1. Membrane Transporter/Ion Channel
  2. Na+/K+ ATPase
  3. Tolbutamide

Tolbutamide is an orally active KATP inhibitor. Tolbutamide inhibits cell proliferation, stimulates exocytosis of glucagon and reduces fetal lethality of mice. Tolbutamide can be used in the research of diabete.

For research use only. We do not sell to patients.

Tolbutamide Chemical Structure

Tolbutamide Chemical Structure

CAS No. : 64-77-7

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10 mM * 1 mL in DMSO
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Tolbutamide:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Tolbutamide is an orally active KATP inhibitor. Tolbutamide inhibits cell proliferation, stimulates exocytosis of glucagon and reduces fetal lethality of mice. Tolbutamide can be used in the research of diabete[1][2][3][4].

In Vitro

Tolbutamide (400 μM, 24h) with dbcAMP reduces glioma cell proliferation by increasing connexin43 (Cx43)[1].
Tolbutamide (0.1 μM, 1 min) stimulates exocytosis by activation of a mitochondrial­like KATP channel in rat A-cells[2].

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

Western Blot Analysis[1]

Cell Line: Glioma cell
Concentration: 400 μM
Incubation Time: 24h
Result: Increasing the level of Cx43.
In Vivo

Tolbutamide (125 mg/kg, Supplemented in daily diet for 27 weeks) reduces the incidence of diabetes mellitus in the non-obese-diabetic mouse[3].
Tolbutamide (100-400 mg/kg, Intraperitoneal injection, 400 mg/kg on day 13; 100 mg/kg on day 10-13; combined treatment: 100 mg/kg on day 10-12 and 400 mg/kg on day 13) reduces fetal lethality in pregnant mice[4].

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

Animal Model: Non-obese-diabetic mouse [3]
Dosage: 125 mg/kg
Administration: Supplemented in daily diet for 27 weeks
Result: Showed 10 of 23 animals developed diabetes compared with 18 of 24 in the control groups.
Animal Model: Pregnant mice [4]
Dosage: 100 mg/kg, 400 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Showed a significant reduction (50 %) in the frequency of living fetuses for the group of 400 mg/kg on day 13.
Had significantly fewer petechiae and more late resorptions for the group of 400 mg/kg on day 13.
Clinical Trial
Molecular Weight

270.35

Formula

C12H18N2O3S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=CC=C(C)C=C1)(NC(NCCCC)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 34 mg/mL (125.76 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.6989 mL 18.4945 mL 36.9891 mL
5 mM 0.7398 mL 3.6989 mL 7.3978 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
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: ≥ 2.08 mg/mL (7.69 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (7.69 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 99.96%

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.6989 mL 18.4945 mL 36.9891 mL 92.4727 mL
5 mM 0.7398 mL 3.6989 mL 7.3978 mL 18.4945 mL
10 mM 0.3699 mL 1.8495 mL 3.6989 mL 9.2473 mL
15 mM 0.2466 mL 1.2330 mL 2.4659 mL 6.1648 mL
20 mM 0.1849 mL 0.9247 mL 1.8495 mL 4.6236 mL
25 mM 0.1480 mL 0.7398 mL 1.4796 mL 3.6989 mL
30 mM 0.1233 mL 0.6165 mL 1.2330 mL 3.0824 mL
40 mM 0.0925 mL 0.4624 mL 0.9247 mL 2.3118 mL
50 mM 0.0740 mL 0.3699 mL 0.7398 mL 1.8495 mL
60 mM 0.0616 mL 0.3082 mL 0.6165 mL 1.5412 mL
80 mM 0.0462 mL 0.2312 mL 0.4624 mL 1.1559 mL
100 mM 0.0370 mL 0.1849 mL 0.3699 mL 0.9247 mL
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Tolbutamide 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.

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