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

GW311616 hydrochloride (Synonyms: GW311616A)

Cat. No.: HY-15891A Purity: 98.84%
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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 215 In-stock
Estimated Time of Arrival: December 31
5 mg USD 195 In-stock
Estimated Time of Arrival: December 31
10 mg USD 325 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 3 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].

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].

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

Formula

C₁₉H₃₂ClN₃O₄S

CAS No.

197890-44-1

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

H2O : ≥ 100 mg/mL (230.42 mM)

*"≥" means soluble, but saturation unknown.

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.
References

Purity: 98.84%

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Keywords:

GW311616GW311616AGW 311616GW-311616ElastaseInhibitorinhibitorinhibit

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GW311616 hydrochloride
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HY-15891A
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