Name: Timolol Maleate
Brand: Selleck Chemicals
SKU: S4123
Availability: InStock
Rating: 5 (2 reviews)

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Quality Control

Batch: Purity: 99.97%

99.97

Related Targets	AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Other Adrenergic Receptor Inhibitors	Zenidolol (ICI-118551) Hydrochloride Yohimbine HCl L755507 Atipamezole Higenamine hydrochloride Fenoterol hydrobromide Medetomidine HCl Rauwolscine hydrochloride Deoxycorticosterone acetate Detomidine HCl

Solubility

In vitro
Batch:

DMSO : 86 mg/mL (198.84 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 86 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

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%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	432.49	Formula	C₁₃H₂₄N₄O₃S.C₄H₄O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	26921-17-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	MK-950,(S)-Timolol Maleate			Smiles	CC(C)(C)NCC(COC1=NSN=C1N2CCOCC2)O.C(=CC(=O)O)C(=O)O

Mechanism of Action

Targets/IC₅₀/Ki	β1-adrenergic receptor 1.97 nM(Ki) β2-adrenergic receptor 2.0 nM(Ki)
In vitro	Timolol Maleate is a beta-adrenergic antagonist similar in action to propranolol. The levo-isomer is the more active. This compound has been proposed as an antihypertensive, antiarrhythmic, antiangina, and antiglaucoma agent. Similar to propranolol and nadolol, this compound is a non-selective, beta-adrenergic receptor antagonist. This chemical has a higher affinity for the beta 2-adrenoceptor than for the beta 1-adrenoceptor in human atrium. It does not have significant intrinsic sympathomimetic, direct myocardial depressant, or local anesthetic (membrane-stabilizing) activity, but does possess a relatively high degree of lipid solubility. When applied topically to the eye, this agent has the action of reducing elevated, as well as normal, intraocular pressure, whether or not accompanied by glaucoma. Elevated intraocular pressure is a major risk factor in the pathogenesis of glaucomatous visual field loss and optic nerve damage. Like propranolol and nadolol, it competes with adrenergic neurotransmitters such as catecholamines for binding at β1-adrenergic receptors in the heart and vascular smooth muscle and β2-receptors in the bronchial and vascular smooth muscle. β1-receptor blockade results in a decrease in resting and exercise heart rate and cardiac output, a decrease in both systolic and diastolic blood pressure, and, possibly, a reduction in reflex orthostatic hypotension. β2-blockade results in an increase in peripheral vascular resistance. The exact mechanism whereby this compound reduces ocular pressure is still not known. The most likely action is by decreasing the secretion of aqueous humor.
References	[1] https://pubmed.ncbi.nlm.nih.gov/238479/ [2] https://pubmed.ncbi.nlm.nih.gov/1686051/ [3] https://pubmed.ncbi.nlm.nih.gov/8864321/ [4] https://pubmed.ncbi.nlm.nih.gov/10870519/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04828057	Completed	Ocular Surface Disease\|Primary Open Angle Glaucoma	Santen Pharmaceutical (Taiwan) Co. LTD	September 1 2021	--
NCT03282981	Completed	Chronic Diabetic Foot Ulcers\|Diabetic Neuropathic Ulcers\|Non Healing Wound	VA Office of Research and Development\|VA Northern California Health Care System	June 14 2018	Phase 3
NCT04903366	Completed	Glaucoma Open-Angle\|Chronic Wounds	VA Northern California Health Care System	November 21 2017	--

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Timolol Maleate Adrenergic Receptor antagonist

Chemical Structure

Molecular Weight: 432.49