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Sivelestat - 98% (HPLC), haute pureté, inhibiteur de l'élastase leucocytaire, CAS No.127373-66-4, Leukocyte elastase inhibitor

En stock
Item Number
S166827
Articles du produit groupé
SKU Taille
Disponibilité
Prix Qté
S166827-5mg
5mg
5
61,90$US
S166827-25mg
25mg
5
251,90$US
S166827-100mg
100mg
5
906,90$US
S166827-250mg
250mg
5
2 039,90$US
S166827-1g
1g
5
7 341,90$US
S166827-5g
5g
2
33 034,90$US

Inhibiteur puissant, sélectif, compétitif par rapport au substrat de l'élastase neutrophile

Description générale

Synonymes dl-N-Acetylhomocysteinethiolactone | ONO5046;LY544349;EI546 | SIVELESTAT [INN] | SIVELESTAT [MART.] | Acide 2,2-diméthyl-propionique 4-[2-(carboxyméthyl-carbamoyl)-phénylsulfamoyl]-phényl ester | P,.ALPHA.,.ALPHA.-TRIMETHYLBENZYL ALCOHOL [FHFI] | J-005486
Spécifications et pureté Moligand™, ≥98%(HPLC)
Mécanismes biochimiques et physiologiques Inhibiteur puissant, sélectif et compétitif du substrat de l'élastase neutrophile (les valeurs IC 50 sont de 19-49 nM et 5,6 μM pour l'élastase leucocytaire et l'élastase du pancréas respectivement). Supprime la perméabilité capillaire induite par les neu
Température de stockage A l'abri de la lumière,A conserver à -20°C
Expédié en Glacière + blocs de glace
Grade Moligand™
Type d'action INHIBITOR
Mécanisme d'action Leukocyte elastase inhibitor
Note Dans la mesure du possible, les solutions doivent être préparées et utilisées le même jour. Toutefois, si vous devez préparer des solutions de base à l'avance, nous vous recommandons de les conserver sous forme d'aliquotes dans des flacons hermétiques à -20°C. Ces aliquotes sont généralement utilisables pendant un mois. En général, ces solutions peuvent être utilisées pendant un mois. Avant utilisation, et avant d'ouvrir le flacon, nous vous recommandons de laisser votre produit s'équilibrer à température ambiante pendant au moins 1 heure. Besoin de plus de conseils sur la solubilité, l'utilisation et la manipulation ? Veuillez consulter notre page de questions fréquemment posées (FAQ) pour plus de détails.
Product Description

Description du produit

Le sivelestat (EI546) est un inhibiteur compétitif de l'élastase des neutrophiles humains, avec une IC50 de 44 nM et un Ki de 200 nM. Le sivelestat (EI546) pourrait être utilisé dans l'étude des lésions pulmonaires aiguës/syndrome de détresse respiratoire aiguë ou de la coagulation intravasculaire disséminée dans le cadre de l'étude COVID-19

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Benzenoids
Classe Benzene and substituted derivatives
Subclass Benzoic acids and derivatives
Intermediate Tree Nodes Benzamides - Hippuric acids and derivatives
Direct Parent Hippuric acids
Alternative Parents N-acyl-alpha amino acids  Benzenesulfonamides  Sulfanilides  Phenol esters  Benzenesulfonyl compounds  Phenoxy compounds  Benzoyl derivatives  Organosulfonamides  Dicarboxylic acids and derivatives  Vinylogous amides  Aminosulfonyl compounds  Carboxylic acid esters  Secondary carboxylic acid amides  Carboxylic acids  Organopnictogen compounds  Hydrocarbon derivatives  Carbonyl compounds  Organic oxides  Organonitrogen compounds  
Molecular Framework Aromatic homomonocyclic compounds
Substituents Hippuric acid - N-acyl-alpha-amino acid - N-acyl-alpha amino acid or derivatives - Alpha-amino acid or derivatives - Benzenesulfonamide - Phenol ester - Sulfanilide - Benzenesulfonyl group - Phenoxy compound - Benzoyl - Dicarboxylic acid or derivatives - Organosulfonic acid amide - Vinylogous amide - Aminosulfonyl compound - Sulfonyl - Organosulfonic acid or derivatives - Organic sulfonic acid or derivatives - Carboxylic acid ester - Carboxamide group - Secondary carboxylic acid amide - Carboxylic acid - Carboxylic acid derivative - Organooxygen compound - Organonitrogen compound - Organic nitrogen compound - Hydrocarbon derivative - Organic oxide - Organosulfur compound - Organic oxygen compound - Organopnictogen compound - Carbonyl group - Aromatic homomonocyclic compound
Description This compound belongs to the class of organic compounds known as hippuric acids. These are compounds containing hippuric acid, which consists of a of a benzoyl group linked to the N-terminal of a glycine.
External Descriptors Not available

