GW311616 - 10mM in DMSO , CAS No.198062-54-3

CAS: 198062-54-3 Cat. No.: G654886 Summenformel: C₁₉H₃₁N₃O₄S Molekulargewicht: 397.53 PubChem CID: 9800961

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Übersicht

GW-311616 is a potent, orally bioavailable, long duration and selective human neutrophil elastase ( HNE ) inhibitor with IC 50 value of 22 nM and K i value of 0.31 nM

In Vitro

GW-311616 (150 μM; 48 hours) markedly suppresses NE activity in U937 and K562 cells lines. GW-311616 (20-320 μM; 48 hours; U937 cells) treatment inhibits proliferation and induces apoptosis in leukemia cells. GW-311616 (150 μM; U937 cells) treatment can increase the protein expression levels of Bax and decrease the expression of Bcl-2. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: U937 and K562 cells Concentration: 150 μM Incubation Time: 48 hours Result: Markedly suppressed NE activity. Apoptosis AnalysisCell Line: U937 cells Concentration: 20 μM, 40 μM, 80 μM, 160 μM, 320 μM Incubation Time: 48 hours Result: The rate of apoptosis was enhanced. Western Blot AnalysisCell Line: U937 cells Concentration: 150 μM Incubation Time: 48 hours Result: Increased the protein expression levels of Bax and decreased the expression of Bcl-2.

In Vivo

GW-311616 (2 mg/kg; oral administration) rapidly abolishes the circulation of neutrophil elastase (NE) in dogs, while >90% inhibition is maintained for 4 days. This prolonged effect is independent to be due to penetration of neutrophils in bone marrow by orally administrated GW-311616. GW-311616 has moderate terminal elimination half-life (t 1/2 ) of 1.1 hours and 1.5 hours for dog (2 mg/kg, oral), rat (2 mg/kg, oral), respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Dogs (9-month-old)Dosage: 0.22 mg/kg, 0.66 mg/kg and 2 mg/kg (Pharmacokinetic study) Administration: Oral administration Result: At 0.22 mg/kg, greater than 50% inhibition of elastase was achieved 6 hours after dosing, with activity returning towards control values. Single oral dose of 2 mg/kg rapidly abolished circulating enzyme activity, and greater than 90% inhibition was maintained for 4 days.

IC50& Target:IC50: 22 nM (HNE), Ki: 0.31 nM (HNE)

Specifications

Spezifikationen & Reinheit

10mM in DMSO

Biochemische und physiologische Mechanismen

GW-311616 is a potent, orally bioavailable, long duration and selective human neutrophil elastase ( HNE ) inhibitor with IC 50 value of 22 nM and K i value of 0.31 nM.

Storage

Store at -80°C

Verschickt in

Dry ice packs + Cold packs

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Namen und Kennungen

Isomere SMILES

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

Alternative CAS-Nummer

198062-54-3

PubChem CID

9800961

MeSH-Eintrag

GW 311616;GW311616;GW311616A

Molekulargewicht

397.53

Häufig gestellte Fragen

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 198062-54-3, the molecular formula is C19H31N3O4S, and the molecular weight is 397.53 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.