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Nefiracetam

Cat. No. M3344
Nefiracetam Structure
Synonym:

DZL 221; DM9384

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 36  USD40 In stock
50mg USD 36  USD40 In stock
100mg USD 58.5  USD65 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Nefiracetam is cognitive enhancer with an IC50 of approximately 150–200 μM for Ro 5-4864. It displays various pharmacological effects. It activates L/N-type calcium channels, cholinergic, monoaminergic and GABAergic systems. It displays potent neuroprotective action in the retinal ischemia-reperfusion model in vivo.

Protocol
Cell Experiment
Cell lines Oocytes
Preparation method Transferring the injected oocytes to the recording chamber 24 to 48 hours after incubation and continuously superfused at room temperature (20 to 22 °C) in a standard frog Ringer's solution (115 mM NaCl, 2 mM KCl, 1.8 mM CaCl2, and 5 mM HEPES, pH 7.0). Ca2+ -free extracellular solution consisted of 115 mM NaCl, 2 mM KCl, 5 mM MgCl2, 5 mM HEPES, and 1 mM EGTA, pH 7.0. To remove the effect of the muscarinic ACh receptor, adding 1 μM atropine the extracellular solution. Using two-electrode, voltage-clamp techniques to record ACh-activated currents. Analyzing the currents on a microcomputer using pClamp software. ACh is bath-applied to oocytes. Nefiracetam is dissolved in distilled water at 1 mM for stock solution and diluted into concentrations which are required with the extracellular solution.
Concentrations ~1 μM
Incubation time 24 hours - 48 hours
Animal Experiment
Animal models Adult male EL mice weighing 25–30 g and adult male DDY mice
Formulation
Dosages
Administration Administered via i.v. or 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 246.3
Formula C14H18N2O2
CAS Number 77191-36-7
Purity >98%
Solubility DMSO 25 mg/mL
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Nefiracetam, DZL 221; DM9384 supplier, GABA Receptor, inhibitors

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