Phenoxybenzamine hydrochloride

SKU: orb1224377

Description

Phenoxybenzamine HCl is a non-specific, irreversible alpha antagonist with long duration of action.(In Vitro):Phenoxybenzamine hydrochloride (0-100 μM; 96 h) markedly inhibits U251 and U87MG cells proliferation.Phenoxybenzamine hydrochloride (10 μM; 24 h or 72 h) inhibits migration and invasion of U251 and U87MG cells.Phenoxybenzamine hydrochloride (10 μM; 12 h) activates LINGO-1 and inhibits the TrkB-Akt pathway.Phenoxybenzamine (0.1 μM-1 mM; 0-16 h) prevents hippocampal cell death after oxygen glucose deprivation.(In Vivo):Phenoxybenzamine hydrochloride (20 nM; s.c.; 2-day interval for 26 days) shows anti-tumorigenic effect in mice.Phenoxybenzamine (1.0 mg/kg; i.v.; daily for 30 days) is neuroprotective in a rat model of severe traumatic brain injury.

Key Properties

• CAS Number: 63-92-3
• MW: 340.3
• Purity: >98% (HPLC)
• Formula: C₁₈H₂₃Cl₂NO
• SMILES: Cl.CC(COC1=CC=CC=C1)N(CCCl)CC1=CC=CC=C1
• Target: Adrenergic Receptor
• Solubility: Ethanol: 68 mg/mL (199.82 mM); Water: 17 mg/mL (49.95 mM); DMSO: 68 mg/mL (199.82 mM)

Bioactivity

• In Vivo:
  Phenoxybenzamine hydrochloride (20 nM; s. c. ; 2-day interval for 26 days) shows anti-tumorigenic effect in mice. Phenoxybenzamine (1.0 mg/kg; i. v. ; daily for 30 days) is neuroprotective in a rat model of severe traumatic brain injury. Animal model: Nude mice, U87MG tumor model. Dosage: 20 nM. Administration: Subcutaneous injection, 2-day interval for 26 days. Result: Reduced the tumor cells. Animal model: Male Wistar rats (350–500 g), traumatic brain injury (TBI) model. Dosage: 1.0 mg/kg. Administration: Intravenous injection, daily for 30 days. Result: Showed significant improvements in neurological severity score (NSS) and foot fault scoring on days 14, 21, and 30. Reduced cognitive impairment associated with severe TBI and reduced the expression of pro-inflammatory genes.
• In Vitro:
  Phenoxybenzamine hydrochloride (0-100 μM; 96 h) markedly inhibits U251 and U87MG cells proliferation. Phenoxybenzamine hydrochloride (10 μM; 24 h or 72 h) inhibits migration and invasion of U251 and U87MG cells. Phenoxybenzamine hydrochloride (10 μM; 12 h) activates LINGO-1 and inhibits the TrkB-Akt pathway. Phenoxybenzamine (0.1 μM-1 mM; 0-16 h) prevents hippocampal cell death after oxygen glucose deprivation. Cell Proliferation Assay Cell line: U251 and U87MG cells. Concentration: 0.1, 1, 10, 50 and 100 μM Incubation time: 96 h. Result: Cell proliferation was inhibited markedly, the inhibition rate being 26.5 % for U251 cells and 27.3 % for U87MG cells at 10 μM. Cell Migration Assay Cell line: U251 and U87MG cells. Concentration: 10 μM. Incubation time: 24 h. Result: Apparent inhibition on migration was observed, and the inhibition rate was 28.6 and 39.8 % for U251 and U87MG, respectively. Cell Invasion Assay Cell line: U251 and U87MG cells. Concentration: 10 μM. Incubation time: 72 h. Result: Attenuated the invasion properties of both U251 and U87MG markedly, as represented by the number of invaded cells per field declining from 365/field to 132/field (36.2 %) for U251 and 444/field to 298/field (67.1 %) for U87MG. Western blot analysis. Cell line: U251. Concentration: 10 μM. Incubation time: 12 h. Result: Decreased the protein level of TrkB, p-TrkB, and p-Akt, but Akt remained unchanged significantly.

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

Dibenzyline? | NSC 37448

Quick Database Links

Gene Symbol

Adrenergic Receptor