Timolol
Based on 6 publication(s) in Google Scholar
Timolol is a β-blocker available for both topical and systemic administration. Topical Timolol is primarily used to reduce intraocular pressure with open-angle glaucoma and ocular hypertension. Timolol can also be used for the research of infantile hemangiomas, hypertension, myocardial infarction, migraine prophylaxis, and atrial fibrillation.Timolol also has cardioprotective effect.
For research use only. We do not sell to patients.
- CAS No.: 26839-75-8
- Formula: C13H24N4O3S
- Molecular Weight:316.42
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
Publications Citing Use of MedChemExpress (MCE) Timolol
More
Customer Validation & Images
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In Vivo Efficacy Study
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Cell Imaging/Staining
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In Vivo Efficacy Study
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Cell Imaging/Staining
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Cell Proliferation/Viability Assay
All Adrenergic Receptor Isoforms
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Biological Activity
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β adrenergic receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
>100 μM
Compound: Timolol
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Antiproliferative activity against human A375 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
Antiproliferative activity against human A375 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
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[PMID: 32216987] |
| SK-MEL-28 | IC50 |
>100 μM
Compound: Timolol
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Antiproliferative activity against human SK-MEL-28 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
Antiproliferative activity against human SK-MEL-28 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
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[PMID: 32216987] |
| SK-MEL-5 | IC50 |
>100 μM
Compound: Timolol
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Antiproliferative activity against human SK-MEL-5 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
Antiproliferative activity against human SK-MEL-5 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
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[PMID: 32216987] |
Timolol can significantly prevent the increased lipid peroxidation level of the heart from diabetic rats. Timolol can induce a well-balanced ratio between oxidative stress and antioxidant defense system in the diabetic animals, can have an important cardioprotection against diabetes-induced ERS and associated apoptotic effects[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Experimental diabetes model: 3-month old male Wistar rats[3].
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Dosage:5 mg/kg
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Administration:Timolol (5 mg/kg daily for 12-week)
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Result:Showed cardioprotective effect.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 26839-75-8
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Appearance Oil
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Molecular Weight 316.42
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Formula C13H24N4O3S
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Color Colorless to light yellow
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SMILES
O[C@H](COC1=NSN=C1N2CCOCC2)CNC(C)(C)C
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Synonyms
(S)-L-714,465; MK 950 free base
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (6)
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Journal Impact Factor
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Most Recent
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Adv Mater
Colloid-Forming Prodrug-Hydrogel Composite Prolongs Lower Intraocular Pressure in Rodent Eyes after Subconjunctival Injection. [Abstract]2025 Feb;37(8):e2419306. PMID: 39763100
Timolol purchased from MedChemExpress. Usage Cited in: Adv Mater. 2025 Feb;37(8):e2419306. [Abstract]
Live-cell percentages were assessed by calcein-AM and Hoechst staining in hTCEpi cells after treatment with Timolol maleate ((S)-Timolol Maleate; 0.137% w/v; 24 h). The Timolol maleate group showed a significantly lower percentage of live cells.
Timolol purchased from MedChemExpress. Usage Cited in: Adv Mater. 2025 Feb;37(8):e2419306. [Abstract]
IOP was monitored over 24 h and 56 d in rats after a single subconjunctival injection of soluble Timolol maleate ((S)-Timolol Maleate; 0.137% w/v, 30 μL). Timolol maleate significantly reduced IOP at 6 h, but the effect was no longer significant at 24 h.
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Timolol purchased from MedChemExpress. Usage Cited in: Adv Funct Mater. 2026 Jun 11.
IOP was monitored in New Zealand white rabbits after a single subconjunctival injection of (S)-timolol maleate solution or DSGS-T (DSGS loaded with (S)-timolol maleate) (Timolol maleate; both 1 mg/mL, 0.1 mL per eye; single dose). Timolol maleate and DSGS-T significantly decreased IOP compared with saline.
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Protein Cell
Identification of serotonin 2A receptor as a novel HCV entry factor by a chemical biology strategy. [Abstract]2019 Mar;10(3):178-195. PMID: 29542010
Timolol purchased from MedChemExpress. Usage Cited in: Protein Cell. 2019 Mar;10(3):178-195. [Abstract]
Cell viability was assessed in Huh7.5.1 cells after treatment with (S)-timolol maleate ((S)-timolol; 10 μM; 48 h) and expressed relative to 0.5% DMSO-treated control cells.
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Redox Biol
2025 Feb:79:103481. PMID: 39721495 -
Mater Today Bio
Transdermal delivery of timolol maleate using hydrogel microneedles for the treatment of infantile haemangiomas. [Abstract]2025 Apr 12:32:101752. PMID: 40290897
Timolol purchased from MedChemExpress. Usage Cited in: Mater Today Bio. 2025 Apr 12:32:101752. [Abstract]
Live-dead cell staining demonstrates the effects of different timolol maleate ((S)-Timolol maleate,TIM; 600-1500 μM; 24 h) concentrations on the cell morphology of 3D-cultured HemECs. Compared to control group, TIM-treated HemECs showed the disappearance of filopodia, exhibited a rounded shape, and had a significant reduction in cell count.
