SKF 89976A hydrochloride

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

Catalog # 1081

Citations (1)

COA / SDS

Order Information

Bio-Techne Corporation

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$35 to United States

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Key Product Details

Description:	Potent GAT-1 inhibitor; brain penetrant
Chemical Name:	1-(4,4-Diphenyl-3-butenyl)-3-piperidinecarboxylic acid hydrochloride
Purity:	≥99% (HPLC)
Molecular Weight:	371.91

View Full Technical Details for SKF 89976A hydrochloride

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 (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.

Licensing Information

Sold with the permission of GlaxoSmithKline

Compound Libraries

SKF 89976A hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	371.91
Formula	C₂₂H₂₅NO₂.HCl
Storage	Desiccate at +4°C
Purity	≥99% (HPLC)
CAS Number	85375-15-1
PubChem ID	6917797
InChi Key	SNGGBKYQZVAQKA-UHFFFAOYSA-N
Smiles	Cl[H].OC(=O)C1CCCN(CC\C=C(\C2=CC=CC=C2)C2=CC=CC=C2)C1

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

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	water		100 with gentle warming
	DMSO	37.19	100

Preparing Stock Solutions

The following data is based on the product molecular weight 371.91.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.69 mL	13.44 mL	26.89 mL
5 mM	0.54 mL	2.69 mL	5.38 mL
10 mM	0.27 mL	1.34 mL	2.69 mL
50 mM	0.05 mL	0.27 mL	0.54 mL

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References

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

Krause and Schwarz Identification and selective inhibition of the channel mode of the neuronal GABA transporter 1. Mol.Pharmacol. 2005 PMID: 16150932
Murali Dha On the bioactive conformation of the GABA uptake inhibitor SK&F 89976-A. Bioorg.Med.Chem.Lett.
Ali Orally active and potent inhibitors of γ-aminobutyric acid. J.Med.Chem. 1985 PMID: 2985785

Citations for SKF 89976A hydrochloride (1)

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Citations are publications that use Bio-Techne products. Selected citations for SKF 89976A hydrochloride include:

Sousa et al. (2011) Regulation of hippocampal cannabinoid CB1 receptor actions by adenosine A1 receptors and chronic caffeine administration: implications for the effects of δ9-tetrahydrocannabinol on spatial memory. Neuropsychopharmacology. 36:472
PMID: 20927050

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