NNC 05-2090 hydrochloride

SKU: orb1704295

Description

NNC 05-2090 hydrochloride is a selective inhibitor of the betaine/GABA transporter BGT-1 (IC₅₀ = 10.6 µM). This compound serves as a pharmacological tool for investigating the role of BGT-1 in epilepsy and related neurological disorders in both in vitro and in vivo experimental models.

Research Area

Metabolism Research, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 184845-18-9
• MW: 451
• Purity: 99.11%
• Formula: C₂₇H₃₁ClN₂O₂
• SMILES: Cl.OC1(C=2C=CC=CC2OC)CCN(CCCN3C=4C=CC=CC4C=5C=CC=CC53)CC1
• Target: GABA Receptor,Transaminase
• Solubility: DMSO:50 mg/mL (110.86 mM);Ethanol:< 5.64 mg/mL

Bioactivity

• In Vivo:
  NNC05-2090 hydrochloride (i.p.; PSL mice) dose-dependently protects mice from maximal electric shock (MES) ED50 of 73 μmol/kg and against tonic and clonic convulsions in DBA/2 mice with an ED50 of 19 μmol /kg and 26 μmol/kg. NNC05-2090 hydrochloride (0.01, 0.1, 0.3 mg/kg; intraperitoneal or intrathecal injection; once) can dose-dependently reverse mechanical allodynia in PSL model mice by both intraperitoneal injection and intrathecal injection.
• In Vitro:
  NNC05-2090 hydrochloride binds to prazosin and spiperone with IC50 values of 266 nM and 1632 nM, respectively. NNC05-2090 hydrochloride (0.1-100 μM) inhibits [3H]GABA uptake in rat cortical synaptosomes with an IC50 value of 4.4 μM. NNC05-2090 hydrochloride (0.1-100 μM) inhibits [3H]GABA uptake in inferior colliculus synaptosomes with an IC50 value of 2.5 μM. NNC05-2090 hydrochloride inhibits serotonin, norepinephrine, dopamine transporter, and BGT-1 with IC50 values of 5.29, 7.91, 4.08, and 10.6 μM respectively. NNC05-2090 hydrochloride inhibits GAT-1, GAT-2 and GAT-3 with IC50s of 29.62, 45.29 and 22.51 μM respectively.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NNC 05 2090 hydrochloride, NNC 052090 hydrochloride, NNC 05-2090 Hydrochloride, GABA Receptor, GABA transaminase, GABAReceptor

Compound Identifiers

PubChem CID

18782760