A negative allosteric modulator of α5 subunit-containing GABAA receptors
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Basmisanil

Item No. 21137

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(1,1-dioxido-4-thiomorpholinyl)[6-[[3-(4-fluorophenyl)-5-methyl-4-isoxazolyl]methoxy]-3-pyridinyl]-methanone
CAS Number
1159600-41-5
Synonyms
  • RG-1662
Molecular Formula
C21H20FN3O5S
Formula Weight
445.5
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/ml
λmax
233 nm
SMILES
O=S1(CCN(C(C2=CC=C(OCC3=C(C)ON=C3C4=CC=C(F)C=C4)N=C2)=O)CC1)=O
InChi Code
InChI=1S/C21H20FN3O5S/c1-14-18(20(24-30-14)15-2-5-17(22)6-3-15)13-29-19-7-4-16(12-23-19)21(26)25-8-10-31(27,28)11-9-25/h2-7,12H,8-11,13H2,1H3
InChi Key
VCGRFBXVSFAGGA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $178

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    10 mg

    $312

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    25 mg

    $680

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    Product Description

    Basmisanil is a negative allosteric modulator of α5 subunit-containing GABAA receptors (Ki = 0.005 µM in HEK293 cells expressing the human α5β3γ2 subunit-containing GABAA receptor).1 It selectively binds to α5 over α1, α2, or α3 subunit-containing GABAA receptors (Kis = 1.031, 0.458, and 0.51 µM, respectively) as well as a panel of 78 receptors, transporters, and ion channels at 10 µM. Basmisanil inhibits GABA-induced currents in Xenopus oocytes expressing the human α5β3γ2 subunit-containing GABAA receptor (IC50 = 0.008 µM), an effect that can be blocked by flumazenil (Item No. 14252). It reverses diazepam-induced cognitive impairments in rats in the Morris water maze when administered at a dose of 10 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hipp, J.F., Knoflach, F., Comley, R., et al. Basmisanil, a highly selective GABAA-α5 negative allosteric modulator: Preclinical pharmacology and demonstration of functional target engagement in man. Sci. Rep. 11(1), 7700 (2021).