A positive allosteric modulator of EAAT2
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(R)-AS-1

Item No. 41673

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
αR-methyl-2,5-dioxo-N-(phenylmethyl)-1-pyrrolidineacetamide
CAS Number
2506367-95-7
Molecular Formula
C14H16N2O3
Formula Weight
260.3
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Sparingly soluble: 1-10 mg/ml
SMILES
C[C@H](C(NCC1=CC=CC=C1)=O)N(C(CC2)=O)C2=O
InChi Code
InChI=1S/C14H16N2O3/c1-10(16-12(17)7-8-13(16)18)14(19)15-9-11-5-3-2-4-6-11/h2-6,10H,7-9H2,1H3,(H,15,19)/t10-/m1/s1
InChi Key
XVSYJYYNUSOPAQ-SNVBAGLBSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $43

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    5 mg

    $172

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    10 mg

    $323

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    25 mg

    $752

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    Product Description

    (R)-AS-1 is a positive allosteric modulator of excitatory amino acid transporter 2 (EAAT2; EC50 = 11 nM in a glutamate uptake assay).1 It is selective for EAAT2 over EAAT1, EAAT3, and a panel of 30 other ion channels, transporters, receptors, and enzymes. (R)-AS-1 (60 and 90 mg/kg) increases spontaneous locomotor activity in mice. It has anticonvulsant activity in mouse models of seizures induced by maximal electroshock (MES), pentylenetetrazole (PTZ; Item No. 18682), or electrical stimuli of 32 or 44 mA (ED50s = 66.3, 36.3, 15.6, and 41.6 mg/kg, respectively).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Abram, M., Jakubiec, M., Reeb, K., et al. Discovery of (R)-N-benzyl-2-(2,5-dioxopyrrolidin-1-yl)propanamide [(R)-AS-1], a novel orally bioavailable EAAT2 modulator with drug-like properties and potent antiseizure activity in vivo. J. Med. Chem. 65(17), 11703-11725 (2022).