An inverse agonist of α5β3γ2 subunit-containing GABAA receptors
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TB 21007

Item No. 27674

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6,7-dihydro-3-[(2-hydroxyethyl)thio]-6,6-dimethyl-1-(2-thiazolyl)-benzo[c]thiophen-4(5H)-one
CAS Number
207306-50-1
Molecular Formula
C15H17NO2S3
Formula Weight
339.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 100 mMEthanol: 25 mM
SMILES
O=C1C2=C(SCCO)SC(C3=NC=CS3)=C2CC(C)(C)C1
InChi Code
InChI=1S/C15H17NO2S3/c1-15(2)7-9-11(10(18)8-15)14(20-6-4-17)21-12(9)13-16-3-5-19-13/h3,5,17H,4,6-8H2,1-2H3
InChi Key
QILRYFCEXLFIDS-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $121

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    10 mg

    $215

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    25 mg

    $505

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    Product Description

    TB 21007 is an inverse agonist of α5β3γ2 subunit-containing GABAA receptors (Ki = 1.6 nM).1 It selectively inhibits α5β3γ2 subunit-containing GABAA receptors over α1-4 and α6 subunit-containing GABAA receptors that also contain β3 and γ2 subunits (Kis = 20, 16, 20, 106, and 1,800 nM, respectively). TB 21007 reduces the latency to find the hidden platform in a matching-to-place variant of the Morris water maze, indicating enhanced spatial memory, in rats when administered at a dose of 0.3 mg/kg. It reduces paw tactile allodynia induced by reserpine (Item No. 16474) in a rat model of fibromyalgia-like pain when administered intrathecally at doses of 1.5, 15, and 150 nmol.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Chambers, M.S., Atack, J.R., Broughton, H.B., et al. Identification of a novel, selective GABAA α5 receptor inverse agonist which enhances cognition. J. Med. Chem. 46(11), 2227-2240 (2003).

    2. Buchwaldt, L., and Green, H. Phytotoxicity of destruxin B and its possible role in the pathogenesis of Alternaria brassicae. Plant Pathol. 41(1), 55-63 (1992).