Biological Activity
GABA uptake inhibitor that displays moderate selectivity for BGT-1 (mGAT-2) transporters (Ki values are 1.4, 15, 19 and 41 μM for hBGT-1, hGAT-3, hGAT-1 and hGAT-2 respectively). Anticonvulsive; inhibits sound-induced tonic and clonic convulsions in DBA/2 mice. Also displays affinity at α1- and D2-receptors (IC50 values are 266 and 1632 nM respectively).
Compound Libraries
NNC 05-2090 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 451.01 |
| Formula | C27H30N2O2.HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 184845-18-9 |
| PubChem ID | 18782760 |
| InChI Key | WDFXPKKFSNMGOO-UHFFFAOYSA-N |
| Smiles | Cl.COC1=C(C=CC=C1)C1(O)CCN(CCCN2C3=C(C=CC=C3)C3=C2C=CC=C3)CC1 |
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 | 45.1 | 100 | |
| ethanol | 5.64 | 12.5 |
Preparing Stock Solutions
The following data is based on the product molecular weight 451.01. 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 | 2.22 mL | 11.09 mL | 22.17 mL |
| 5 mM | 0.44 mL | 2.22 mL | 4.43 mL |
| 10 mM | 0.22 mL | 1.11 mL | 2.22 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Thomsen et al (1997) 1-(3-(9H-carbazol-9-yl)-1-propyl)-4-(2-methoxyphenyl)-4-piperidinol, a novel subtype selective inhibitor of the mouse type II GABA-transporter. Br.J.Pharmacol. 120 983 PMID: 9134205
Dalby et al (1997) Anticonvulsive properties of two GABA uptake inhibitors NNC 05-2045 and NNC 05-2090, not acting preferentially on GAT-1. Epilepsy Res. 28 51 PMID: 9255599
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