SKF 89976A hydrochloride

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

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 Plus. 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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

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 solvent 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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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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 PMID:


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Citations for SKF 89976A hydrochloride

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