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AB287090

GW-311616A

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(3 Publications)

MW 434 Da, Purity >98%. A potent and selective intracellular neutrophil elastase (NE, alpha-1-proteinase) inhibitor. Inhibits human neutrophil elastase (HNE) and is selective over other human serine proteases with IC50 values of 22 nM for HNE, >100 μM for trypsin, cathepsin G and plasmin, >3 μM for chymotrypsin and tissue plasminogen activator.

View Alternative Names

Bone marrow serine protease, ELA2, ELANE, ELNE_HUMAN, Elastase 2 neutrophil, Elastase neutrophil expressed, Elastase-2, Granulocyte derived elastase, HLE, HNE, Human leukocyte elastase, Leukocyte elastase, Medullasin, NE, Neutrophil elastase, PMN E, PMN elastase, Polymorphonuclear elastase, SCN1

Key facts

CAS number

197890-44-1

Purity

>98%

Form

Solid

form

Molecular weight

434 Da

Molecular formula

C<sub>1</sub><sub>9</sub>H<sub>3</sub><sub>2</sub>ClN<sub>3</sub>O<sub>4</sub>S

PubChem

9889108

Nature

Synthetic

Solubility

Soluble in DMSO

Soluble in Water

Biochemical name

GW311616 hydrochloride

Biological description

A potent and selective intracellular neutrophil elastase (NE, alpha-1-proteinase) inhibitor. Inhibits human neutrophil elastase (HNE) and is selective over other human serine proteases with IC50 values of 22 nM for HNE, >100 μM for trypsin, cathepsin G and plasmin, >3 μM for chymotrypsin and tissue plasminogen activator.

Canonical smiles

CC(C)C1C2C(CCN2C(=O)C=CCN3CCCCC3)N(C1=O)S(=O)(=O)C.Cl

Isomeric smiles

CC(C)[C@H]1[C@H]2[C@@H](CCN2C(=O)/C=C/CN3CCCCC3)N(C1=O)S(=O)(=O)C.Cl

InChi

InChI=1S/C19H31N3O4S.ClH/c1-14(2)17-18-15(22(19(17)24)27(3,25)26)9-13-21(18)16(23)8-7-12-20-10-5-4-6-11-20;/h7-8,14-15,17-18H,4-6,9-13H2,1-3H3;1H/b8-7+;/t15-,17+,18-;/m1./s1

InChiKey

UFCZUKYPBPXODT-OFTZGUNKSA-N

IUPAC Name

(3aR,6S,6aS)-4-methylsulfonyl-1-[(E)-4-piperidin-1-ylbut-2-enoyl]-6-propan-2-yl-3,3a,6,6a-tetrahydro-2H-pyrrolo[3,2-b]pyrrol-5-one;hydrochloride

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Product details

This product is manufactured by BioVision, an Abcam company and was previously called B2559 GW-311616A. B2559-5 is the same size as the 5 mg size of ab287090.
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Properties and storage information

Shipped at conditions
Blue Ice
Appropriate short-term storage conditions
-20°C
Appropriate long-term storage conditions
-20°C
Storage information
Store under desiccating conditions
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Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

Neutrophil Elastase also known as neutrophil proteinase 3 has a molecular mass of approximately 30 kDa. It is a serine protease expressed mainly in azurophilic granules of neutrophils. This enzyme breaks down various proteins including elastin at sites of inflammation. Neutrophil Elastase releases during degranulation or through neutrophil extracellular traps (NETs) to combat pathogens.
Biological function summary

The target plays a significant role in neutrophil-mediated tissue remodeling and host defense. It leads to the breaking down of extracellular matrix components contributing to tissue remodeling and repair. Neutrophil Elastase is part of a complex interplay with other proteases like matrix metalloproteinases (MMPs). Its activity is regulated by endogenous inhibitors such as alpha-1 antitrypsin to prevent excessive tissue damage.

Pathways

This protease is important in inflammation and immune response pathways. It plays a role in the complement system by activating C5 a component of the complement cascade. It also acts in conjunction with other proteases such as cathepsin G to modulate immune and inflammatory responses. Neutrophil Elastase's role within these pathways is pivotal for the regulation of inflammation and destruction of pathogens.

Individuals with conditions such as chronic obstructive pulmonary disease (COPD) and cystic fibrosis often exhibit dysregulation or excessive activity of Neutrophil Elastase. This excessive activity leads to tissue damage and exacerbates disease progression. The enzyme also interacts with proteins like elastin and collagen in these diseases further contributing to pathological tissue remodeling and damage.
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Product protocols

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Publications (3)

Recent publications for all applications. Explore the full list and refine your search

Modern rheumatology 30:345-349 PubMed30789095

2019

Activated neutrophil carbamylates albumin the release of myeloperoxidase and reactive oxygen species regardless of NETosis.

Applications

Unspecified application

Species

Unspecified reactive species

Shuichiro Nakabo,Koichiro Ohmura,Shuji Akizuki,Kosaku Murakami,Ran Nakashima,Motomu Hashimoto,Hajime Yoshifuji,Masao Tanaka,Tsuneyo Mimori

Journal of ethnopharmacology 113:312-7 PubMed17689902

2007

Achillea millefolium L. s.l. -- is the anti-inflammatory activity mediated by protease inhibition?

Applications

Unspecified application

Species

Unspecified reactive species

Birgit Benedek,Brigitte Kopp,Matthias F Melzig

Bioorganic & medicinal chemistry letters 11:895-8 PubMed11294386

2001

The discovery of a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase--GW311616A a development candidate.

Applications

Unspecified application

Species

Unspecified reactive species

S J Macdonald,M D Dowle,L A Harrison,P Shah,M R Johnson,G G Inglis,G D Clarke,R A Smith,D Humphreys,C R Molloy,A Amour,M Dixon,G Murkitt,R E Godward,T Padfield,T Skarzynski,O M Singh,K A Kumar,G Fleetwood,S T Hodgson,G W Hardy,H Finch
View all publications
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Complementary Products

Assay Kits

AB270204

Human Neutrophil Elastase ELISA Kit

Recombinant|SimpleStep

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Biochemicals

AB147047

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Primary Antibodies

AB68672

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Immunohistochemistry (Formalin/PFA-fixed paraffin-embedded sections) - Anti-Neutrophil Elastase antibody (AB68672)

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Assay Kits

AB118971

Neutrophil Elastase Inhibitor Assay Kit

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