A 5-HT6 receptor antagonist
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AVN-492

Item No. 28079

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N2,N6,N6,5,7-pentamethyl-3-(phenylsulfonyl)-pyrazolo[1,5-a]pyrimidine-2,6-diamine
CAS Number
1220646-23-0
Molecular Formula
C17H21N5O2S
Formula Weight
359.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMF:PBS (pH 7.2) (1:20): 0.04 mg/mlDMSO: 25 mg/mlEthanol: 1 mg/ml
λmax
247 nm
SMILES
CN(C)C(C(C)=N1)=C(C)N2C1=C(S(C3=CC=CC=C3)(=O)=O)C(NC)=N2
InChi Code
InChI=1S/C17H21N5O2S/c1-11-14(21(4)5)12(2)22-17(19-11)15(16(18-3)20-22)25(23,24)13-9-7-6-8-10-13/h6-10H,1-5H3,(H,18,20)
InChi Key
SNPPEHMSSOEYDH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice 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

    AVN-492 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 0.09 nM).1 It selectively inhibits the 5-HT6 receptor over the 5-HT2B receptor (IC50s = 0.19 and 268 nM, respectively, in a radioligand binding assay). AVN-492 inhibits increases in cAMP levels induced by 5-HT in HEK293 cells expressing the 5-HT6 receptor (IC50 = 1.5 nM). It increases the time spent in the open arms of the elevated plus maze in rats, indicating anxiolytic activity, when administered at a dose of 0.2 mg/kg. AVN-492 (1 mg/kg) also prevents memory deficits induced by the NMDA receptor antagonist MK-801 in a passive avoidance test.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ivachtchenko, A.V., Okun, I., Aladinskiy, V., et al. AVN-492, a novel highly selective 5-HT6R antagonist: Preclinical evaluation. J. Alzheimers Dis. 58(4), 1043-1063 (2017).