Timolol (maleate)

Timolol is a non-selective beta-adrenergic receptor antagonist with log Kd values of -8.27, -9.86, and -6.8 for binding to human beta1-, beta2-, and beta3-adrenoceptors, respectively. It has been reported that only the (S) enantiomer contributes to the beta-blocking effects of racemic timolol, but the weakly active (R) isomer maintains a beneficial effect on intraocular pressure without the undesirable side-effect of bronchial constriction caused by non-selective action of (S)-timolol on beta1 and beta2 receptors. Timolol has been use alone and in fixed combinations with either prostaglandin analogs or carbonic anhydrase inhibitors to reduce intraocular pressure in research models of ocular hypertension and glaucoma.Formal Name: (2S)-1-[(1,1-dimethylethyl)amino]-3-[[4-(4-morpholinyl)-1,2,5-thiadiazol-3-yl]oxy]-2-propanol, 2Z-butenedioate. CAS Number: 26921-17-5. Synonyms: MK-950, (S)-Timolol (maleate), WP934. Molecular Formula: C13H24N4O3S . C4H4O4. Formula Weight: 432.5. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 16 mg/ml, Ethanol: 0.2 mg/ml, PBS (pH 7.2): 5 mg/ml. lambdamax: 209, 296 nm. SMILES: CC(C)(C)NC[C@H](O)COC1=NSN=C1N2CCOCC2.OC(/C=C\C(O)=O)=O. 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. InChi Key: WLRMANUAADYWEA-NWASOUNVSA-N.