BCATc Inhibitor 2

SKU: orb1306112

Description

BCATc Inhibitor 2

Research Area

Metabolism Research; Pharmacology & Drug Discovery

Key Properties

• CAS Number: 406191-34-2
• MW: 418.77
• Purity: 98.80% (May vary between batches)
• Formula: C₁₆H₁₀ClF₃N₂O₄S
• SMILES: FC(F)(F)c1ccccc1S(=O)(=O)NNC(=O)c1cc2cc(Cl)ccc2o1
• Target: Others
• Solubility: 10% DMSO+90% Corn Oil:2.5 mg/mL (5.97 mM);DMSO:65 mg/mL (155.22 mM)

Bioactivity

• Target IC50:
  BCATc (human):0.8 μM (IC50)|BCATm (rat):3.0 μM (IC50)|BCATc (rat):0.2 μM (IC50)
• In Vivo:
  BCATc Inhibitor 2 blocked calcium influx into neuronal cells following inhibition of glutamate uptake, and demonstrated neuroprotective efficacy in vivo. In Lewis rats, after treatment with 30 mg/kg BCATc Inhibitor 2 (subcutaneous injection), the peak plasma concentration (Cmax) reached 8.28 μg/ml at 0.5 h (tmax). The mean plasma exposure (AUC) value was 19.9 μg h/ml, and the mean terminal half-life ranged from 12 to 15 h, indicating favorable PK parameters of BCATc Inhibitor 2. Daily administration of the mitochondrial neurotoxin, 3-nitroproprionic acid (3-NP) produced striatal lesions and led to motor deficits. Administration of BCATc Inhibitor 2 for 9 days almost completely reversed the effects of 3-NP .
• In Vitro:
  BCATc inhibition is likely to be useful for the treatment of neurodegenerative and other neurological disorders involving disturbances of the glutamatergic system. In the hBCATc assays, BCATc Inhibitor 2 exhibited an IC50 of 0.8 ± 0.05 μM. In a recombinant rat BCATc assay and a crude rat BCATm assay, the IC50 was 0.2 μM ± 0.02 and 3.0 μM ± 0.5 (n=5), respectively. BCATc Inhibitor 2 decreased calcium influx in neuronal cultures with an IC50 of 4.8 ± 1.2 μM (n=4) .

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

disease, cytosolic, BCATc Inhibitor 2, BCATc Inhibitor2, BCATc Inhibitor-2, BCAT, neurodegenerative, mitochondrial, inhibit, hBCATc, Inhibitor, human, rBCATm, rBCATc

Compound Identifiers

PubChem CID

6914573