非选择性β-肾上腺素能受体拮抗剂,(S)-Timolol马来酸盐是非选择性β-肾上腺素受体拮抗剂，对β1和β2受体亚型的Ki分别为1.97和2.0 nM。
中文名称 :Timolol Maleate
中文别名 :马来酸噻吗洛尔;(S)-马来酸噻吗洛尔;(S)-3-[3-(叔丁基氨基)-2-羟基丙氧基]-4-吗啉基-1,2,5-噻二唑马来酸盐;马来酸噻吗咯尔 EP标准品;马来酸噻吗洛尔 USP标准品;马来酸噻吗洛尔 标准品;噻吗咯尔系统适用性 EP标准品;马来酸噻吗心安;噻吗洛尔马来酸;S-马来酸噻吗洛尔
英文名称 :Timolol Maleate
英文别名 :timolol maleate;(S)-[1-(1,1dimethylethyl)amino]-3-[[4-(4-morpholinyl)-1,2,5-thiadiazol-3-yl]oxy]-2-propanol maleate;(S)-(-)-Timolol Maleate;(S)-Timolol maleate;Betim;Timolol maleate salt;S-(−)-1-(t-Butylamino)-3-[(4-morpholino-1,2,5-thiadiazol-3-yl)oxy]-2-propanol maleate salt;Timolol hydrogen maleate;(S)-1-((1,1-Dimethylethyl)amino)-3-((4-(4-morpholinyl)-1,2,5-thiadiazol-3-yl)oxy)-2-propanol (Z)-2-butenedioate (1:1);(S)-3-[3-(tert-butylamino)-2-hydroxypropoxy]-4-morpholino-1,2,5-thiadiazole monom;(S)-3-[3-(tert-butylamino)-2-hydroxypropoxy]-4-morpholino-1,2,5-thiadiazole monomaleate;Timoptic;Blocadren;Timacor;Betime;Timoptic-XE;l-Timolol maleate;(S)-Timolol (Maleate);Timoptic in Ocudose;(S)-Timolol hydrogen maleate;C13H24N4O3S.C4H4O4;MK 950;MLS000028539;P8Y54F701R;(-)-1-(tert-Butylamino)-3-((4-morpholino-1,2,5-thiadiazol-3-yl)oxy)-2-propanol maleate;SMR000058305;(S)-3-[3-(tert-butylamino)-2-hydroxypropoxy]-4-morpholino-1,2,5-thi
Cas No. :26921-17-5
分子式 :C17H28N4O7S
分子量 :432.49
包装储存 :4°C, sealed storage, away from moisture
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
生物活性
(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.
性状
Solid
IC50 & Target[1][2]
Ki: 1.97 nM (β1-adrenoceptor); 2.0 nM (β2-adrenoceptor)
体外研究(In Vitro)
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.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature or refrigerated transportation.
储存方式
4°C, sealed storage, away from moisture
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
ClinicalTrial
参考文献
[1]. Mitrovi? 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. [Information]
[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. [Information]
[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. [Information]
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