| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C19H31N3O4S |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
GW311616 is a potent, orally bioavailable, long-duration and selective inhibitor of human neutrophil elastase (HNE), with an IC50 of 22 nM and a Ki of 0.31 nM[1]. It is supplied as a light brown to brown solid (C19H31N3O4S, MW 397.53) at 99.30% purity.
Physical & Chemical Properties
| CAS Number | 198062-54-3 |
|---|---|
| Molecular Formula | C19H31N3O4S |
| Molecular Weight | 397.53 g/mol |
| Purity | 99.30% |
| Appearance | Solid |
| Color | Light brown to brown |
| SMILES | O=C1[C@@H](C(C)C)[C@@](N(C(/C=C/CN2CCCCC2)=O)CC3)([H])[C@]3([H])N1S(=O)(C)=O |
| Signaling Pathway | Metabolic Enzyme/Protease |
| Solubility | In Vitro: DMSO: 66.67 mg/mL (167.71 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
IC50: 22 nM (HNE)[1] Ki: 0.31 nM (HNE)[1]
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 66.67 mg/mL (167.71 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | 2.5 mg/mL (6.29 mM); clear solution; requires sonication |
| How to prepare | Gives a clear solution at 2.5 mg/mL. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | 2.5 mg/mL (6.29 mM); clear solution; requires sonication |
| How to prepare | Gives a clear solution at 2.5 mg/mL. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Data provided by the manufacturer.
In Vitro
NE activity in U937 and K562 cell lines is markedly suppressed by GW-311616 (150 μM; 48 hours)[2]. In U937 cells, GW-311616 (20-320 μM; 48 hours) inhibits proliferation and induces apoptosis in leukemia cells[2]. In U937 cells treated with GW-311616 (150 μM), Bax protein expression levels can rise and Bcl-2 expression can fall[2].
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
A 2 mg/kg oral dose of GW-311616 rapidly abolishes circulating neutrophil elastase (NE) in dogs, and >90% inhibition is maintained for 4 days. This prolonged effect is attributed to penetration of bone marrow neutrophils by orally administered GW-311616. GW-311616 has a moderate terminal elimination half-life (t1/2) of 1.1 hours in dogs (2 mg/kg, oral) and 1.5 hours in rats (2 mg/kg, oral)[3].
| 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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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FGF19-Induced Inflammatory CAF Promoted Neutrophil Extracellular Trap Formation in the Liver Metastasis of Colorectal Cancer. Adv Sci (Weinh) 2023 Aug;10(24):e2302613. PMID: 37345586
Differences in Staining for Neutrophil Elastase and its Controlling Inhibitor SLPI Reveal Heterogeneity among Neutrophils in Psoriasis. J Invest Dermatol 2020 Jul;140(7):1371-1378.e3.
Neutrophil elastase-mediated proteolysis of the tumor suppressor p200 CUX1 promotes cell proliferation and inhibits cell differentiation in APL. Life Sci 2020 Feb 1:242:117229.
Loss of BRD4 induces cell senescence in HSC/HPCs by deregulating histone H3 clipping. EMBO Rep 2023 Oct 9;24(10):e57032. PMID: 37650863
Inhibition of neutrophil elastase prevents cigarette smoke exposure-induced formation of neutrophil extracellular traps and improves lung function in a mouse model of chronic obstructive pulmonary disease. Int Immunopharmacol 2023 Jan:114:109537. PMID: 36495695
Mineral particles stimulate innate immunity through neutrophil extracellular traps containing HMGB1. Sci Rep 2017 Nov 30;7(1):16628.
Neutrophil extracellular traps formation driven by novel ELANE mutations in cyclic neutropenia patients. Genes Immun 2026 Jun 23. PMID: 42337056
Epigallocatechin-3-gallate reduces neutrophil extracellular trap formation and tissue injury in severe acute pancreatitis. J Leukoc Biol 2022 Dec;112(6):1427-1443. PMID: 35983712
Early recruited neutrophils promote asthmatic inflammation exacerbation by release of neutrophil elastase. Cell Immunol 2020 Jun:352:104101. PMID: 32278493
Neutrophil expression of CD41/CD61 complex contributes to their adhesiveness in both healthy individuals and heart failure patients. BMC Immunol 2025 Aug 30;26(1):63. PMID: 40885916