| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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| 5g |
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Purity: ≥98%
Timolol Maleate (Optimol; Timacar; L714,465; MK-950; Betimol, Blocadren, Istalol, Timoptic), the maleate salt of timolol, is a non-selective β/beta-adrenergic receptor antagonist with antihypertensive, antiarrhythmic, antiangina, and antiglaucoma activities. It has a Kis of 1.97 nM/2.0 nM and inhibits β1/β2 adrenergic receptors. Timolol functions similarly to propranolol as a beta-adrenergic antagonist. More activity is found in the levo-isomer. It has been suggested that timolol works as an antihypertensive, antiarrhythmic, anti-angina, and antiglaucoma drug. The World Health Organization has compiled a list of essential medicines, or those that are absolutely necessary in a basic health system, which includes timol maleate.
| Targets |
β1-adrenergic receptor ( Ki = 1.97 nM ); β2-adrenergic receptor ( Ki = 2.0 nM )
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| ln Vivo |
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| Animal Protocol |
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| References |
| Molecular Formula |
C17H28N4O7S
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|---|---|
| Molecular Weight |
432.49
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| Exact Mass |
432.17
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| Elemental Analysis |
C, 47.21; H, 6.53; N, 12.95; O, 25.89; S, 7.41
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| CAS # |
26921-17-5
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| Related CAS # |
(Rac)-Timolol-d5 maleate; 1217260-21-3; (S)-Timolol-d9 maleate; Timolol; 26839-75-8
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| Appearance |
White to off-white crystalline powder
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| SMILES |
CC(C)(C)NC[C@@H](COC1=NSN=C1N2CCOCC2)O.C(=C\C(=O)O)\C(=O)O
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| InChi Key |
WLRMANUAADYWEA-NWASOUNVSA-N
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| 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
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| Chemical Name |
(Z)-but-2-enedioic acid;(2S)-1-(tert-butylamino)-3-[(4-morpholin-4-yl-1,2,5-thiadiazol-3-yl)oxy]propan-2-ol
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| Synonyms |
MK-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
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.78 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.78 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.78 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 20 mg/mL (46.24 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3122 mL | 11.5610 mL | 23.1219 mL | |
| 5 mM | 0.4624 mL | 2.3122 mL | 4.6244 mL | |
| 10 mM | 0.2312 mL | 1.1561 mL | 2.3122 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03282981 | Active Recruiting |
Drug: Timolol Drug: Non biologically active gel |
Chronic Diabetic Foot Ulcers Non Healing Wound |
VA Office of Research and Development |
June 14, 2018 | Phase 3 |
| NCT03519386 | Active Recruiting |
Drug: Sham surgery + active -comparator eye drops Combination Product: G2-TR intraocular implant containing travoprost |
Glaucoma, Open-Angle Ocular Hypertension |
Glaukos Corporation | July 26, 2018 | Phase 3 |
| NCT01873131 | Recruiting | Drug: topical timolol maleate Device: Pulsed dye laser |
Hemangioma | Massachusetts General Hospital | February 2011 | Not Applicable |
| NCT05597813 | Not yet recruiting | Procedure: microneedling Procedure: microneedling with topical timolol 0.5% |
Acne Scars - Mixed Atrophic and Hypertrophic |
Zagazig University | March 1, 2023 | Not Applicable |
| NCT06120842 | Recruiting | Device: SpyGlass IOL Drug: Bimatoprost Implant System (High Dose) |
Cataract Glaucoma |
SpyGlass Pharma, Inc. | October 13, 2023 | Phase 1 Phase 2 |
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