SKF 89976A hydrochloride

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1081/10
1081/50
SKF 89976A hydrochloride | CAS No. 85375-15-1 | GABA Transporter Inhibitors
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Description: Potent GAT-1 inhibitor; brain penetrant

Chemical Name: 1-(4,4-Diphenyl-3-butenyl)-3-piperidinecarboxylic acid hydrochloride

Purity: ≥99%

Product Details
Citations (1)
Reviews

Biological Activity

SKF 89976A hydrochloride is a potent GABA uptake inhibitor, selective for GAT-1 (IC50 values are 0.13, 550, 944 and 7210 μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1 respectively). Inhibits transport current competitively (Ki = 7 μM) and transmitter-gated current non-competitively (Ki = 0.03 nM). Able to pass the blood-brain barrier after systemic administration and is active in vivo.

Technical Data

M.Wt:
371.91
Formula:
C22H25NO2.HCl
Solubility:
Soluble to 100 mM in water with gentle warming and to 100 mM in DMSO
Purity:
≥99%
Storage:
Desiccate at +4°C
CAS No:
85375-15-1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold with the permission of GlaxoSmithKline

Background References

  1. High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
    Fox JT, Sakamuru S, Huang R
    Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8.
  2. Orally active and potent inhibitors of γ-aminobutyric acid.
    Ali et al.
    J.Med.Chem., 1985;28:653
  3. Identification and selective inhibition of the channel mode of the neuronal GABA transporter 1.
    Krause and Schwarz
    Mol.Pharmacol., 2005;68:1728
  4. On the bioactive conformation of the GABA uptake inhibitor SK&F 89976-A.
    Murali Dha
    Bioorg.Med.Chem.Lett., 1996;6:1535

Product Datasheets

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Citation for SKF 89976A hydrochloride

The citations listed below are publications that use Tocris products. Selected citations for SKF 89976A hydrochloride include:

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