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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。
Teglicar图片
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,Ki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 aKivalue 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 aKivalue 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°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 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 mg5 mg10 mg
1 mM2.5024 mL12.5122 mL25.0244 mL
5 mM0.5005 mL2.5024 mL5.0049 mL
10 mM0.2502 mL1.2512 mL2.5024 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。