CAS Number26921-17-5
Synonyms(-)-1-(tert-Butylamino)-3-[(4-morpholino-1,2,5-thiadiazol-3-yl)oxy]-2-propanol Maleate (1:1) (Salt); Timolol maleate salt; Betim; Tenopt; Proflax; Aquanil; Timorom; (S)-Timolol maleate; Rysmon TG; EINECS 248-111-5; Optimol; (-)-Timolol Maleate; Timacar; (S)-(-)-Timolol Maleate; Temserin; MFCD00058356; Timolol maleate; (S)-Timolol (Maleate)
Molecular FormulaC17H28N4O7S
Molecular Weight437.52
Purity≥98 (CP)%
Boiling Point704.6ºC at 760 mmHg
Melting Point202-203 °C(lit.)
Appearancesolid
EINECS248-111-5
Symbol
Signal WordWarning
| Chemical & Physical Properties | |
|---|---|
| CAS Number | 26921-17-5 |
| Catalog No. | 2A-9008841 |
| Chinese Name | 马来酸噻吗洛尔 |
| Synonyms | (-)-1-(tert-Butylamino)-3-[(4-morpholino-1,2,5-thiadiazol-3-yl)oxy]-2-propanol Maleate (1:1) (Salt); Timolol maleate salt; Betim; Tenopt; Proflax; Aquanil; Timorom; (S)-Timolol maleate; Rysmon TG; EINECS 248-111-5; Optimol; (-)-Timolol Maleate; Timacar; (S)-(-)-Timolol Maleate; Temserin; MFCD00058356; Timolol maleate; (S)-Timolol (Maleate) |
| Molecular Formula | C17H28N4O7S |
| Molecular Weight | 437.52 |
| Purity | ≥98 (CP) |
| Boiling Point | 704.6ºC at 760 mmHg |
| Melting Point | 202-203 °C(lit.) |
| Appearance | solid |
| Water Solubility | H2O: soluble |
| Storage Condition | Store in a compact container in a cool, dry place |
| Application | (S)-Timolol maleate is a non-selective β-adrenergic receptor antagonist with Ki of 1.97 and 2.0 nM for β1 and β2 receptor subtypes, respectively. |
| EINECS | 248-111-5 |
| HTC | 2934999090 |
| MDL Number | MFCD28899668 |
| SMILES | CC(C)(C)NC([2H])([2H])C(O)([2H])C([2H])([2H])OC1=NSN=C1N2CCOCC2.OC(/C=C\C(O)=O)=O |
| UNSPSC | 12352005 |
| Hazard Symbols | Xn |
| Risk Codes | R22-63 |
| Safety Description | S36 |
| MSDS | msds/8841_1_26921_17_5.pdf |
| Bioactivity | (S)-Timolol maleate, is a potent non-selective β-adrenergic receptor antagonist (Ki values are 1.97 and 2.0 nM for β1 and β2 receptor subtypes respectively). IC50 Value: 1.97 nM(Ki for β1); 2.0 nM(Ki for β2)Target: β-adrenergic receptor(S)-Timolol, 50% bioavailability following oral administration. Does not cross the blood brain barrier. Timolol maleate does appear to have some local anesthetic properties in human cornea after chronic use by susceptible individuals. Related Catalog Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor Research Areas >> Neurological Disease References [1]. Deepika Aggarwal, Indu P. Kaur. Improved pharmacodynamics of timolol maleate from a mucoadhesive niosomal ophthalmic drug delivery system. International Journal of Pharmaceutics. 2005, 290(1-2): 155-159. [2]. Mandagere AK, Thompson TN, Hwang KK. Graphical model for estimating oral bioavailability of drugs in humans and other species from their Caco-2 permeability and in vitro liver enzyme metabolic stability rates. J Med Chem. 2002;45(2):304-11. [3]. A.H El-Kamel. In vitro and in vivo evaluation of Pluronic F127-based ocular delivery system for timolol maleate. International Journal of Pharmaceutics. 2002, 241, (1) :47-55. [4]. Konstas AG, Maltezos AC, Gandi S, et al. Comparison of 24-hour intraocular pressure reduction with two dosing regimens of latanoprost and timolol maleate in patients with primary open-angle glaucoma. American Journal of Ophthalmology .1999, 128(1):15-20. Chemical & Physical Properties Boiling Point 704.6ºC at 760 mmHg Melting Point 202-203 °C(lit.) Molecular Formula C17H28N4O7S Molecular Weight 432.492 Flash Point 380ºC Exact Mass 432.167877 PSA 182.58000 LogP 0.67020 Appearance of Characters powder | white to off-white Vapour Pressure 7.7E-21mmHg at 25°C Storage condition Store at RT Water Solubility H2O: soluble |
| Use of | (S)-Timolol maleate, is a potent non-selective β-adrenergic receptor antagonist (Ki values are 1.97 and 2.0 nM for β1 and β2 receptor subtypes respectively). IC50 Value: 1.97 nM(Ki for β1); 2.0 nM(Ki for β2)Target: β-adrenergic receptor(S)-Timolol, 50% bioavailability following oral administration. Does not cross the blood brain barrier. Timolol maleate does appear to have some local anesthetic properties in human cornea after chronic use by susceptible individuals. Properties Articles51 Name (S)-timolol maleate Synonym More Synonyms (S)-timolol maleate Biological Activity Description (S)-Timolol maleate, is a potent non-selective β-adrenergic receptor antagonist (Ki values are 1.97 and 2.0 nM for β1 and β2 receptor subtypes respectively). IC50 Value: 1.97 nM(Ki for β1); 2.0 nM(Ki for β2)Target: β-adrenergic receptor(S)-Timolol, 50% bioavailability following oral administration. Does not cross the blood brain barrier. Timolol maleate does appear to have some local anesthetic properties in human cornea after chronic use by susceptible individuals. Related Catalog Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor Research Areas >> Neurological Disease References [1]. Deepika Aggarwal, Indu P. Kaur. Improved pharmacodynamics of timolol maleate from a mucoadhesive niosomal ophthalmic drug delivery system. International Journal of Pharmaceutics. 2005, 290(1-2): 155-159. [2]. Mandagere AK, Thompson TN, Hwang KK. Graphical model for estimating oral bioavailability of drugs in humans and other species from their Caco-2 permeability and in vitro liver enzyme metabolic stability rates. J Med Chem. 2002;45(2):304-11. [3]. A.H El-Kamel. In vitro and in vivo evaluation of Pluronic F127-based ocular delivery system for timolol maleate. International Journal of Pharmaceutics. 2002, 241, (1) :47-55. [4]. Konstas AG, Maltezos AC, Gandi S, et al. Comparison of 24-hour intraocular pressure reduction with two dosing regimens of latanoprost and timolol maleate in patients with primary open-angle glaucoma. American Journal of Ophthalmology .1999, 128(1):15-20. Chemical & Physical Properties Molecular Formula C17H28N4O7S Exact Mass 432.167877 PSA 182.58000 LogP 0.67020 Appearance of Characters powder | white to off-white Storage condition Store at RT Water Solubility H2O: soluble |
| Tax Rebate | 13.0% |
| Supervision | None. MFN tariff: 6.5%. Ordinary tariff: 20.0% |
| Transport Info | Product name: Summary 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
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