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GNE-7915

Cat. No. M3649
GNE-7915 Structure
Size Price Availability Quantity
10mM*1mL in DMSO USD 50  USD50 In stock
5mg USD 44  USD44 In stock
10mg USD 80  USD80 In stock
50mg USD 240  USD240 In stock
100mg USD 400  USD400 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • 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.

Customer Product Validations & Biological Datas
Source CNS Neurosci Ther (2017). Figure 2. GNE-7915
Method Western blot
Cell Lines WT mice
Concentrations 1 and 3 μM
Incubation Time 2-h
Results In contrast, GSK2578215A and GNE-7915 at all concentrations had no effect on DA release and recovery. Western blot confirmed the dose–response inhibition by the LRRK2 inhibitions
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 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.

Chemical Information
Molecular Weight 443.40
Formula C19H21F4N5O3
CAS Number 1351761-44-8
Purity >98%
Solubility DMSO 10 mM
Storage at -20°C
References

[1] Estrada AA, et al. J Med Chem. Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.

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  Catalog
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Keywords: GNE-7915 supplier, LRRK2, inhibitors

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