SKU : MC537137
CAS Number : 198062-54-3
Molecular Formula : C19H32ClN3O4S | Molecular Weight : 433.99
Quote RequestPurity | NLT 98% |
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Storage | at 20ºC 2 years |
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Chemical Name | GW311616 |
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CAS Number | 198062-54-3 |
MDL Number | MFCD06411566 |
Molecular Formula | C19H32ClN3O4S |
Molecular Weight | 433.99 |
GW-311616 is a potent, orally bioavailable, long duration and selective human neutrophil elastase (HNE) inhibitor with IC50 value of 22 nM and Ki value of 0.31 nM[1]. IC50 & Target: IC50: 22 nM (HNE)[1] Ki: 0.31 nM (HNE)[1] In Vitro: GW-311616 (150 μM; 48 hours) markedly suppresses NE activity in U937 and K562 cells lines[2].
GW-311616 (20-320 μM; 48 hours; U937 cells) treatment inhibits proliferation and induces apoptosis in leukemia cells[2].
GW-311616 (150 μM; U937 cells) treatment can increase the protein expression levels of Bax and decrease the expression of Bcl-2[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 (t1/2) of 1.1 hours and 1.5 hours for dog (2 mg/kg, oral), rat (2 mg/kg, oral), respectively[3].
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