Chemical Name |
GW311616 |
CAS Number |
198062-54-3 |
MDL Number |
MFCD06411566 |
Molecular Formula |
C19H32ClN3O4S |
Molecular Weight |
433.99 |
Introduction of 198062-54-3 :
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].
Purity |
NLT 98% |
Storage |
at 20ºC 2 years |
*The above information is for reference only.