53195-68-9

Upstream product

• 2389-46-0 N-α-tert-butyloxycarbonyl-N-ε-benzyloxycarbonyl-lysine p-nitrophenyl ester 
• 2133-40-6 L-proline methyl ester monohydrochloride 
• 42460-90-2 (S)-Pyrrolidine-2-carboxylic acid methyl ester; compound with trifluoro-acetic acid 
• 84890-96-0 C₂₄H₃₆N₂O₈ 
• 1155-64-2 N₆-[(benzyloxy)carbonyl]-L-lysine 
• 2389-45-9 Boc-Lys(Z)-OH 
• 543-27-1 isobutyl chloroformate 
• 2133-40-6 methyl pyrrolidine-2-carboxylate hydrochloride 
• 56-87-1 L-lysine 
• 1070-19-5 N-(tert-butyloxycarbonyl) azide 
• 2577-48-2 methyl (2S)-pyrrolidine carboxylate 

Downstream Products

• 78314-58-6 Boc-Pro-Lys(Z)-Pro-OCH₃ 
• 78314-62-2 Z₃-Arg-Pro-Lys(Z)-Pro-OH 
• 78314-59-7 Z₃Arg-Pro-Lys(Z)-Pro-OMe 
• 1220668-97-2 Boc-Ile-Lys(Cbz)-Pro-OMe 
• 126733-91-3 Boc-Arg(NO₂)-Pro-Lys(Z)-Pro-Gln-OCH₂Ph 

Relevant academic research and scientific papers

Cyclodipeptide c(Orn-Pro) Conjugate with 4-Ethylpiperic Acid Abrogates Cancer Cell Metastasis through Modulating MDM2

The present work describes the synthesis, characterization, and anticancer properties of c(Lys-Pro), P1; c(Orn-Pro), P2; and conjugates PA-c(Lys-Pro), C1; PA-c(Orn-Pro), C2; EPA-c(Lys-Pro), C3; and EPA-c(Orn-Pro), C4. Among all, conjugate C4 displays pote

Use of Molecular Modeling to Design Selective NTS2 Neurotensin Analogues

Neurotensin exerts potent analgesia by acting at both NTS1 and NTS2 receptors, whereas NTS1 activation also results in other physiological effects such as hypotension and hypothermia. Here, we used molecular modeling approach to design highly selective NT

Stereoselective Synthesis of β-(5-Arylthiazolyl) α-Amino Acids and Use in Neurotensin Analogues

A series of new unnatural amino acids bearing a β-arylthiazole side chain was synthesized by exploiting a diastereoselective alkylation starting from glycine tert-butyl ester Schiff base with hydroxypinanone as the chiral inducer. This strategy afforded β-arylthiazole alanines in good chemical yields and with 98 % ee. Due to their aromatic properties, these newly generated amino acids were used to prepare neurotensin (NT)[8-13] analogues by serving as replacements for the native Tyr11 residue. Incorporation of the (L)-(+)-(β-phenylthiazol-4-yl)alanine residue at NT[8-13] position 11 improved plasma stability and selectivity towards NTS1, while also preserving native receptor binding affinity and biological activity. New β-arylthiazole alanines were synthesized in good chemical yields and with 98 % ee using a diastereoselective alkylation; these alanine derivatives were then used as Tyr11 replacements in the construction of neurotensin (NT)[8-13] analogues. The new NT analogues showed improved plasma stability and selectivity towards NTS1 thus preserving the hypotensive properties of the native peptide.

Solvent-free peptide synthesis assisted by microwave irradiation: Environmentally benign synthesis of bioactive peptides

An efficient and facile, solvent-free peptide synthesis assisted by microwave irradiation, using DIC/HONB as the coupling reagent combination is reported. Key features of this original protocol are solvent-free synthesis, very short reaction time and scal

NOVEL SMALL MOLECULE DNAK INHIBITORS

Methods of inhibiting HSP70 proteins, agents causing the inhibition of HSP70 proteins, and the effects of such inhibition on cell proliferation. Anti-microbial agents comprising small molecules, or pharmaceutical salts thereof, disclosed herein and furthe

Synthesis of new substance P analogues releasing histamine from rat peritoneal mast cells

New analogues of the N-terminal fragment of substance P [Arg-Pro-Lys-Pro, SP(1-4)] were synthesized and their activities on histamine release from rat peritoneal mast cells were compared. The potency of these compounds decreases in the following order (in abbreviation): SP(1-4)C12 > C'12-SP(1-4)-OCH3 > C'12-SP(1-4)-OH, H-Lys-Pro-C12 and SP. Benzalkonium chloride, a competitive antagonist of peptide-induced histamine release from rat mast cells, inhibits the effect of SP and SP analogues with IC50 in the range of micromolar concentrations. SP(1-4)-C12 and C'12-SP(1-4)-OCH3 have been found to be 10-fold more active than SP on the GTPase activity of purified G proteins (G(o)/G(i)). The lack of clear structural relationships for agonist activities supports a receptor-less mechanism for histamine release by SP and its analogs. This effect could be elicited by a direct stimulation of G proteins.

A Thermodynamic and Spectroscopic Study of the Complexes of the Undecapeptide Substance P, of its N-Terminal Fragment and of Model Pentapeptides Containing Two Prolyl Residues with Copper Ions

Eight pentapeptides have been synthesised which either are models of the N-terminal pentapeptide fragment of Substance P (Arg-Pro-Lys-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met-NH2) or assist in understanding its co-ordinating ability; Gly-Pro-Gly-Pro-Gly, Gly-Pro-G

PROLINE DERIVATIVES

Proline derivatives of the formulae: STR1 wherein R 1 through R 11 have defined values, and acid-and base-addition salts thereof, and equilibrium addition compounds of the aldehyde group thereof; processes for their preparation; pharmaceutical compositions; and intermediates for preparing said proline derivatives. The proline derivatives are human leukocyte elastase inhibitors which are useful, for example, in treating pulmonary emphysema.

Le chloroformiate d'isopropenyle (IPCF) en chimie des peptides. I. Un bon reactif pour le couplage peptidique : synthese de dipeptides modeles

Isopropenyl chloroformate was used as an activating agent of N-protected amino-acids in the mixed anhydride method.This new reagent allows to run mixed anhydrides couplings at room temperature.

Intramolecular Transfer of Excitation Energy, Complexation with Metal Ions, and Interactions with Liposomes of Cycloε-dansyllysyl-prolyl>

A cyclic pentapeptide containing an energy donor group and an energy acceptor group within the molecule, cyclo, was synthesized.Its conformation, complexation with metal ions, intramolecular energy transfer, and interaction with