1. Metabolic Enzyme/Protease
  2. Elastase
  3. GW311616

GW311616 

Cat. No.: HY-15891 Purity: 99.52%
Handling Instructions

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.

For research use only. We do not sell to patients.

GW311616 Chemical Structure

GW311616 Chemical Structure

CAS No. : 198062-54-3

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Solution
10 mM * 1 mL in DMSO USD 462 Get quote
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10 mM * 1 mL
ready for reconstitution
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Solid
5 mg USD 550 In-stock
Estimated Time of Arrival: December 31
10 mg USD 880 Get quote
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Customer Review

Based on 4 publication(s) in Google Scholar

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Description

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: U937 and K562 cells
Concentration: 150 μM
Incubation Time: 48 hours
Result: Markedly suppressed NE activity.

Apoptosis Analysis[2]

Cell 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 Analysis[2]

Cell 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 (t1/2) of 1.1 hours and 1.5 hours for dog (2 mg/kg, oral), rat (2 mg/kg, oral), respectively[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Dogs (9-month-old)[3]
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.
Molecular Weight

397.53

Formula

C₁₉H₃₁N₃O₄S

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 44 mg/mL (110.68 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5155 mL 12.5777 mL 25.1553 mL
5 mM 0.5031 mL 2.5155 mL 5.0311 mL
10 mM 0.2516 mL 1.2578 mL 2.5155 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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GW311616
Cat. No.:
HY-15891
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