Propriétés du produit

ALogP 3

Cibles associées (humaines)

ELANE Tclin Neutrophil elastase (13 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PRTN3 Tchem Myeloblastin (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
F2 Tclin Thrombin (11687 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ESR1 Tclin Estrogen receptor alpha (17718 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
NR3C1 Tclin Glucocorticoid receptor (14987 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PGR Tclin Progesterone receptor (8562 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ADRB2 Tclin Beta-2 adrenergic receptor (11824 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CHRM2 Tclin Muscarinic acetylcholine receptor M2 (10671 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ADRB1 Tclin Beta-1 adrenergic receptor (6630 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HTR1A Tclin Serotonin 1a (5-HT1a) receptor (14969 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ADRA2A Tclin Alpha-2a adrenergic receptor (9450 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AR Tclin Androgen Receptor (11781 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CHRM1 Tclin Muscarinic acetylcholine receptor M1 (12690 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
DRD2 Tclin Dopamine D2 receptor (23596 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
GABRA1 Tclin GABA receptor alpha-1 subunit (399 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAOA Tclin Monoamine oxidase A (11911 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CNR1 Tclin Cannabinoid CB1 receptor (20913 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
DRD1 Tclin Dopamine D1 receptor (9720 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PTGS1 Tclin Cyclooxygenase-1 (9233 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SLC6A2 Tclin Norepinephrine transporter (10102 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HRH2 Tclin Histamine H2 receptor (5428 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HTR2A Tclin Serotonin 2a (5-HT2a) receptor (14758 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HTR2C Tclin Serotonin 2c (5-HT2c) receptor (11471 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AVPR2 Tclin Vasopressin V2 receptor (2912 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ADORA1 Tclin Adenosine A1 receptor (17603 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AGTR1 Tclin Type-1 angiotensin II receptor (5176 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SLC6A4 Tclin Serotonin transporter (12625 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PTGS2 Tclin Cyclooxygenase-2 (13999 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HRH1 Tclin Histamine H1 receptor (7573 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
OPRM1 Tclin Mu opioid receptor (19785 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
DRD3 Tclin Dopamine D3 receptor (14368 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AVPR1A Tclin Vasopressin V1a receptor (5412 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
OPRD1 Tclin Delta opioid receptor (15096 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
OPRK1 Tclin Kappa opioid receptor (16155 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HTR3A Tclin Serotonin 3a (5-HT3a) receptor (3366 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SLC6A3 Tclin Dopamine transporter (10535 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
GRIN1 Tclin Glutamate (NMDA) receptor subunit zeta 1 (122 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KCNH2 Tclin HERG (29587 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CACNA1C Tclin Voltage-gated L-type calcium channel alpha-1C subunit (766 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PDE3A Tclin Phosphodiesterase 3A (3309 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ADRA2B Tclin Alpha-2b adrenergic receptor (4412 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ADRA2C Tclin Alpha-2c adrenergic receptor (4876 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CHRM3 Tclin Muscarinic acetylcholine receptor M3 (7750 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HTR2B Tclin Serotonin 2b (5-HT2b) receptor (10323 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ELANE Tclin Leukocyte elastase (8173 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
TBXA2R Tclin Thromboxane A2 receptor (5717 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
EDNRA Tclin Endothelin receptor ET-A (5008 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ADORA2A Tclin Adenosine A2a receptor (16305 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ADORA3 Tchem Adenosine A3 receptor (15931 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BDKRB2 Tclin Bradykinin B2 receptor (3970 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HRH3 Tclin Histamine H3 receptor (10389 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CTSG Tchem Cathepsin G (2304 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Cibles associées (non humaines)

