1. GPCR/G Protein
    Neuronal Signaling
  2. Adrenergic Receptor
  3. (S)-Timolol Maleate

(S)-Timolol Maleate (Synonyms: L-714,465 Maleate; MK 950)

Cat. No.: HY-17380 Purity: 99.85%
Handling Instructions

(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.

For research use only. We do not sell to patients.

(S)-Timolol Maleate Chemical Structure

(S)-Timolol Maleate Chemical Structure

CAS No. : 26921-17-5

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10 mM * 1 mL in DMSO USD 70 In-stock
Estimated Time of Arrival: December 31
100 mg USD 64 In-stock
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200 mg USD 102 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

(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[1][2][3].

IC50 & Target

Ki: 1.97 nM (β1-adrenoceptor); 2.0 nM (β2-adrenoceptor)

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[1].

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[1].

Molecular Weight

432.49

Formula

C₁₇H₂₈N₄O₇S

CAS No.

26921-17-5

SMILES

O[[email protected]](COC1=NSN=C1N2CCOCC2)CNC(C)(C)C.O=C(O)/C=C\C(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (231.22 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.78 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.78 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.78 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

(S)-TimololL-714,465MK 950MK950MK-950Adrenergic ReceptorBeta ReceptorNon-cardioselectivehydrophilicβ-adrenoceptorintraocularpressureglaucomahypertensionanginapectorismyocardialinfarctionInhibitorinhibitorinhibit

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Product Name:
(S)-Timolol Maleate
Cat. No.:
HY-17380
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