So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Fredholt, K.; Adrian, C.; Just, L.; Hoj Larsen, D.; Weng, S.; Moss, B.; Juel Friis, G. researched the compound: H-Leu-NH2.HCl( cas:10466-61-2 ).Product Details of 10466-61-2.They published the article 《Chemical and enzymic stability as well as transport properties of a Leu-enkephalin analog and ester prodrugs》 about this compound( cas:10466-61-2 ) in Journal of Controlled Release. Keywords: Leu enkephalin ester prodrug. We’ll tell you more about this compound (cas:10466-61-2).
The Leu-enkephalin analog (Tyr-d-Ala-Gly-Phe-Leu-NH2) was synthesized together with three esters prodrugs. The prodrugs synthesized were the O-acetyl, O-propionyl and O-pivaloyl esters of the tyrosine phenol group. The compounds were isolated with good purity (HPLC purity >99%) and in good yields (60-75%). The chem. and enzymic stability of the prodrugs has been investigated in detail. The prodrugs studied are quite chem. stable and the degradation of the prodrugs follows the pattern previously shown for similar esters (U-shaped pH-profile; maximal stability at pH 4-5). The prodrugs are degraded quant. in plasma to the parent peptide with half-lives in the range 2.9 min-2.6 h. Type B esterases were shown to be involved in the degradation as the half-lives increased in the presence of paraoxon. No significant stabilization was seen in 10% porcine gut homogenate. Half-lives in the same order were seen for the analog and the prodrugs in pure Leucine aminopeptidase solution The analog was stable in Carboxypeptidase A solution whereas a faster degradation of the prodrugs was seen in this media. Furthermore the transport properties of the compounds has been studied. A Papp value of 0.284×10-6 cm/s for the analog was obtained for the transport across Caco-2 cell monolayers in the BL-AP direction. The Papp values were increased by a factor of 2, 7 and 18 for the acetyl-, propionyl- and pivaloyl prodrug. The increase could be explained by higher lipophilicities of the prodrugs compared to the analog.
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