SKF 89976A hydrochloride

Name: SKF 89976A hydrochloride
Brand: Tocris Bioscience
SKU: 1081

Tocris Bioscience, part of Bio-Techne | Catalog # 1081

Citations (8)

COA / SDS

Potent GAT-1 inhibitor; brain penetrant

Key Product Details

Chemical Name:	1-(4,4-Diphenyl-3-butenyl)-3-piperidinecarboxylic acid hydrochloride
Purity:	≥99%
Molecular Weight:	371.91 kDa

View Full Technical Details for SKF 89976A hydrochloride

Technical Data
Citations

Biological Activity for SKF 89976A hydrochloride

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 (K_i = 7 μM) and transmitter-gated current non-competitively (K_i = 0.03 nM). Able to pass the blood-brain barrier after systemic administration and is active in vivo.

Technical Data for SKF 89976A hydrochloride

M. Wt	371.91 kDa
Formula	C₂₂H₂₅NO₂.HCl
Storage	Desiccate at +4°C
Purity	≥99%
CAS Number	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.

Solubility for SKF 89976A hydrochloride

Solubility

Soluble Soluble to 100 mM in water with gentle warming and to 100 mM in DMSO

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References for SKF 89976A hydrochloride

References are publications that support the biological activity of the product.

Fox JT, Sakamuru S, Huang R High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death. Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8. 2012 PMID: 22431602
Ali et al. Orally active and potent inhibitors of γ-aminobutyric acid. J.Med.Chem., 1985;28:653 PMID: 2985785
Krause and Schwarz Identification and selective inhibition of the channel mode of the neuronal GABA transporter 1. Mol.Pharmacol., 2005;68:1728 PMID: 16150932
Murali Dha On the bioactive conformation of the GABA uptake inhibitor SK&F 89976-A. Bioorg.Med.Chem.Lett., 1996;6:1535