Timolol purchased from MedChemExpress. Usage Cited in: Mater Today Bio. 2025 Apr 12:32:101752. [Abstract]
Cell viability was assessed by CCK-8 in 3D-cultured HemECs after treatment with Timolol maleate ((S)-Timolol maleate,TIM; 600-1500 μM; 24 h) and in 2D-cultured HemECs after treatment with TIM (10-10000 mM; 24 or 48 h). TIM inhibited HemEC growth in a concentration-dependent manner.
Timolol purchased from MedChemExpress. Usage Cited in: Mater Today Bio. 2025 Apr 12:32:101752. [Abstract]
Hemangioma appearance and volume were evaluated in mouse with haemangiomas and tumour grafts after treatment for 2 weeks with Free TIM ((S)-Timolol maleate; 0.5%, 40 μL/cm²; topical administration; three times daily) or BSAMA-TIM-MNs (9 mg/mL; transdermal microneedles; replaced every 3 d). BSAMA-TIM-MNs controlled hemangioma volume more effectively than Free TIM or blank microneedles and produced a decreasing trend in hemangioma size.
Timolol purchased from MedChemExpress. Usage Cited in: Mater Today Bio. 2025 Apr 12:32:101752. [Abstract]
H&E staining of hemangiomas from mouse with haemangiomas and tumour grafts after treatment for 2 weeks with Free TIM ((S)-Timolol maleate; 0.5%, 40 μL/cm²; topical administration; three times daily) or BSAMA-TIM-MNs (9 mg/mL; transdermal microneedles; replaced every 3 d). H & E staining of the haemangioma tissue revealed a reduced number of microvessels in the BSAMA-TIM-MNs group compared to those in the other three groups.
Timolol purchased from MedChemExpress. Usage Cited in: Mater Today Bio. 2025 Apr 12:32:101752. [Abstract]
GLUT-1 immunofluorescence staining and fluorescence intensity in mouse with haemangiomas and tumour grafts after treatment for 2 weeks with Free TIM ((S)-Timolol maleate; 0.5%, 40 μL/cm²; topical administration; three times daily) or BSAMA-TIM-MNs (9 mg/mL; transdermal microneedles; replaced every 3 d). The fluorescence intensity of GLUT-1 was weaker after treatment with BSAMA-TIM-MNs than in the other three groups.
Timolol purchased from MedChemExpress. Usage Cited in: Mater Today Bio. 2025 Apr 12:32:101752. [Abstract]
GLUT-1 expression was examined by western blotting in mouse with haemangiomas and tumour grafts after treatment for 2 weeks with Free TIM ((S)-Timolol maleate; 0.5%, 40 μL/cm²; topical administration; three times daily) or BSAMA-TIM-MNs (9 mg/mL; transdermal microneedles; replaced every 3 d). GLUT-1 expression was reduced by treatment with BSAMA-TIM-MNs and Free TIM.
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Solvent & Solubility
DMSO : 100 mg/mL (316.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 5 mg/mL (15.80 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (15.80 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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 (557 KB)
- English - EN (557 KB)
- Français - FR (557 KB)
- Deutsch - DE (557 KB)
- Norwegian - NO (557 KB)
- Español - ES (557 KB)
- Swedish - SV (557 KB)
- Italian - IT (557 KB)
- Korean - KR (557 KB)
- Portuguese - PT (557 KB)
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Handling Instructions (2659 KB)
References
[1]. James Barnes; Majid Moshirfar. Timolol.
[2]. E. Ansari, et al. Treatment of open-angle glaucoma and ocular hypertension with preservative-free tafuprost/timolol fxed-dose combination therapy: 6 case reports and clinical outcomes. BMC Ophthalmol. 2022 Apr 2;22(1):152. [Content Brief]
[3]. Figen Amber Cicek, et al. Beta-blocker timolol alleviates hyperglycemia-induced cardiac damage via inhibition of endoplasmic reticulum stress. J Bioenerg Biomembr. 2014 Oct;46(5):377-87. [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, 6 months; -20°C, 1 month (protect from light). 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1604 mL | 15.8018 mL | 31.6036 mL | 79.0089 mL |
| 5 mM | 0.6321 mL | 3.1604 mL | 6.3207 mL | 15.8018 mL | |
| 10 mM | 0.3160 mL | 1.5802 mL | 3.1604 mL | 7.9009 mL | |
| 15 mM | 0.2107 mL | 1.0535 mL | 2.1069 mL | 5.2673 mL | |
| 20 mM | 0.1580 mL | 0.7901 mL | 1.5802 mL | 3.9504 mL | |
| 25 mM | 0.1264 mL | 0.6321 mL | 1.2641 mL | 3.1604 mL | |
| 30 mM | 0.1053 mL | 0.5267 mL | 1.0535 mL | 2.6336 mL | |
| 40 mM | 0.0790 mL | 0.3950 mL | 0.7901 mL | 1.9752 mL | |
| 50 mM | 0.0632 mL | 0.3160 mL | 0.6321 mL | 1.5802 mL | |
| 60 mM | 0.0527 mL | 0.2634 mL | 0.5267 mL | 1.3168 mL | |
| 80 mM | 0.0395 mL | 0.1975 mL | 0.3950 mL | 0.9876 mL | |
| 100 mM | 0.0316 mL | 0.1580 mL | 0.3160 mL | 0.7901 mL |
Timolol Related Classifications
HY-17494 Related Classifications
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