogenesis and improves glucose homeostasis. Diabetes. 2011 Feb;60(2):644-51. [Content Brief]

. Carla Bertapelle, et al. The Reversible Carnitine Palmitoyltransferase 1 Inhibitor (Teglicar) Ameliorates the Neurodegenerative Phenotype in a Drosophila Huntington's Disease Model by Acting on the Expression of Carnitine-Related Genes. Molecules [Content Brief]

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Teglicar 替格列卡,98.0%

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