127373-66-4
127373-66-4 structure
- Name: Sivelestat sodium salt hydrate
- Chemical Name: 2-[[2-[[4-(2,2-dimethylpropanoyloxy)phenyl]sulfonylamino]benzoyl]amino]acetic acid
- CAS Number: 127373-66-4
- Molecular Formula: C20H22N2O7S
- Molecular Weight: 434.463
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Elastase
- Create Date: 2018-02-12 08:00:00
- Modify Date: 2026-07-01 16:19:26
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Sivelestat(ONO5046; LY544349; EI546) is a competitive inhibitor of human neutrophil elastase(IC50 = 44 nM; Ki=200 nM); also inhibited leukocyte elastase obtained from rabbit, rat, hamster and mouse.IC50 value: 44 nM [1]Target: neutrophil elastaseONO-5046 did not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G even at 100 microM. In in vivo studies, ONO-5046 suppressed lung hemorrhage in hamster (ID50 = 82 micrograms/kg) by intratracheal administration and increase of skin capillary permeability in guinea pig (ID50 = 9.6 mg/kg) by intravenous administration, both of which were induced by human neutrophil elastase [1]. Sivelestat sodium hydrate is an anti-neutrophil elastase inhibitor and may be one of the treatment options for acute respiratory failure due to pneumocystis pneumonia in AIDS patients [2].
| Name | 2-[[2-[[4-(2,2-dimethylpropanoyloxy)phenyl]sulfonylamino]benzoyl]amino]acetic acid |
|---|---|
| Synonyms |
2-[[2-[(4-pivaloyloxyphenyl)sulfonylamino]benzoyl]amino]acetic acid
Sivelestat sodium Impurity Sivelestat(anhydrous, free acid) n-(2-(((4-(2,2-dimethyl-1-oxopropoxy)phenyl)sulfonyl)amino)benzoyl)glycine Elastase Inhibitor IV Sivelestat-d9 Sivelestat, 10 mM in DMSO 2-{[2-({4-[(2,2-diMethylpropanoyl)oxy]benzene}sulfonaMido)phenyl]forMaMido}acetic acid Glycine, N-[2-[[[4-(2,2-diMethyl-1-oxopropoxy)phenyl]sulfonyl]amino]benzoyl] sivelestat Ono-5046 sodium salt hydrate Propanoic acid, 2,2-dimethyl-, 4-[[[2-[[(carboxymethyl)amino]carbonyl]phenyl]amino]sulfonyl]phenyl ester Sivelestat-d4 Propanoic acid, 2,2-dimethyl-, 4-[[[2-[[(cboxymethyl)amino]carbonyl]phenyl]amino]sulfonyl]phenyl ester N-[2[[[4-(2,2-Dimethylpropanoyl)oxy]phenyl]sulfonyl)amino]benzoyl]glycine Sivelestat, neutrophil elastase inhibitor LY 544349 sodium salt hydrate Sivelestate Severus N-(2-(((4-(2,2-Dimethyl-1-oxopropoxy)phenyl)sulfonyl)amino)benzoyl)glycine o-(p-Hydroxybenzenesulfonamido)hippuric Acid Pivalate (Ester) Sivelestat Sivelestat (ONO-5046) EI 546 o-(p-Hydroxybenzenesulfonamido)hippuric acid, pivalate (ester) sodium salt hydrate EI 546 sodium salt hydrate 2-[[2-[[4-(2,2-dimethylpropanoyloxy)phenyl]sulfonylamino]benzoyl]amino]aceticaci 2-[[2-[[4-(2,2-dimethylpropanoyloxy)phenyl]sulfonylamino]phenyl]cbonylamino]ethanoic acid EI-546;LY-544349;ONO-5046 Sivelestat RS Elastase Inhibitor IV - - Calbiochem Sivelestat SodiuM anhydrous, free acid Sivelestate sodium ONO5046 SIVELESTAT(ONO5046; LY544349; EI546) Elaspol sodium salt hydrate N-[2-{N'-(cboxy-methyl-)-amino-carbonyl-}-phenyl-]-4-t-butyl-carbonyl-oxy-benz-enesulfo-mide (2-((4-(Pivaloyloxy)phenyl)sulfonamido)benzoyl)glycine N-{2-[({4-[(2,2-Dimethylpropanoyl)oxy]phenyl}sulfonyl)amino]benzoyl}glycine |
| Description | Sivelestat(ONO5046; LY544349; EI546) is a competitive inhibitor of human neutrophil elastase(IC50 = 44 nM; Ki=200 nM); also inhibited leukocyte elastase obtained from rabbit, rat, hamster and mouse.IC50 value: 44 nM [1]Target: neutrophil elastaseONO-5046 did not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G even at 100 microM. In in vivo studies, ONO-5046 suppressed lung hemorrhage in hamster (ID50 = 82 micrograms/kg) by intratracheal administration and increase of skin capillary permeability in guinea pig (ID50 = 9.6 mg/kg) by intravenous administration, both of which were induced by human neutrophil elastase [1]. Sivelestat sodium hydrate is an anti-neutrophil elastase inhibitor and may be one of the treatment options for acute respiratory failure due to pneumocystis pneumonia in AIDS patients [2]. |
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| Related Catalog | |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Molecular Formula | C20H22N2O7S |
| Molecular Weight | 434.463 |
| Exact Mass | 434.114777 |
| PSA | 147.25000 |
| LogP | 2.96 |
| Index of Refraction | 1.598 |
| Storage condition | -20℃ |
| HS Code | 2935009090 |
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~%
127373-66-4 |
| Literature: Bioorganic and Medicinal Chemistry, , vol. 4, # 12 p. 2115 - 2134 |
|
~71%
127373-66-4 |
| Literature: Bijukumar; Maloyesh; Sampat; Bhirud; Rajendra Synthetic Communications, 2008 , vol. 38, # 11 p. 1718 - 1724 |
|
~%
127373-66-4 |
| Literature: Bioorganic and Medicinal Chemistry, , vol. 4, # 12 p. 2115 - 2134 |
|
~%
127373-66-4 |
| Literature: Bioorganic and Medicinal Chemistry, , vol. 4, # 12 p. 2115 - 2134 |
|
~%
127373-66-4 |
| Literature: Bioorganic and Medicinal Chemistry, , vol. 4, # 12 p. 2115 - 2134 |
| Precursor 5 | |
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| DownStream 0 | |
| HS Code | 2935009090 |
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| Summary | 2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0% |