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Butyryltimolol

Cat. No. M27734
Butyryltimolol Structure
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Quality Control & Documentation
Biological Activity

Butyryltimolol is the active precursor compound of Timolol, and is also a β-adrenergic (β-AR) blocker, which can pass through the cornea of the eye, and is enzymatically hydrolyzed to produce Timolol after entering the eye.

Chemical Information
Molecular Weight 386.51
Formula C17H30N4O4S
CAS Number 106351-79-5
Form Liquid
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Shih-Jen Chang, et al. Pharmaceutics. Evaluation of Transdermal Transport and Concurrent Cutaneous Hydrolysis of Timolol Prodrυg for the Treatment of Infantile Hemangiomas

[2] S C Chang, et al. Invest Ophthalmol Vis Sci. Low dose O-butyryl timolol improves the therapeutic index of timolol in the pigmented rabbit

[3] S C Chang, et al. Exp Eye Res. Relative effectiveness of prodrυg and viscous solution approaches in maximizing the ratio of ocular to systemic absorption of topically applied timolol

[4] D S Chien, et al. J Ocul Pharmacol. Influence of corneal epithelial integrity on the penetration of timolol prodrυgs

[5] D E Potter, et al. Curr Eye Res. Ocular and cardiac beta-antagonism by timolol prodrυgs, timolol and levobunolol

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