Identification | Back Directory | [Name]
HOE 140 | [CAS]
130308-48-4 | [Synonyms]
S-0765 HOE I40 HOE 140 H0E-140 JE-049) Icatibant Icatibant [inn] HOE 140 USP/EP/BP HOE 140 2ACOH 4H2O Icatibatide Acetate Icatibant
(HOE-140 [DES-ARG10] HOE 140 138614-30-9 (Acetate) RRP-(HYP)-G-(THI)-S-(D-TIC)-(OIC)-R D-Arg-[Hyp3,Thi5,D-Tic7,Oic8]bradykinin D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-D-Tic-Oic D-ARG-ARG-PRO-HYP-GLY-THI-SER-D-TIC-OIC-ARG D-ARGINYL-[HYP3,THI5,D-TIC7,OIC8]-BRADYKININ Des-Arg9-D-Arg[Hyp3,Thi5,D-Tic7,Oic8]bradykinin 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 D-ARG-ARG-PRO-HYP-GLY-THI-SER-D-TIC-OIC-ARG 2ACOH 4H2O D-ARGINYL-[HYP3,THI5,D-TIC7,OIC8]-BRADYKININ 2ACOH 4H2O D-Arg-L-Arg-L-Pro-L-t4Hyp-Gly-L-Thi-L-Ser-D-Tic-L-Oic-L-Arg-OH D-Arg-L-Arg-L-Pro-L-t4Hyp-Gly-3-(2-Thienyl)-L-Ala-L-Ser-D-Tic-[(3aS,7aS)-L-Oic-]-OH D-Arg-L-Arg-L-prolyl-L-Hyp-Gly-L-(2-thienyl)Ala-L-Ser-D-1,2,3,4-tetrahydro-3-isoquinolinecarbonyl-L-(2α,3β,7aβ)-octahydro-1H-indole-2-carboxylic acid D-ARGINYL-L-ARGINLYL-L-PROLYL-TRANS-4-HYDROXY-L-PROLYLGLYCYL-3-(2-THIENYL)-L-ALANYL-L-SERYL-D-1,2,3,4-TETRAHYDRO-3-ISOQUINOLINECARBONYL-L-(2ALPHA, 3BETA, 7ABETA)-OCTAHYDRO-1H-INDOLE-2-CARBONYL L-Arginine, D-arginyl-L-arginyl-L-prolyl-(4R)-4-hydroxy-L-prolylglycyl-3-(2-thienyl)-L-alanyl-L-seryl-(3R)-1,2,3,4-tetrahydro-3-isoquinolinecarbonyl-(2S,3aS,7aS)-octahydro-1H-indole-2-carbonyl- D-ARGINYL-L-ARGINLYL-L-PROLYL-TRANS-4-HYDROXY-L-PROLYLGLYCYL-3-(2-THIENYL)-L-ALANYL-L-SERYL-D-1,2,3,4-TETRAHYDRO-3-ISOQUINOLINECARBONYL-L-(2ALPHA,3BETA,7A-BETA)-OCTAHYDRO-1H-INDOLE-2-CARBONYL-L-ARGININE L-Arginine, D-arginyl-L-arginyl-L-prolyl-trans-4-hydroxy-L-prolylglycyl-3-(2-thienyl)-L-alanyl-L-seryl-D-1,2,3,4-tetrahydro-3-isoquinolinecarbonyl-L-(2alpha,3abeta,7abeta)-octahydro-1H-indole-2-carbonyl- Nw-(((S)-2-(2-((2S,4R)-1-(D-arginyl-L-arginyl-L-prolyl)-4-hydroxypyrrolidine-2-carboxamido)acetamido)-3-(thiophen-2-yl)propanoyl)-L-seryl)-N2-((3aS,7aS)-octahydro-1H-indole-2-carbonyl)-N2-((R)-1,2,3,4-tetrahydroisoquinoline-3-carbonyl)-L-arginine | [Molecular Formula]
C59H89N19O13S | [MDL Number]
MFCD00213940 | [MOL File]
130308-48-4.mol | [Molecular Weight]
1304.52 |
Chemical Properties | Back Directory | [density ]
1.60±0.1 g/cm3(Predicted) | [storage temp. ]
−20°C
| [solubility ]
Water:100.0(Max Conc. mg/mL);76.66(Max Conc. mM) | [form ]
powder
| [pka]
3.60±0.21(Predicted) | [color ]
white
| [Water Solubility ]
Soluble to 1 mg/ml in water | [Sequence]
H-D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-D-Tic-Oic-Arg-OH | [InChIKey]
QASONHYHOCRAHL-DOMVFXHKSA-N | [CAS DataBase Reference]
130308-48-4 |
Hazard Information | Back Directory | [Description]
Hoe 140 (D-Arg-[Hyp3, Thi5, D-Tic7, Oic8]-bradykinin), on bradykinin- and platelet-activating factor (PAF)-induced bronchoconstriction and airway microvascular leakage in anesthetized guinea pigs. Hoe 140 is highly potent and long-acting in inhibiting BK-induced hypotensive responses in the rat. Four hours after s.c. administration of 20nmol kg-1, inhibition still amounted to 60% whereas the effect of 200nmol kg-1 of d-Arg-[Hyp2, Thi5,8, d-Phe7]BK was not significant[1-2].
| [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. | [Brand name]
Metastat (CollaGenex). | [Biological Activity]
A potent and selective bradykinin B2 antagonist. HOE-140 is a useful tool for discrimination of the physiological roles of bradykinin B2 versus B1 receptors. Displays a protective effect in myocardial reperfusion injury. | [storage]
Store at -20°C | [References]
[1] K. Wirth. “Hoe 140 a new potent and long acting bradykinin-antagonist: in vivo studies.” British Journal of Pharmacology 102 3 (1991): 774–777. [2] T Sakamoto. “Effect of Hoe 140, a new bradykinin receptor antagonist, on bradykinin- and platelet-activating factor-induced bronchoconstriction and airway microvascular leakage in guinea pig.” European journal of pharmacology 213 3 (1992): 367–73.
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