HOE 140 TFA structure
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Common Name | HOE 140 TFA | ||
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CAS Number | 130308-48-4 | Molecular Weight | 1304.522 | |
Density | 1.6±0.1 g/cm3 | Boiling Point | N/A | |
Molecular Formula | C59H89N19O13S | Melting Point | N/A | |
MSDS | N/A | Flash Point | N/A |
Use of HOE 140 TFAIcatibant(HOE-140) is a selective and specific antagonist of bradykinin B2 receptor with IC50 and Ki of 1.07 nM and 0.798 nM respectively.IC50 value: 1.07 nM [1]Target: bradykinin B2 receptor antgonistin vitro: In receptor binding studies in guinea-pig ileum preparations, Hoe 140 showed an IC50 of 1.07 x 10(-9) mol l-1 and a KI value of 7.98 x 10(-10) mol l-1. In isolated organ preparations Hoe 140 and D-Arg-[Hyp2,Thi5,8, D-Phe7]BK inhibited bradykinin-induced contractions concentration dependently, with IC50-values in the guinea-pig ileum preparation of 1.1 x 10(-8) mol l-1 and 3 x 10(-5) mol l-1, respectively. pA2 values in this tissue were 8.42 and 6.18, respectively [1].in vivo: HOE 140 (1, 3, or 10 μg/10 μl physiological saline) was administered into the wound by a sterile micropipette. HOE 140 (1, 3, 10 μg) significantly relieved mechanical allodynia and guarding in comparison with vehicle-treated group [2]. HOE-140 (10 nmol/kg) protected against memory impairment. This treatment attenuated the brain edema, interleukin-1β, tumor necrosis factor-α, and nitric oxide metabolites content elicited by mLFPI. Accordingly, HOE-140 administration protected against the increase of nicotinamide adenine dinucleotide phosphate oxidase activity, thiobarbituric-acid-reactive species, protein carbonylation generation, and Na+ K+ ATPase inhibition induced by trauma [3]. |
Name | icatibant |
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Synonym | More Synonyms |
Description | Icatibant(HOE-140) is a selective and specific antagonist of bradykinin B2 receptor with IC50 and Ki of 1.07 nM and 0.798 nM respectively.IC50 value: 1.07 nM [1]Target: bradykinin B2 receptor antgonistin vitro: In receptor binding studies in guinea-pig ileum preparations, Hoe 140 showed an IC50 of 1.07 x 10(-9) mol l-1 and a KI value of 7.98 x 10(-10) mol l-1. In isolated organ preparations Hoe 140 and D-Arg-[Hyp2,Thi5,8, D-Phe7]BK inhibited bradykinin-induced contractions concentration dependently, with IC50-values in the guinea-pig ileum preparation of 1.1 x 10(-8) mol l-1 and 3 x 10(-5) mol l-1, respectively. pA2 values in this tissue were 8.42 and 6.18, respectively [1].in vivo: HOE 140 (1, 3, or 10 μg/10 μl physiological saline) was administered into the wound by a sterile micropipette. HOE 140 (1, 3, 10 μg) significantly relieved mechanical allodynia and guarding in comparison with vehicle-treated group [2]. HOE-140 (10 nmol/kg) protected against memory impairment. This treatment attenuated the brain edema, interleukin-1β, tumor necrosis factor-α, and nitric oxide metabolites content elicited by mLFPI. Accordingly, HOE-140 administration protected against the increase of nicotinamide adenine dinucleotide phosphate oxidase activity, thiobarbituric-acid-reactive species, protein carbonylation generation, and Na+ K+ ATPase inhibition induced by trauma [3]. |
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Related Catalog | |
References |
Density | 1.6±0.1 g/cm3 |
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Molecular Formula | C59H89N19O13S |
Molecular Weight | 1304.522 |
Exact Mass | 1303.660767 |
PSA | 544.46000 |
LogP | -2.63 |
Index of Refraction | 1.742 |
Storage condition | −20°C |
WGK Germany | 3 |
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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-(2a,3ab,7ab)-octahydro-1H-indole-2-carbonyl-L-arginine |
(2S)-2-({[(3aS,7aS)-1-({(3R)-2-[(2S)-2-{[(2S)-2-{[({[(2S,4R)-1-({(2S)-1-[(2S)-2-{[(2R)-2-Amino-5-carbamimidamidopentanoyl]amino}-5-carbamimidamidopentanoyl]pyrrolidin-2-yl}carbonyl)-4-hydroxypyrrolidin-2-yl]carbonyl}amino)acetyl]amino}-3-(2-thienyl)propanoyl]amino}-3-hydroxypropanoyl]-1,2,3,4-tetrahydroisoquinolin-3-yl}carbonyl)octahydro-1H-indol-2-yl]carbonyl}amino)-5-carbamimidamidopentanoic acid (non-preferred name) |
H0E-140 |
HOE I40 |
(2S)-2-({[(3aS,7aS)-1-({(3R)-2-[(2S)-2-{[(2S)-2-{[({[(2S,4R)-1-({(2S)-1-[(2S)-2-{[(2R)-2-Amino-5-carbamimidamidopentanoyl]amino}-5-carbamimidamidopentanoyl]-2-pyrrolidinyl}carbonyl)-4-hydroxy-2-pyrrolidinyl]carbonyl}amino)acetyl]amino}-3-(2-thienyl)propanoyl]amino}-3-hydroxypropanoyl]-1,2,3,4-tetrahydro-3-isoquinolinyl}carbonyl)octahydro-1H-indol-2-yl]carbonyl}amino)-5-carbamimidamidopentanoic acid |
Icatibant |