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Diphenylcyclohexane Derivatives for Optimization of Pharmacokinetics in Blood
Ethyl 6-[(2-cyanoethoxy)(4,4-diphenylcyclohexyloxy)phosphoryloxy]hexanoate (1) is utilized for the improvement of peptide half-life in vivo.1) According to Zobel’s report, it is found that a peptide modified with 1 has about 50-fold longer half-life time in plasma compared to a non-modified peptide. This idea is based on the notion that diphenylcyclohexyl phosphate moiety of 1 has high affinity to serum albumin.2) Furthermore, ethyl 2-[(2-cyanoethoxy)(4,4-diphenylcyclohexyloxy)phosphoryloxy]acetate (2), whose alkyl chain length is different from 1, is also available as a building block to introduce similar moiety in order to improve pharmacokinetics of peptides in blood.
Related Products
- E1313
- Ethyl 6-[(2-Cyanoethoxy)(4,4-diphenylcyclohexyloxy)phosphoryloxy]hexanoate
- E1268
- Ethyl 2-[(2-Cyanoethoxy)(4,4-diphenylcyclohexyloxy)phosphoryloxy]acetate
References
- 1)Phosphate Ester Serum Albumin Affinity Tags Greatly Improve Peptide Half-Life In Vivo
- 2)MS-325: albumin-targeted contrast agent for MR angiography.