Timolol (Synonyms: (S)-L-714,465; MK 950 free base)

Cat. No.: HY-17494: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form ((S)-Timolol maleate) usually boasts enhanced water solubility and stability.

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

Timolol Chemical Structure

CAS No. : 26839-75-8

Size	Price	Stock
5 mg		Ask For Quote & Lead Time
10 mg		Ask For Quote & Lead Time
25 mg		Ask For Quote & Lead Time
50 mg		Ask For Quote & Lead Time
100 mg		Ask For Quote & Lead Time

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This product is a controlled substance and not for sale in your territory.

Other In-stock Forms of Timolol:

(S)-Timolol maleate

Other Forms of Timolol:

5 Publications Citing Use of MCE Timolol

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View All Adrenergic Receptor Isoform Specific Products:

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α adrenergic receptor β adrenergic receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

β adrenergic receptor

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	> 100 μM Compound: Timolol	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	[PMID: 32216987]
SK-MEL-28	IC₅₀	> 100 μM Compound: Timolol	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	[PMID: 32216987]
SK-MEL-5	IC₅₀	> 100 μM Compound: Timolol	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	[PMID: 32216987]

In Vitro

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.

In Vivo

Timolol has a cardioprotective effect via inhibition of ERS response in diabetic rats^[3].

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

Animal Model:	Experimental diabetes model: 3-month old male Wistar rats^[3].
Dosage:	5 mg/kg
Administration:	Timolol (5 mg/kg daily for 12-week)
Result:	Showed cardioprotective effect.

Clinical Trial

Molecular Weight

316.42

Formula

C₁₃H₂₄N₄O₃S

CAS No.

26839-75-8

Appearance

Oil

Color

Colorless to light yellow

SMILES

O[C@H](COC1=NSN=C1N2CCOCC2)CNC(C)(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.1604 mL	15.8018 mL	31.6036 mL
5 mM	0.6321 mL	3.1604 mL	6.3207 mL
10 mM	0.3160 mL	1.5802 mL	3.1604 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 (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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (15.80 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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: 96.72%

Select Batch:

Data Sheet (277 KB) SDS (557 KB)

COA (251 KB) HNMR (142 KB) RP-HPLC (171 KB) LCMS (109 KB)

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

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

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:

Timolol26839-75-8(S)-L-714,465MK 950MK950MK-950Adrenergic ReceptorBeta Receptorβ-blockeropen-angle glaucomaocular hypertensioninfantile hemangiomashypertensionmyocardial infarctionmigraine prophylaxisatrial fibrillationInhibitorinhibitorinhibit

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