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GSK-1014802

Cat. No. M6085
GSK-1014802 Structure
Synonym:

CNV1014802; CNV-1014802; Raxatrigine

Size Price Availability Quantity
5mg USD 200 In stock
10mg USD 350 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Like lamotrigine, both GSK2 and GSK3 were able to prevent the deficit in reversal learning produced by PCP, thus confirming their potential in the treatment of cognitive symptoms of schizophrenia. However, higher doses than those required for anticonvulsant efficacy of the drugs were needed for activity in the reversal-learning model, suggesting a lower therapeutic window relative to mechanism-dependent central side effects for this indication. CNV1014802 received orphan-drug designation from the US Food and Drug Administration in July 2013.

Protocol
Cell Experiment
Cell lines HEK cells
Preparation method Activity of CNV1014802 was assessed in HEK cells heterologously expressing NaV1.1–NaV1.8 using FLIPR membrane potential assays.
Concentrations 1 mM
Incubation time 5 minutes
Animal Experiment
Animal models adult male C57BL/6J mice
Formulation phosphate-buffered saline/10% DMSO
Dosages 30 mg/kg
Administration i.v.
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 314.35
Formula C18H19FN2O2
CAS Number 934240-30-9
Purity >99%
Solubility 10 mM in DMSO
Storage at -20°C
References

Analgesic Effects of GpTx-1, PF-04856264 and CNV1014802 in a Mouse Model of NaV1.7-Mediated Pain.
Deuis JR, et al. Toxins (Basel). 2016 Mar 17;8(3). pii: E78. PMID: 26999206.

Novel design for a phase IIa placebo-controlled, double-blind randomized withdrawal study to evaluate the safety and efficacy of CNV1014802 in patients with trigeminal neuralgia.
Zakrzewska JM, et al. Trials. 2013 Nov 23;14:402. PMID: 24267010.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GSK-1014802, CNV1014802; CNV-1014802; Raxatrigine supplier, Sodium Channel, inhibitors

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