A positive allosteric modulator of the GABAA receptor
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Alogabat

Item No. 46377

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-[[5-methyl-3-(6-methyl-3-pyridinyl)-4-isoxazolyl]methoxy]-N-(tetrahydro-2H-pyran-4-yl)-3-pyridazinecarboxamide
CAS Number
2230009-48-8
Synonyms
  • RG-7816
  • RO7017773
Molecular Formula
C21H23N5O4
Formula Weight
409.4
Purity
≥98%
Formulation (Request formulation change)
A solid
SMILES
CC1=C(COC2=CC=C(N=N2)C(NC3CCOCC3)=O)C(C4=CC=C(C)N=C4)=NO1
InChi Code
InChI=1S/C21H23N5O4/c1-13-3-4-15(11-22-13)20-17(14(2)30-26-20)12-29-19-6-5-18(24-25-19)21(27)23-16-7-9-28-10-8-16/h3-6,11,16H,7-10,12H2,1-2H3,(H,23,27)
InChi Key
ACZCJTHHWMBFKC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $75

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    5 mg

    $338

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    10 mg

    $525

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    25 mg

    $750

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    Product Description

    Alogabat is a positive allosteric modulator of the GABAA receptor (GABAAR).1 It potentiates GABA-stimulated currents in X. laevis oocytes expressing α5β3γ2 and α5β3γ3 subunit-containing GABAARs (EC50s = 12 and 20 nM, respectively). It is selective for α5β3γ2 subunit-containing GABAARs over α1β3γ2, α2β3γ2, and α3β3γ2 subunit-containing GABAARs (Kis = 10.9, 415.8, 178.3, and 113 nM, respectively) and is greater than 917-fold selective over a panel of 56 receptors, ion channels, and enzymes at 10 µM. Alogabat (60-120 mg/kg, i.p.) reduces repetitive self-grooming behavior in a BTBR mouse model of autism spectrum disorder (ASD). It inhibits seizures induced by pentylenetetrazole (PTZ; Item No. 18682) in rats when administered orally at a dose of 15 or 30 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Cecere, G., Ballard, T.M., Knoflach, F., et al. Preclinical pharmacology of alogabat: A novel GABAA-α5 positive allosteric modulator targeting neurodevelopmental disorders with impaired GABAA signaling. Front. Pharmacol. 16:1626078, (2025).