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Timolol Maleate(L-714,465 Maleate MK 950)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Timolol Maleate(L-714,465 Maleate MK 950)图片
CAS NO:26921-17-5
规格:≥98%
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议
1g电议
2g电议
5g电议
10g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)432.49
FormulaC13H24N4O3S.C4H4O4
CAS No.26921-17-5
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 86 mg/mL (198.8 mM)
Water: <1 mg/mL
Ethanol: 86 mg/mL (198.8 mM)
Other InfoChemical Name: (S)-1-(tert-butylamino)-3-((4-morpholino-1,2,5-thiadiazol-3-yl)oxy)propan-2-ol maleate
InChi Key: WLRMANUAADYWEA-NWASOUNVSA-N
InChi Code: InChI=1S/C13H24N4O3S.C4H4O4/c1-13(2,3)14-8-10(18)9-20-12-11(15-21-16-12)17-4-6-19-7-5-17;5-3(6)1-2-4(7)8/h10,14,18H,4-9H2,1-3H3;1-2H,(H,5,6)(H,7,8)/b;2-1-/t10-;/m0./s1
SMILES Code: CC(C)(NC[C@H](O)COC1=NSN=C1N2CCOCC2)C.O=C(O)/C=C\C(O)=O
SynonymsMK-950; L 714,465; MK950; Optimol; Timacar; Timolol maleate;L-714,465; L714,465; MK 950; MK-950; brand name: Betimol, Blocadren, Istalol, Timoptic, Timoptic-XE, Timoptic OcuDose.
实验参考方法
In Vitro

In vitro activity: 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. 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. 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. 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.

In Vivo
Animal model
Formulation & Dosage
ReferencesArch Int Pharmacodyn Ther. 1975 Feb;213(2):251-63; Br J Clin Pharmacol. 1996 Aug;42(2):217-23.