SKF 89976A hydrochloride
Tocris Bioscience, part of Bio-Techne | Catalog # 1081
Potent GAT-1 inhibitor; brain penetrant
Key Product Details
Description
Potent GAT-1 inhibitor; brain penetrant
Product Description
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.Licensing Information
Sold with the permission of GlaxoSmithKlineProduct Specifications
Molecular Weight
371.91
Formula
C22H25NO2.HCl
Storage
Desiccate at +4°C
Purity
≥98% (HPLC)
Chemical Name
1-(4,4-Diphenyl-3-butenyl)-3-piperidinecarboxylic acid hydrochloride
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 100 with gentle warming | ||
| DMSO | 37.19 | 100 |
Preparing Stock Solutions
for SKF 89976A hydrochloride
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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background 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
Product Specific Notices for SKF 89976A hydrochloride
For research use only
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