Npy1r Neuropeptide Y receptor type 1 (8 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Trypsin (394 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Cckar Cholecystokinin A receptor (90 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Pde4d Phosphodiesterase 4D (4 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Hdac6 Histone deacetylase 6 (222 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Kallikrein 1 (28 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Cavia porcellus (23802 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Mus musculus (284745 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Cricetinae gen. sp. (3197 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
NIH3T3 (5395 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Elane Neutrophil elastase (15 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Plasma (328 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CELA2A Pancreatic elastase (395 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Liver microsome (341 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mécanismes d'action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name Références

Noms et identifiants

Pubchem Sid 488187416
Pubchem Sid Url https://pubchem.ncbi.nlm.nih.gov/substance/488187416
IUPAC Name 2-[[2-[[4-(2,2-dimethylpropanoyloxy)phenyl]sulfonylamino]benzoyl]amino]acetic acid
INCHI InChI=1S/C20H22N2O7S/c1-20(2,3)19(26)29-13-8-10-14(11-9-13)30(27,28)22-16-7-5-4-6-15(16)18(25)21-12-17(23)24/h4-11,22H,12H2,1-3H3,(H,21,25)(H,23,24)
InChIKey BTGNGJJLZOIYID-UHFFFAOYSA-N
Smiles CC(C)(C)C(=O)OC1=CC=C(C=C1)S(=O)(=O)NC2=CC=CC=C2C(=O)NCC(=O)O
Isomères SMILES CC(C)(C)C(=O)OC1=CC=C(C=C1)S(=O)(=O)NC2=CC=CC=C2C(=O)NCC(=O)O
CAS alternatif 331731-18-1,127373-66-4
Termes d'entrée MeSH N-(2-(4-(2,2-dimethylpropionyloxy)phenylsulfonylamino)benzoyl)aminoacetic acid;ONO 5046;ONO-5046;Ono-EI-600;sivelestat
Poids moléculaire 434.46
Reaxy-Rn 7666855
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=7666855&ln=

Certificats (CoA, COO, BSE/TSE et tableau d'analyse)

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Lot Number Certificate Type Date Article
D2308477 Certificate of Analysis Feb 20, 2023 S166827
D2308483 Certificate of Analysis Feb 20, 2023 S166827
D2308485 Certificate of Analysis Feb 20, 2023 S166827
D2308473 Certificate of Analysis Feb 20, 2023 S166827
D2308475 Certificate of Analysis Feb 20, 2023 S166827
D2308470 Certificate of Analysis Feb 20, 2023 S166827
D2308479 Certificate of Analysis Feb 20, 2023 S166827
D2308478 Certificate of Analysis Feb 20, 2023 S166827
D2308481 Certificate of Analysis Feb 20, 2023 S166827
D2308476 Certificate of Analysis Feb 20, 2023 S166827
D2308461 Certificate of Analysis Feb 20, 2023 S166827
D2308615 Certificate of Analysis Feb 20, 2023 S166827

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Propriétés chimiques et physiques

Sensibilité light sensitive
Poids moléculaire 434.500 g/mol
XLogP3 3.000
Hydrogen Bond Donor Count 3
Hydrogen Bond Acceptor Count 8
Rotatable Bond Count 9
Exact Mass 434.115 Da
Monoisotopic Mass 434.115 Da
Topological Polar Surface Area 147.000 Ų
Heavy Atom Count 30
Formal Charge 0
Complexity 731.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 0
Undefined Atom Stereocenter Count 0
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

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