Naftopidil

SKU: orb1224628

Description

Naftopidil (INN, marketed under the brand name Flivas) is an antihypertensive drug which acts as a selective α1-adrenergic receptor antagonist or alpha blocker.(In Vitro):Naftopidil suppresses human prostate tumor growth by altering interactions between tumor cells and stroma.Naftopidil (10 μM for PCa cells, 0.1-10 μM for PrSC; 3 days) shows growth inhibitory effects on PCa cells and PrSC.Naftopidil (50 μM for E9 cells, 25 μM for PrSC; 48 hours) increases the level of cell-cycle regulatory protein p27 in E9 cells, but not PrSC.(In Vivo):Naftopidil (10 mg/kg; p.o; daily; for 28 days) decreases microvessel density (MVD) in E9+PrSC tumors mice model.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 57149-07-2
• MW: 392.49
• Purity: >98% (HPLC)
• Formula: C₂₄H₂₈N₂O₃
• SMILES: OC(COC1=C2C=CC=CC2=CC=C1)CN3CCN(C4=CC=CC=C4OC)CC3
• Target: Adrenergic Receptor
• Solubility: DMSO: 79 mg/mL (201.27 mM)

Bioactivity

• In Vivo:
  Naftopidil (10 mg/kg; p. o; daily; for 28 days) decreases microvessel density (MVD) in E9+PrSC tumors mice model. Animal model: Male athymic mice (7-8 weeks), with E9+PrSC xenograft. Dosage: 10 mg/kg. Administration: Oral administration, daily, for 28 days. Result: Decreased tumor weights.
• In Vitro:
  Naftopidil suppresses human prostate tumor growth by altering interactions between tumor cells and stroma. Naftopidil (10 μM for PCa cells, 0.1-10 μM for PrSC; 3 days) shows growth inhibitory effects on PCa cells and PrSC. Naftopidil (50 μM for E9 cells, 25 μM for PrSC; 48 hours) increases the level of cell-cycle regulatory protein p27 in E9 cells, but not PrSC. Cell Proliferation Assay Cell line: PCa cells, PrSC. Concentration: 10 μM (PCa cells); 0.1 μM, 1 μM, 10 μM (PrSC) Incubation time: 3 days. Result: Exhibited growth inhibitory effects on PCa cells and PrSC in dose-dependent manners. Western blot analysis. Cell line: PCa cells, PrSC. Concentration: 50 μM (E9 cells), 25 μM (PrSC). Incubation time: 48 hours. Result: Increased the level of cell-cycle regulatory protein p27 in E9 cells, but not PrSC.

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

Naftopidil | BM-15275 | KT-611 | BM 15275 | KT 611 | BM15275 | KT611 | Flivas

Quick Database Links

Gene Symbol

Adrenergic Receptor