212716-36-4

Upstream product

• 108695-16-5 Boc-N-Me-Arg(Tos)-OH 
• 175216-23-6 N¹-benzyloxycarbonyl-N⁸-D-leucyl-1,8-octanediamine 
• 175216-22-5 N¹-benzyloxycarbonyl-N⁸-(t-butoxycarbonyl-D-leucyl)-1,8-octanediamine 
• 16937-99-8 N-Boc-D-Leu 

Downstream Products

• 205874-66-4 N¹-benzyloxycarbonyl-N⁸-(N^α-methyl-N^g-tosylarginyl-D-leucyl)-1,8-octanediamine 
• 205874-67-5 N¹-benzyloxycarbonyl-N⁸-(N^α-t-butoxycarbonyl-N^g-tosylarginyl-N^α-methyl-N^g-tosylarginyl-D-leucyl)-1,8-octanediamine 
• 212716-37-5 N¹-(4-nitrobenzo-6-oxa-5,7-diazolyl)-N⁸-(N^α-t-butoxycarbonyl-N^g-tosylarginyl-N^g-tosyl-N^α-methylarginyl-D-leucyl)-1,8-octanediamine 

Relevant academic research and scientific papers

Intestinal absorption of fluorescence-derivatized cationic peptide 001-C8-NBD via adsorptive-mediated transcytosis

The intestinal absorption of an intact oligopeptide was investigated in rats using a synthetic cationic peptide, 001-C8 (H-MeTyr-Arg-MeArg-d-Leu-NH(CH2)8NH2). The peptide was coupled with 4-nitrobenzo-2-oxa-1,3-diazole (NBD) to prepare a fluorescence-labeled derivative 001-C8-NBD (H-MeTyr-Arg-MeArg-d-Leu-NH(CH2)8NH-NBD) for the purpose of quantification. The degradation half-life of 001-C8-NBD in jejunal homogenate (1mg/mL) was 99.5min, which was significantly longer than that of natural leucine enkephalin (1.14min). The absorption of 001-C8-NBD was evaluated by the vascular-perfusion method. Intact 001-C8-NBD appeared in the blood time-dependently and the absorption volume at 30min (2.75 ± 0.14μL/cm intestine) was significantly larger than that of [3H]PEG 900 (0.88 ± 0.13μL/cm intestine), of which membrane permeability is very low. The absorption of 001-C8-NBD was greatly reduced by an adsorptive-mediated endocytosis inhibitor, protamine (10mM). No inhibition of the absorption of [3H]PEG 900 by protamine was observed. The intestinal absorption was also measured by an in vivo loop method. The absorption clearance of 001-C8-NBD measured by this method (0.083 ± 0.008μL/min/cm intestine) was comparable to that obtained by the vascular perfusion method (0.092 ± 0.005μL/min/cm intestine). All of these data suggested that 001-C8-NBD was absorbed as the intact oligopeptide in the intestine in vivo. Adsorptive-mediated transcytosis is suggested to have enormous potential as an oral delivery system for peptide and/or protein drugs. Copyright (C) 1998 Elsevier Science Ltd.