NV-5138

SKU: orb1218474

Description

NV-5138 is a selective and orally active activator of brain mTORC1, with antidepressant effects.

Key Properties

• CAS Number: 2095886-80-7
• MW: 181.18
• Purity: >98% (HPLC)
• Formula: C₇H₁₃F₂NO₂
• SMILES: O=C(O)[C@@H](N)CC(C)(C)C(F)F
• Target: mTOR
• Solubility: In Vitro: DMSO : 10 mg/mL (55.19 mM)

Bioactivity

• In Vivo:
  NV-5138 is found to be essentially 100% orally bioavailable with an elimination half-life in plasma of ~ 3 h determined following intravenous and oral dosing in rats. NV-5138 (160 mg/kg, po, single dose) rapidly increases levels of phospho-mTOR as well as the downstream targets, phospho-p70S6K1, and phosphor-4EB-P1, in synaptosomal preparations of PFC. NV-5138 (80 mg/kg, po, daily for a total of 7 days) also produces antidepressant effects. Animal model: Male Sprague-Dawley rats weighing 250-260 g. Dosage: 40, 80, 160 mg/kg. Administration: PO, single dose (160 mg/kg) or daily for a total of 7 days (40, 80 mg/kg). Result: Produced antidepressant effects. Animal model: Male Sprague–Dawley (SD) rats weighed 250-400 g. Dosage: 1 mg/kg, 5 mg/kg (Pharmacokinetic Design). Administration: I. V at 1 mg/kg and PO at 5 mg/kg. Result: Essentially 100% orally bioavailable with an elimination half-life in plasma of ~ 3 h.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

mTOR