Tolbutamide
Based on 10 publication(s) in Google Scholar
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.
- Purity: 99.69%
- CAS No.: 64-77-7
- Formula: C12H18N2O3S
- Molecular Weight:270.35
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Tolbutamide
More- Cell Stem Cell. 2025 Apr 3;32(4):547-563.e7. [Abstract]
- Acta Pharm Sin B. 2024 Aug;14(8):3493-3512. [Abstract]
- Int J Biol Macromol. 2026 Mar:352:151224. [Abstract]
- ACS Environ Au. 2025 Aug 5;5(6):573-582. [Abstract]
- Anal Chem. 2025 Jun 3;97(21):11099-11109. [Abstract]
- Cancer Cell Int. 2023 Jan 31;23(1):14. [Abstract]
- AAPS J. 2021 Jun 28;23(4):91. [Abstract]
- Biology (Basel). 2025 Jul 20;14(7):889. [Abstract]
- Egypt J Neurosurg. 2026 Jan 8;41(1):4.
- medRxiv. 2024 Jul 23.
Customer Validation & Images
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Others
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Sf21 | IC50 |
>1000 μM
Compound: Tolbutamide
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Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
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[PMID: 21965623] |
| Sf21 | IC50 |
>1000 μM
Compound: Tolbutamide
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Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
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[PMID: 21965623] |
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.
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Cell Line:Glioma cell
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Concentration:400 μM
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Incubation Time:24h
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Result:Increasing the level of Cx43.
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.
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Animal Model:Non-obese-diabetic mouse [3]
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Dosage:125 mg/kg
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Administration:Supplemented in daily diet for 27 weeks
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Result:Showed 10 of 23 animals developed diabetes compared with 18 of 24 in the control groups.
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Animal Model:Pregnant mice [4]
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Dosage:100 mg/kg, 400 mg/kg
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Administration:Intraperitoneal injection (i.p.)
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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.
Chemical Information
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CAS No. 64-77-7
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Appearance Solid
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Molecular Weight 270.35
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Formula C12H18N2O3S
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Color White to off-white
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SMILES
O=S(C1=CC=C(C)C=C1)(NC(NCCCC)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (10)
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Journal Impact Factor
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Most Recent
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Cell Stem Cell
Enhanced viability and functional maturity of iPSC-derived islet organoids by collagen-VI-enriched ECM scaffolds. [Abstract]2025 Apr 3;32(4):547-563.e7. PMID: 39999846 -
Acta Pharm Sin B
Phenylalanine deprivation inhibits multiple myeloma progression by perturbing endoplasmic reticulum homeostasis. [Abstract]2024 Aug;14(8):3493-3512. PMID: 39220878 -
Int J Biol Macromol
Reticuline isomerase AKR1B1 with aldo-keto reductase activity and detoxification function from the insect Blaps rhynchopetera. [Abstract]2026 Mar:352:151224. PMID: 41791543 -
ACS Environ Au
Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]2025 Aug 5;5(6):573-582. PMID: 41277996 -
Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
Cancer Cell Int
In vitro co-culture systems of hepatic and intestinal cells for cellular pharmacokinetic and pharmacodynamic studies of capecitabine against colorectal cancer. [Abstract]2023 Jan 31;23(1):14. PMID: 36717845 -
AAPS J
Cannabinoid Interactions with Cytochrome P450 Drug Metabolism: a Full-Spectrum Characterization. [Abstract]2021 Jun 28;23(4):91. PMID: 34181150 -
Biology (Basel)
Germination Enhances Phytochemical Profiles of Perilla Seeds and Promotes Hair Growth via 5α-Reductase Inhibition and Growth Factor Pathways. [Abstract]2025 Jul 20;14(7):889. PMID: 40723446 -
Tolbutamide purchased from MedChemExpress. Usage Cited in: Egypt J Neurosurg. 2026 Jan 8;41(1):4.
Perforated cell recording of GT1-7 cells incubated in bath solution supplemented 2.5 mM glucose before and after perfusion of vehicle (top trace) or 10 nM leptin (bottom trace). After the membrane potential stabilized, 300 µM tolbutamide (tolb) was added to block KATP currents.
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Solvent & Solubility
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Sánchez‐Alvarez R, et al. Tolbutamide reduces glioma cell proliferation by increasing connexin43, which promotes the up‐regulation of p21 and p27 and subsequent changes in retinoblastoma phosphorylation [J]. Glia, 2006, 54(2): 125-134. [Content Brief]
[2]. Hœy M, et al. Tolbutamide stimulates exocytosis of glucagon by inhibition of a mitochondrial‐like ATP‐sensitive K+ (KATP) conductance in rat pancreatic A‐cells [J]. The Journal of Physiology, 2000, 527(1): 109-120. [Content Brief]
[3]. Williams A J K, et al. Tolbutamide reduces the incidence of diabetes mellitus, but not insulitis, in the non-obese-diabetic mouse [J]. Diabetologia, 1993, 36: 487-492. [Content Brief]
[4]. Belisle R J, et al. Tolbutamide treatment of pregnant mice: repeated administration reduces fetal lethality [J]. Teratology, 1976, 13(1): 65-70. [Content Brief]
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 |
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| 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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