Proparacaine hydrochloride

SKU: orb1224569

Description

An irreversible local anesthetic; inhibits pain sensations that is believed to act as an antagonist on voltage-gated sodium channels.Pain Approved(In Vitro):Proparacaine Hydrochloride (>588.93 μM; 4-28 hours) has a dose- and time-dependent cytotoxicity to HCS cells at concentrations in vitro.Proparacaine Hydrochloride (294.47-18.85 mM; 4-12 hours) can induce apoptosis of HCS cells .Proparacaine Hydrochloride (4.71 mM; 4-12 hours) induces G1 phase arrest, plasma membrane permeability elevation, phosphatidylserine externalization, DNA fragmentation, chromatin condensation, and apoptotic body formation of HCS cells.Proparacaine Hydrochloride induces caspase-2, -3 and -9 activation, and mitochondrial transmembrane potential disruption.Proparacaine Hydrochloride (4.71 mM; 4-12 hours) downregulates and upregulates the expression of Bcl-xL and Bax, respectively, and remarkably upregulates cytoplasmic cytochrome C and apoptosis inducing factor.(In Vivo):Proparacaine Hydrochloride (75 μg/30 μL; intranasal administration; for 7 days) significantly decreases nasal symptoms, number of eosinophils, goblet cells, and mast cells in the lamina propria of the nasal mucosa.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 5875-06-9
• MW: 330.8502
• Purity: >98% (HPLC)
• Formula: C₁₆H₂₇ClN₂O₃
• SMILES: CCCOC1=C(C=C(C=C1)C(=O)OCCN(CC)CC)N.Cl
• Target: Sodium Channel
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  Proparacaine Hydrochloride (75 μg/30 μL; intranasal administration; for 7 days) significantly decreases nasal symptoms, number of eosinophils, goblet cells, and mast cells in the lamina propria of the nasal mucosa. Animal model: 7-week-old female BALB/c mice, allergic rhinitis model. Dosage: 75 μg/30 μL. Administration: Intranasal administration, for 7 days. Result: Significantly reduced nasal rubbing and sneezing.
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• In Vitro:
  Proparacaine Hydrochloride (>588.93 μM; 4-28 hours) has a dose- and time-dependent cytotoxicity to HCS cells at concentrations in vitro. Proparacaine Hydrochloride (294.47-18.85 mM; 4-12 hours) can induce apoptosis of HCS cells. Proparacaine Hydrochloride (4.71 mM; 4-12 hours) induces G1 phase arrest, plasma membrane permeability elevation, phosphatidylserine externalization, DNA fragmentation, chromatin condensation, and apoptotic body formation of HCS cells. Proparacaine Hydrochloride induces caspase-2, -3 and -9 activation, and mitochondrial transmembrane potential disruption. Proparacaine Hydrochloride (4.71 mM; 4-12 hours) downregulates and upregulates the expression of Bcl-xL and Bax, respectively, and remarkably upregulates cytoplasmic cytochrome C and apoptosis inducing factor. Cell Viability Assay Cell line: HCS cells. Concentration: 294.47 μM, 588.93 μM, 1.18 mM, 2.35 mM, 4.71 mM, 9.42 mM, 18.85 mM Incubation time: 4 hours, 8 hours, and 12 hours, 16 hours, 20 hours, 24 hours, 28 hours. Result: Decreased the viability of HCS cells with concentration and time at concentrations above 588.93 μM. Apoptosis Analysis Cell line: HCS cells. Concentration: 294.47 μM, 588.93 μM, 1.18 mM, 2.35 mM, 4.71 mM, 9.42 mM, 18.85 mM Incubation time: 4 hours, 8 hours, and 12 hours. Result: Induced apoptosis of HCS cells. Cell Cycle Analysis Cell line: HCS cells. Concentration: 4.71 mM Incubation time: 4 hours, 8 hours, and 12 hours. Result: Arrested HCS cells at the G1 phase of the cell cycle. Western blot analysis. Cell line: HCS cells. Concentration: 4.71 mM Incubation time: 4 hours, 8 hours, and 12 hours. Result: Down-regulated the expression level of anti-apoptotic protein Bcl-xL and up-regulated the pro-apoptotic protein Bax, whereas significantly up-regulated the cytoplasmic amounts of mitochondria-released cytochrome C and apoptosis-inducing factor (AIF).
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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

Proxymetacaine hydrochloride

Quick Database Links

Gene Symbol

Sodium Channel