SKF 89976A hydrochloride

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Cat.No. 1081 - SKF 89976A hydrochloride | C22H25NO2.HCl | CAS No. 85375-15-1
Description: Potent GAT-1 inhibitor; brain penetrant
Chemical Name: 1-(4,4-Diphenyl-3-butenyl)-3-piperidinecarboxylic acid hydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations (1)
Reviews
Literature (5)

Biological Activity

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.

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 Data

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.

Select a batch to recalculate based on the batch molecular weight:
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.

Ali et al (1985) Orally active and potent inhibitors of γ-aminobutyric acid. J.Med.Chem. 28 653 PMID: 2985785

Krause and Schwarz (2005) Identification and selective inhibition of the channel mode of the neuronal GABA transporter 1. Mol.Pharmacol. 68 1728 PMID: 16150932

Murali Dha (1996) On the bioactive conformation of the GABA uptake inhibitor SK&F 89976-A. Bioorg.Med.Chem.Lett. 6 1535


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1 Citation for SKF 89976A hydrochloride

Citations are publications that use Tocris 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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