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AWD 131-138

Cat. No. M2555
AWD 131-138 Structure
Synonym:

Imepitoin

Size Price Availability Quantity
10mM*1mL USD 157.5  USD175 In stock
5mg USD 90  USD100 In stock
10mg USD 162  USD180 In stock
50mg USD 630  USD700 In stock
100mg USD 1080  USD1200 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

AWD 131-138 is a new low-affinity partial benzodiazepine receptor agonist, which has potent anticonvulsant and anxiolytic properties in rodent models. AWD 131-138 dose-dependently stimulated GABA currents (Recombinant gamma aminobutyric acid A (GABA(A)) receptors of the subunit compositions alpha1beta2gamma2, alpha1beta3gamma2, alpha2beta2gamma2, alpha3beta2gamma2 and alpha5beta2gamma2). At 10 microM AWD 131-138, this allosteric stimulation amounted to nearly 12-21% of the maximal stimulation achieved using diazepam in average. AWD 131-138 did not produce midazolam-like responding or alter response rates at cumulative doses up to 18.0 mg/kg i.m. (plasma levels over 2100 ng/ml).

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 279.72
Formula C13H14ClN3O2
CAS Number 188116-07-6
Purity >98%
Solubility DMSO
Storage at -20°C
References

The antiepileptic drug AWD 131-138 stimulates different recombinant isoforms of the rat GABA(A) receptor through the benzodiazepine binding site.
Sigel E,et al. Neurosci Lett. 1998 Apr 3;245(2):85-8. PMID: 9605491.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: AWD 131-138, Imepitoin supplier, GABA Receptor, inhibitors

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