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GW311616

Cat. No. M5147
GW311616 Structure
Size Price Availability Quantity
2mg USD 250  USD250 In stock
5mg USD 400  USD400 In stock
10mg USD 580  USD580 In stock
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Quality Control & Documentation
Biological Activity

GW311616 is a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase(HNE) with IC50 of 22 nM. GW311616 is the free base form of GW311616A. The HNE inhibitor GW311616A is selective over other human serine proteases (IC50 values >100 uM for trypsin, cathepsin G, and plasmin, >3 mM for chymotrypsin and tissue plasminogen activator). Acetylcholinesterase is not inhibited by GW311616A at 100 uM.

Customer Product Validations & Biological Datas
Source Mol Med Rep (2015). Figure 4. GW311616
Method proliferation assay
Cell Lines U937 cells
Concentrations 150 μmol/l
Incubation Time 48 h
Results In the GW311616A.treated group, the rate of apoptosis was enhanced, as compared with the control group
Chemical Information
Molecular Weight 397.53
Formula C19H31N3O4S
CAS Number 198062-54-3
Solubility (25°C) DMSO 10 mM
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Macdonald SJ, et al. Bioorg Med Chem Lett. The discovery of a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase--GW311616A a development candidate.

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