| Bioactivity | (S)-Timolol Maleate (L-714,465 Maleate) is a non-cardioselective hydrophilic β-adrenoceptor blocker. (S)-Timolol Maleate is widely used as standard medication for intraocular pressure (glaucoma) by preventing the production of aqueous humor. (S)-Timolol Maleate can be used for hypertension, angina pectoris and myocardial infarction[1][2][3]. |
| Target | Ki: 1.97 nM (β1-adrenoceptor); 2.0 nM (β2-adrenoceptor) |
| Invitro | Timolol maleate represents a chiral compound with one asymmetric carbon in its structure. Single isomer, (S)-enantiomer, is the commercially available form and as a non-cardioselective β-adrenergic blocker. Its commonest application is in topical treatment of increasing intraocular pressure in patients with chronic open angle glaucoma and also in aphakic patients[1]. |
| In Vivo | There are reports that indicate lower biological activity of (R)-isomer compared to (S)-isomer. Namely, (R)-timolol is 49 times less potent than (S)-timolol on β-adrenoceptor in animals, 13 times less potent in constricting the airways of normal subjects[1]. |
| Name | (S)-Timolol Maleate |
| CAS | 26921-17-5 |
| Formula | C17H28N4O7S |
| Molar Mass | 432.49 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Mitrović M, et al. Analytical quality by design development of an ecologically acceptable enantioselective HPLC method for timolol maleate enantiomeric purity testing on ovomucoid chiral stationary phase. J Pharm Biomed Anal. 2020 Feb 20;180:113034. [2]. Wedian F, et al. Simultaneous spectrofluorometric analysis of tablets containing hydrochlorothiazide combined with timolol maleate or amiloride hydrochloride. Acta Pharm. 2020 Sep 1;70(3):373-385. [3]. Sun L, et al. Fractional 2940-nm Er:YAG Laser-Assisted Drug Delivery of Timolol Maleate for the Treatment of Deep Infantile Hemangioma. J Dermatolog Treat. 2020 Feb 11:1-24. |
(S)-Timolol Maleate
CAS: 26921-17-5 F: C17H28N4O7S W: 432.49
(S)-Timolol Maleate (L-714,465 Maleate) is a non-cardioselective hydrophilic β-adrenoceptor blocker. (S)-Timolol Maleat
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