Galanthamine HBr

SKU: orb1225785

Description

Galanthamine hydrobromide is a long-acting, centrally active acetylcholinesterase(AChE) inhibitor (IC50 = 410 nM) and allosteric potentiator at neuronal nicotinic ACh receptors.(In Vitro):Galanthamine hydrobromide is 53-fold selectivity for AChE over butyrylcholinesterase.Galanthamine hydrobromide (25-1000 μM) inhibits both Aβ 1-40 (50 μM) and Aβ 1-42 (50 μM) aggregation.Galanthamine hydrobromide (25-1000 μM) protects against Aβ(1-40) and Aβ(1-42) toxicity in SH-SY5Y cells.Galanthamine hydrobromide also dramatically reduces Aβ(1-40)-induced cellular apoptosis.(In Vivo):Galanthamine hydrobromide (1.25-2.5 mg/kg; i.p. ) reduces cognitive deficits in APP23 mice.Galanthamine hydrobromide (10 mg/kg; i.g.) displays short elimination half-life of approximately 2 h in wild-type mice.

Key Properties

• CAS Number: 1953-04-4
• MW: 368.27
• Purity: >98% (HPLC)
• Formula: C₁₇H₂₁NO₃·HBr
• SMILES: CN1CC[C@@]23C=C[C@@H](C[C@@H]2OC4=C(C=CC(=C34)C1)OC)O.Br
• Target: AChR
• Solubility: Water: 36 mg/mL (97.75 mM)

Bioactivity

• In Vivo:
  Galanthamine hydrobromide (1.25-2.5 mg/kg; i.p.) reduces cognitive deficits in APP23 mice. Galanthamine hydrobromide (10 mg/kg; i. g.) displays short elimination half-life of approximately 2 h in wild-type mice. Animal model: APP23 mice. Dosage: 1.25 mg/kg, 2.5 mg/kg. Administration: Intraperitoneal injection, daily, 1 week. Result: Effectively remedied the spatial learning deficit. Animal model: Female 57B1/6J wild type. Dosage: 10 mg/kg. Administration: Oral gavage (Pharmacokinetic Analysis). Result: Cmax (0.31 μg/mL), t1/2β (1.6 h), AUC0-24h (0.67 μg h/mL).
• In Vitro:
  Galanthamine hydrobromide is 53-fold selectivity for AChE over butyrylcholinesterase. Galanthamine hydrobromide (25-1000 μM) inhibits both Aβ 1-40 (50 μM) and Aβ 1-42 (50 μM) aggregation. Galanthamine hydrobromide (25-1000 μM) protects against Aβ(1-40) and Aβ(1-42) toxicity in SH-SY5Y cells. Galanthamine hydrobromide also dramatically reduces Aβ(1-40)-induced cellular apoptosis.

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

AChR