130308-48-4

Basic information

• Product Name: HOE 140
• Synonyms: RRP-(HYP)-G-(THI)-S-(D-TIC)-(OIC)-R;H-D-ARG-ARG-PRO-HYP-GLY-THI-SER-D-TIC-OIC-ARG-OH;H2N-D-ARG-ARG-PRO-HYP-GLY-THI-SER-D-TIC-OIC-ARG-OH;HOE 140;HOE 140 2ACOH 4H2O;D-ARG-ARG-PRO-HYP-GLY-THI-SER-D-TIC-OIC-ARG;D-ARG-ARG-PRO-HYP-GLY-THI-SER-D-TIC-OIC-ARG 2ACOH 4H2O;D-ARGINYL-[HYP3,THI5,D-TIC7,OIC8]-BRADYKININ
• CAS NO: 130308-48-4
• Molecular Formula: C59H89N19O13S
• Molecular Weight: 1304.52
• Product Categories: peptide
• Mol File: 130308-48-4.mol
• Article Data: 5

Chemical Properties

• Appearance: white/powder
• Density: 1.6 g/cm³
• Refractive Index: 1.742
• Storage Temp.: −20°C
• PKA: 3.60±0.21(Predicted)
• CAS DataBase Reference: HOE 140(CAS DataBase Reference)
• NIST Chemistry Reference: HOE 140(130308-48-4)
• EPA Substance Registry System: HOE 140(130308-48-4)

Safety Data

• WGK Germany: 3
• Hazardous Substances Data: 130308-48-4(Hazardous Substances Data)

Usage

Uses

Antagonist (bradykinin).

Definition

ChEBI: A ten-membered synthetic oligopeptide consisting of D-Arg, Arg, Pro, Hyp, Gly, Thi, Ser, D-Tic, Oic, and Arg residues joined in sequrence. A bradykinin receptor antagonist used as its acetate salt for the treatment of acut attacks of hereditary angioedema in adult patients.

InChI:InChI=1/C59H89N19O13S/c60-37(14-5-19-67-57(61)62)48(82)72-38(15-6-20-68-58(63)64)52(86)75-22-8-18-43(75)54(88)77-30-35(80)26-44(77)50(84)70-28-47(81)71-40(27-36-13-9-23-92-36)49(83)74-41(31-79)53(87)76-29-34-12-2-1-10-32(34)24-46(76)55(89)78-42-17-4-3-11-33(42)25-45(78)51(85)73-39(56(90)91)16-7-21-69-59(65)66/h1-2,9-10,12-13,23,33,35,37-46,79-80H,3-8,11,14-22,24-31,60H2,(H,70,84)(H,71,81)(H,72,82)(H,73,85)(H,74,83)(H,90,91)(H4,61,62,67)(H4,63,64,68)(H4,65,66,69)/t33-,35+,37+,38?,39-,40-,41-,42-,43?,44?,45?,46?/m0/s1

Upstream product

• 71989-33-8 Fmoc-Ser(tBu)-OH 
• 130309-33-0 N-Fmoc-D-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid 
• 130309-37-4 1‐fluorenylmethoxycarbonyl-(2S,3aS,7aS)‐octahydroindole‐2‐carboxylic acid 
• 130309-35-2 Fmoc-β-(2-thienyl)-L-alanine 
• 187618-60-6 Nα-(9-fluorenylmethyloxycarbonyl)-Nγ-2,2,4,6,7-pentamethyldihydrobenzofuran-5-sulfonyl-L-arginine 
• 29022-11-5 N-(fluoren-9-ylmethoxycarbonyl)glycine 
• 71989-31-6 Fmoc-Pro-OH 
• 268729-12-0 (2S,4R)-4-tert-butoxy-1-(9H-fluoren-9-ylmethoxycarbonyl)pyrrolidine-2-carboxylic acid 
• 187618-60-6 N-α-[(9H-fluoren-9-ylmethoxy)carbonyl]-N^G-(2,2,4,6,7-pentamethyldihydrobenzofuran-5-sulfonyl)-D-arginine 

Relevant articles and documents

A METHOD FOR PRODUCTION OF HIGH PURITY ICATIBANT

The present invention provides a process for the manufacture of peptidomimetic drug icatibant with high yield and purity by fragment condensation on the solid phase. In particular, it describes a convergent synthesis by condensation of a protected C-terminal fragment bound to a solid support and a protected N-terminal fragment, followed by cleavage from the support and resulting in a crude peptide of high purity, which is further purified to obtain pure icatibant in high yield. The invention further provides intermediates useful in the manufacturing process.

Use of bradykinin antagonists for the production of pharmaceuticals for the treatment of chronic fibrogenetic liver disorders and acute liver disorders

This invention relates to a method of treating a chronic fibrogenetic liver disorder and/or an acute liver disorder and/or complications associated therewith, comprising administering to a patient a therapeutically effective amount of a bradykinin antagonist. Particular complications associated with said liver disorders include portal hypertension, decompensation phenomena such as ascites, edema formation, hepatorenal syndrome, hypertensive gastropathy and colopathy, splenomegaly and hemorrhagic complications in the gastrointestinal tract due to portal hypertension, collateral circulation and hyperemia and a cardiopathy as a result of a chronically hyperdynamic circulatory situation and its consequences.

Cytolytic bradykinin antagonists

The present invention provides bradykinin antagonists effective to inhibit cancer cell growth. Also provided are methods of inhibiting lung cancer cell growth by administering a therapeutically effective amount of a dimerized bradykinin antagonist.