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GNE-7915

Cat. No. M3649

GNE-7915 Structure
Size Price Availability Quantity
10mg USD 120 In stock
50mg USD 350 In stock
100mg USD 550 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

GNE-7915 is a moderately potent 5-HT2B antagonist. GNE-7915 demonstrates excellent in vitro DMPK with minimal turnover in human hepatocytes. GNE-7915 demonstrates excellent in vivo PK profiles with long half-lives, good oral exposure and high passive permeability.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation
Formulation Suspended in 1% microcrystalline cellulose
Dosages 50 mg/kg
Administration i.p. ; p.o.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 443.40
Formula C19H21F4N5O3
CAS Number 1351761-44-8
Purity >99%
Solubility DMSO
Storage at -20°C
References

Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
Estrada AA, et al. J Med Chem. 2012 Nov 26;55(22):9416-33. PMID: 22985112.

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GSK2578215A

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PF-06447475

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GNE-7915 supplier, LRRK2, inhibitors

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