GW311616

Cat. No.: HY-15891 Purity: 99.30%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

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

GW311616 Chemical Structure

CAS No. : 198062-54-3

Size	Price	Stock
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 429	Ask For Quote & Lead Time
Solution
10 mM * 1 mL in DMSO	USD 429	Ask For Quote & Lead Time
Solid
5 mg	USD 390	Ask For Quote & Lead Time
10 mg	USD 580	Ask For Quote & Lead Time

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This product is a controlled substance and not for sale in your territory.

Other In-stock Forms of GW311616:

GW311616 hydrochloride

Other Forms of GW311616:

GW311616 hydrochloride In-stock

8 Publications Citing Use of MCE GW311616

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Biological Activity
Purity & Documentation
References
Customer Review

Description

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.

Molecular Weight

397.53

Formula

C₁₉H₃₁N₃O₄S

CAS No.

198062-54-3

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.30%

Select Batch:

Data Sheet (283 KB) SDS (252 KB)

COA (256 KB) LCMS (263 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

GW311616 Related Classifications

Inflammation/Immunology

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GW311616198062-54-3GW 311616GW-311616ElastaseInhibitorinhibitorinhibit

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