Timolol Maleate

Catalog No.S4123 Synonyms: MK-950

Timolol Maleate Chemical Structure

Molecular Weight(MW): 432.49

Timolol Maleate is a non-selective, beta-adrenergic receptor antagonist for β1/β2 with Ki of 1.97 nM/2.0 nM.

Size Price Stock Quantity  
In DMSO USD 130 In stock
USD 60 In stock
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Biological Activity

Description Timolol Maleate is a non-selective, beta-adrenergic receptor antagonist for β1/β2 with Ki of 1.97 nM/2.0 nM.
Targets
β1-adrenergic receptor [2] β2-adrenergic receptor [2]
1.97 nM(Ki) 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. Timolol has been proposed as an antihypertensive, antiarrhythmic, antiangina, and antiglaucoma agent. Similar to propranolol and nadolol, timolol is a non-selective, beta-adrenergic receptor antagonist. [1] Timolol has a higher affinity for the beta 2-adrenoceptor than for the beta 1-adrenoceptor in human atrium. Timolol 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. [3] Timolol, when applied topically to the eye, 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. [4] Like propranolol and nadolol, timolol 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 timolol reduces ocular pressure is still not known. The most likely action is by decreasing the secretion of aqueous humor. [2]

Protocol

Solubility (25°C)

In vitro DMSO 86 mg/mL (198.84 mM)
Ethanol 86 mg/mL (198.84 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 432.49
Formula

C13H24N4O3S.C4H4O4

CAS No. 26921-17-5
Storage powder
in solvent
Synonyms MK-950

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03648229 Not yet recruiting Open-angle Glaucoma West Virginia University|University of Pittsburgh|University of Michigan September 1 2019 Phase 4
NCT03648229 Not yet recruiting Open-angle Glaucoma West Virginia University|University of Pittsburgh|University of Michigan September 1 2019 Phase 4
NCT03842631 Recruiting Infantile Hemangioma XiaoXi Lin|Shanghai Ninth People''s Hospital Affiliated to Shanghai Jiao Tong University February 16 2019 --
NCT03842631 Recruiting Infantile Hemangioma XiaoXi Lin|Shanghai Ninth People''s Hospital Affiliated to Shanghai Jiao Tong University February 16 2019 --
NCT03822559 Recruiting Open-angle Glaucoma Ocular Hypertension Santen Pharmaceutical Co. Ltd. January 20 2019 Phase 3
NCT03579160 Recruiting Wound of Skin|Wound Heal|Surgical Wound|Full Thickness Skin Graft Healing Brigham and Women''s Hospital January 2 2019 Phase 2|Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID