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Merck
CN

T6394

噻吗洛尔 马来酸盐

≥98% (TLC), β-adrenoceptor antagonist, powder

别名:

(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 马来酸盐, (S)-马来酸噻吗洛尔

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关于此项目

经验公式（希尔记法）:
C13H24N4O3S · C4H4O4
化学文摘社编号:
26921-17-5
分子量:
432.49
NACRES:
NA.77
PubChem Substance ID:
24277810
UNSPSC Code:
12352200
EC Number:
248-111-5
MDL number:
MFCD00058356

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产品名称

噻吗洛尔 马来酸盐, ≥98% (TLC), powder

InChI key

WLRMANUAADYWEA-NWASOUNVSA-N

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 string

[H]\C(=C(/[H])C(O)=O)C(O)=O.CC(C)(C)NC[C@H](O)COc1nsnc1N2CCOCC2

assay

≥98% (TLC)

form

powder

optical activity

[α]25/D -5.4°, c = 4.9 in 1 M HCl(lit.)

color

white to off-white

mp

202-203 °C (lit.)

solubility

H2O: soluble, ethanol: soluble

ε (extinction coefficient)

8,700 at 294 nm at 1 M

originator

Merck & Co., Inc., Kenilworth, NJ, U.S.

Quality Level

200

Gene Information

human ... ADRB1(153), ADRB2(154), ADRB3(155)

相关类别

Application

Timolol maleate has been used as an adrenergic β-blocker for evaluating cardiovascular functions in mice5. It has also been used for evaluating the uptake of 86Rb+ in rat cardiomyocytes6.

Biochem/physiol Actions

Timolol maleate is a class II anti-arrhythmic agent that functions as a non-selective β-adrenoceptor antagonist, a vasodilator and an anti-glaucoma agent. Studies have reported that timolol maleate can be used for the treatment of infantile hemangioma (IH)7.

Features and Benefits

This compound was developed by Merck & Co., Inc., Kenilworth, NJ, U.S.. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Preparation Note

Timolol maleate is soluble in ethanol and water.

pictograms

Health hazardExclamation mark
GHS08,GHS07

signalword

Warning

hcodes

H302,H361

Hazard Classifications

Acute Tox. 4 Oral - Repr. 2

存储类别

11 - Combustible Solids

wgk

WGK 3

ppe

Eyeshields, Gloves, type P3 (EN 143) respirator cartridges

法规信息

监管及禁止进口产品
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历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
SLBC3834V
061K1290
045H1255
045H1254
073H0074

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Ajith Chakkittakandiyil et al.
Pediatric dermatology, 29(1), 28-31 (2011-12-14)
Therapeutic options for superficial infantile hemangiomas (IH) are limited. Recently, timolol maleate gel, a topical nonselective beta-blocker, has been reported as a potentially effective treatment for superficial IH. This study is an extension of a previously published pilot study designed
G C Chiou et al.
Journal of ocular pharmacology, 8(3), 183-190 (1992-01-01)
An ocular hypertensive rabbit eye model was used to study the effect of L- and D-timolol on retinal and choroidal blood flow. Ocular hypertension was induced artificially by raising the intraocular pressure to 40 mmHg which reduced the ocular blood
Verena Prokosch et al.
PloS one, 8(2), e49730-e49730 (2013-03-08)
Optic nerve atrophy caused by abnormal intraocular pressure (IOP) remains the most common cause of irreversible loss of vision worldwide. The aim of this study was to determine whether topically applied IOP-lowering eye drugs affect retinal ganglion cells (RGCs) and
A Tomidokoro et al.
Current eye research, 18(5), 381-390 (1999-06-18)
To evaluate the effects of topical carteolol or timolol on tissue circulation in the iris and posterior choroid. After a topical instillation of 20 microl of 2% carteolol, 0.5% timolol, or physiological saline (for control) into one eye, and physiological
Jin-Wei Cheng et al.
PloS one, 7(9), e45079-e45079 (2012-10-03)
The first goal of medical therapy in glaucoma is to reduce intraocular pressure (IOP), and the fixed-combination medications are needed to achieve sufficiently low target IOP. The aim of this systematic review and meta-analysis is to evaluate IOP-lowering effect of
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