Elenbecestat

SKU: orb1218866

Description

Elenbecestat is an effective oral bioutilization and CNS penetrating ACE-1 inhibitor for the treatment of Alzheimer's disease.(In Vitro):Elenbecestat (E2609) is a potent BACE1 inhibitor with an IC50 of ~7 nmol/L in cell-based assay.Elenbecestat has been shown to reduce Ab production in the plasma, brain, and cerebrospinal fluid (CSF) of rodents.(In Vivo):Elenbecestat (E2609; 0.3-30 mg/kg; p.o.) potently inhibits Ab1-40 and Ab1-42 production in the plasma and CSF of non-human primates.Elenbecestat displays the plasma half-life of 12-16 hours after once daily dosing.

Key Properties

• CAS Number: 1388651-30-6
• MW: 437.44
• Purity: >98% (HPLC)
• Formula: C₁₉H₁₈F₃N₅O₂S
• SMILES: C[C@H]1OC[C@]2(c(cc(cc3)NC(c4ncc(C(F)F)nc4)=O)c3F)N=C(N)SC[C@H]12
• Target: BACE
• Solubility: DMSO:250 mg/mL (571.51 mM)

Bioactivity

• In Vivo:
  Elenbecestat (E2609; 0.3-30 mg/kg; p.o.) potently inhibits Ab1-40 and Ab1-42 production in the plasma and CSF of non-human primates. Elenbecestat displays the plasma half-life of 12-16 hours after once daily dosing. Animal model: Cynomolgus monkeys (Pharmacokinetic analysis). Dosage: 0.3 mg/kg; 1 mg/kg; 3 mg/kg; 30 mg/kg. Administration: Oral administration. Result: Potently inhibits Ab1-40 and Ab1-42 production in the plasma and CSF.
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• In Vitro:
  Elenbecestat (E2609) is a potent BACE1 inhibitor with an IC50 of ~7 nmol/L in cell-based assay. Elenbecestat has been shown to reduce Ab production in the plasma, brain, and cerebrospinal fluid (CSF) of rodents.
  Read more...

Storage & Handling

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

Alternative Names

E2609

Quick Database Links

Gene Symbol

BACE