2. Metabolic Enzyme/Protease
  3. Endogenous Metabolite
  4. Teglicar

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 Ki 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).

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Teglicar Chemical Structure

Teglicar Chemical Structure

CAS No. : 250694-07-6

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Based on 1 publication(s) in Google Scholar

Teglicar Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

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 Ki 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)[1][2].

IC50 & Target

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

Teglicar has L-CPT1 inhibitory activity with an IC50 value of 0.68 μM and a Ki value of 0.36 μM[1].
Teglicar (10 μM; 2 h) induces a concentration-dependent reduction of ketone bodies and glucose production[1].

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

Teglicar Related Antibodies
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].

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

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.
Molecular Weight

399.61

Formula

C22H45N3O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N[C@H](CC([O-])=O)C[N+](C)(C)C)NCCCCCCCCCCCCCC
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

Ethanol : 100 mg/mL (250.24 mM; ultrasonic and heat to 60°C)

DMSO : 19 mg/mL (47.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 3.33 mg/mL (8.33 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.33 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (33.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.9 mg/mL (4.75 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.9 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (19.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: ≥98.0%

COA (241 KB) HNMR (283 KB) MS (68 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO / Ethanol 1 mM 2.5024 mL 12.5122 mL 25.0244 mL 62.5610 mL
5 mM 0.5005 mL 2.5024 mL 5.0049 mL 12.5122 mL
10 mM 0.2502 mL 1.2512 mL 2.5024 mL 6.2561 mL
15 mM 0.1668 mL 0.8341 mL 1.6683 mL 4.1707 mL
20 mM 0.1251 mL 0.6256 mL 1.2512 mL 3.1280 mL
25 mM 0.1001 mL 0.5005 mL 1.0010 mL 2.5024 mL
DMSO / Ethanol 30 mM 0.0834 mL 0.4171 mL 0.8341 mL 2.0854 mL
40 mM 0.0626 mL 0.3128 mL 0.6256 mL 1.5640 mL
Ethanol 50 mM 0.0500 mL 0.2502 mL 0.5005 mL 1.2512 mL
60 mM 0.0417 mL 0.2085 mL 0.4171 mL 1.0427 mL
80 mM 0.0313 mL 0.1564 mL 0.3128 mL 0.7820 mL
100 mM 0.0250 mL 0.1251 mL 0.2502 mL 0.6256 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Teglicar Related Classifications

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:

Teglicar250694-07-6Endogenous Metaboliteaminocarnitine derivativecarnitine palmitoyl-transferase 1 (L-CPT1)diabetesneurodegenerative diseaseHuntington's disease (HD)Inhibitorinhibitorinhibit

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