Day: November 28, 2022

Modulating Oxytocin Activity and Plasma Stability by Disulfide Bond Engineering was written by Muttenthaler, Markus;Andersson, Asa;de Araujo, Aline D.;Dekan, Zoltan;Lewis, Richard J.;Alewood, Paul F.. And the article was included in Journal of Medicinal Chemistry in 2010.Recommanded Product: 156311-83-0 The following contents are mentioned in the article:

Disulfide bond engineering is an important approach to improve the metabolic half-life of cysteine-containing peptides. Eleven analogs of oxytocin were synthesized including disulfide bond replacements by thioether, selenylsulfide, diselenide, and ditelluride bridges, and their stabilities in human plasma and activity at the human oxytocin receptor were assessed. The cystathionine (K_i = 1.5 nM, and EC₅₀ = 32 nM), selenylsulfide (K_i = 0.29/0.72 nM, and EC₅₀ = 2.6/154 nM), diselenide (K_i = 11.8 nM, and EC₅₀ = 18 nM), and ditelluride analogs (K_i = 7.6 nM, and EC₅₀ = 27.3 nM) retained considerable affinity and functional potency as compared to oxytocin (K_i = 0.79 nM, and EC₅₀ = 15 nM), while shortening the disulfide bridge abolished binding and functional activity. The mimetics showed a 1.5-3-fold enhancement of plasma stability as compared to oxytocin (t_1/2 = 12 h). By contrast, the all-D-oxytocin and head to tail cyclic oxytocin analogs, while significantly more stable with half-lives greater than 48 h, had little or no detectable binding or functional activity. This study involved multiple reactions and reactants, such as ((3H-[1,2,3]Triazolo[4,5-b]pyridin-3-yl)oxy)tri(pyrrolidin-1-yl)phosphonium hexafluorophosphate(V) (cas: 156311-83-0Recommanded Product: 156311-83-0).

((3H-[1,2,3]Triazolo[4,5-b]pyridin-3-yl)oxy)tri(pyrrolidin-1-yl)phosphonium hexafluorophosphate(V) (cas: 156311-83-0) belongs to triazole derivatives. Triazoles exhibit substantial isomerism, depending on the positioning of the nitrogen atoms within the ring. The presence of the three nitrogen atoms in triazole structures afforded opportunities for a plethora of structural modification with the generation of novel therapeutically potential agents, which is different from other heterocyclic compounds.Recommanded Product: 156311-83-0

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Microparticle Matrix Encoding of Beads was written by Meldal, Morten;Christensen, Soeren Flygering. And the article was included in Angewandte Chemie, International Edition in 2010.Application In Synthesis of ((3H-[1,2,3]Triazolo[4,5-b]pyridin-3-yl)oxy)tri(pyrrolidin-1-yl)phosphonium hexafluorophosphate(V) The following contents are mentioned in the article:

The authors present a versatile, simple encoding principle that may solve many problems in solid-phase screening and decoding: optical microparticle matrix encoding (MPM encoding) with fluorescent microparticles. The utility of this technique has been demonstrated in the identification of avidin ligands from a focused library, in which compounds could not be distinguished with mass spectrometric methods. The library design was based upon previously reported L– and D-amino acid libraries for avidin and streptavidin, thus indicating selectivity for aromatic residues. Uniform 10 μm Tentagel microparticles labeled with a chem. stable fluorophore ATOTA [tris(dialkylamino)trioxatriangulenium ion] were randomly distributed in a bis(acrylamido)polyethylene glycol (PEG) macromonomer (64,000 cm^-3) by ultrasound and homogenization. Inverse suspension polymerization of the microparticle-containing macromonomer in the presence of bis(tert-butyldiphenylmethylsilyl)PEG1500 stabilizer provided 500,000 uniform, amino-functionalized, uniquely encoded beads (72 mL; ca 6.5 g dry weight), which contained an average of 8 microparticles per bead, with a bead size of (550±100) μm. This study involved multiple reactions and reactants, such as ((3H-[1,2,3]Triazolo[4,5-b]pyridin-3-yl)oxy)tri(pyrrolidin-1-yl)phosphonium hexafluorophosphate(V) (cas: 156311-83-0Application In Synthesis of ((3H-[1,2,3]Triazolo[4,5-b]pyridin-3-yl)oxy)tri(pyrrolidin-1-yl)phosphonium hexafluorophosphate(V)).

((3H-[1,2,3]Triazolo[4,5-b]pyridin-3-yl)oxy)tri(pyrrolidin-1-yl)phosphonium hexafluorophosphate(V) (cas: 156311-83-0) belongs to triazole derivatives. Triazoles are important five-member nitrogen heterocycles involved in a wide range of industrial applications such as agrochemicals, corrosion inhibitors, dyes, optical brighteners, as well as biologically active agents. 1,2,3-Triazoles are usually prepared following (3+2) cycloaddition protocols. A common technique for unsubstituted triazoles is the Huisgen azide-alkyne 1,3-dipolar cycloaddition: a azide and an alkyne react at high temperature to form a ring. However, the Huisgen strategy produces a mixture of isomers (typically 1,4- and 1,5-disubstituted) when used to produce substituted triazoles.Application In Synthesis of ((3H-[1,2,3]Triazolo[4,5-b]pyridin-3-yl)oxy)tri(pyrrolidin-1-yl)phosphonium hexafluorophosphate(V)

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics