Art. -Nr.: HY-15891

GW311616

11 Cited Publications

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Based on 11 publication(s) in Google Scholar

GW-311616 is a potent, orally bioavailable, long duration and selective human neutrophil elastase (HNE) inhibitor with IC₅₀ value of 22 nM and K_i value of 0.31 nM.

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Reinheit: 99.30%
CAS. Nr.: 198062-54-3
Formel: C₁₉H₃₁N₃O₄S
Molecular Weight:397.53

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

GW311616 Chemical Structure

CAS. Nr.: 198062-54-3

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (11)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

GW-311616 is a potent, orally bioavailable, long duration and selective human neutrophil elastase (HNE) inhibitor with IC₅₀ value of 22 nM and K_i 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].

MedChemExpress (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 (t_1/2) of 1.1 hours and 1.5 hours for dog (2 mg/kg, oral), rat (2 mg/kg, oral), respectively^[3].

MedChemExpress (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.

Chemical Information

CAS. Nr. 198062-54-3
Appearance Solid
Molecular Weight 397.53
Formel C₁₉H₃₁N₃O₄S
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (11)

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Journal Impact Factor

Adv Sci (Weinh)

FGF19-Induced Inflammatory CAF Promoted Neutrophil Extracellular Trap Formation in the Liver Metastasis of Colorectal Cancer. [Abstract]

2023 Aug;10(24):e2302613. PMID: 37345586
J Invest Dermatol

Differences in Staining for Neutrophil Elastase and its Controlling Inhibitor SLPI Reveal Heterogeneity among Neutrophils in Psoriasis. [Abstract]

2020 Jul;140(7):1371-1378.e3. PMID: 31945345
Life Sci

Neutrophil elastase-mediated proteolysis of the tumor suppressor p200 CUX1 promotes cell proliferation and inhibits cell differentiation in APL. [Abstract]

2020 Feb 1:242:117229. PMID: 31887298
EMBO Rep

Loss of BRD4 induces cell senescence in HSC/HPCs by deregulating histone H3 clipping. [Abstract]

2023 Oct 9;24(10):e57032. PMID: 37650863
Int Immunopharmacol

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. [Abstract]

2023 Jan:114:109537. PMID: 36495695
Sci Rep

Mineral particles stimulate innate immunity through neutrophil extracellular traps containing HMGB1. [Abstract]

2017 Nov 30;7(1):16628. PMID: 29192209
Genes Immun

Neutrophil extracellular traps formation driven by novel ELANE mutations in cyclic neutropenia patients. [Abstract]

2026 Jun 23. PMID: 42337056
J Leukoc Biol

Epigallocatechin-3-gallate reduces neutrophil extracellular trap formation and tissue injury in severe acute pancreatitis. [Abstract]

2022 Dec;112(6):1427-1443. PMID: 35983712
Cell Immunol

Early recruited neutrophils promote asthmatic inflammation exacerbation by release of neutrophil elastase. [Abstract]

2020 Jun:352:104101. PMID: 32278493
BMC Immunol

Neutrophil expression of CD41/CD61 complex contributes to their adhesiveness in both healthy individuals and heart failure patients. [Abstract]

2025 Aug 30;26(1):63. PMID: 40885916
Res Sq

2025 Mar 30.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 66.67 mg/mL (167.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.5 mg/mL (6.29 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (6.29 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Ohbayashi H,et al. Neutrophil elastase inhibitors as treatment for COPD. Expert Opin Investig Drugs. 2002 Jul;11(7):965-80. [Content Brief]

[2]. Jiang KL, et al. Neutrophil elastase and its therapeutic effect on leukemia cells. Mol Med Rep. 2015 Sep;12(3):4165-4172. [Content Brief]

[3]. Macdonald SJ, et al. The discovery of a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase--GW311616A a development candidate. Bioorg Med Chem Lett. 2001 Apr 9;11(7):895-8. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5155 mL	12.5777 mL	25.1553 mL	62.8883 mL
	5 mM	0.5031 mL	2.5155 mL	5.0311 mL	12.5777 mL
	10 mM	0.2516 mL	1.2578 mL	2.5155 mL	6.2888 mL
	15 mM	0.1677 mL	0.8385 mL	1.6770 mL	4.1926 mL
	20 mM	0.1258 mL	0.6289 mL	1.2578 mL	3.1444 mL
	25 mM	0.1006 mL	0.5031 mL	1.0062 mL	2.5155 mL
	30 mM	0.0839 mL	0.4193 mL	0.8385 mL	2.0963 mL
	40 mM	0.0629 mL	0.3144 mL	0.6289 mL	1.5722 mL
	50 mM	0.0503 mL	0.2516 mL	0.5031 mL	1.2578 mL
	60 mM	0.0419 mL	0.2096 mL	0.4193 mL	1.0481 mL
	80 mM	0.0314 mL	0.1572 mL	0.3144 mL	0.7861 mL
	100 mM	0.0252 mL	0.1258 mL	0.2516 mL	0.6289 mL

Keywords

GW311616

11 Cited Publications

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GW311616

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) GW311616

Biologische Aktivität

Chemical Information

Publications (11)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GW311616

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) GW311616

Biologische Aktivität

Chemical Information

Publications (11)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GW311616 Related Classifications

HY-15891 Related Classifications