| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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Purity: ≥98%
Proparacaine HCl (Proxymetacaine; Proxymetacaine), the hydrochloride salt of proparacaine, is a voltage-gated sodium channels antagonist approved as an ophthalmic solution for topical anesthetic use in ophthalmic practice. It inhibits voltage-gated sodium channels with ED50 of 3.4 mM. Proparacaine is more potent and less toxic than cocaine. Proparacaine significantly increases in FHV-1, C. felis, and 28S rDNA Ct values when fusidic acid is used. Proparacaine inhibits corneal epithelial migration and adhesion through alteration of the actin cytoskeleton. