2. Metabolic Enzyme/Protease
  3. Elastase
  4. GW311616 hydrochloride

GW311616 hydrochloride  (Synonyms: GW311616A)

Cat. No.: HY-15891A Purity: 98.71%
COA 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 hydrochloride Chemical Structure

GW311616 hydrochloride Chemical Structure

CAS No. : 197890-44-1

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Based on 6 publication(s) in Google Scholar

Other Forms of GW311616 hydrochloride:

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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].
GW311616A (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.
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 is achieved 6 hours after dosing, with activity returning towards control values. Single oral dose of 2 mg/kg rapidly abolishes circulating enzyme activity, and greater than 90% inhibition is maintained for 4 days.
Molecular Weight

433.99

Appearance

Solid

Formula

C19H32ClN3O4S
CAS No.
SMILES

O=C1[[email protected]@H](C(C)C)[[email protected]@](N(C(/C=C/CN2CCCCC2)=O)CC3)([H])[[email protected]]3([H])N1S(=O)(C)=O.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (230.42 mM; Need ultrasonic)

H2O : 100 mg/mL (230.42 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3042 mL 11.5210 mL 23.0420 mL
5 mM 0.4608 mL 2.3042 mL 4.6084 mL
10 mM 0.2304 mL 1.1521 mL 2.3042 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (5.76 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (5.76 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.76 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 98.84%

COA (257 KB) HNMR (146 KB) LCMS (122 KB)

Handling Instructions (2659 KB)
References
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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.

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Keywords:

GW311616197890-44-1GW311616AGW 311616GW-311616ElastaseInhibitorinhibitorinhibit

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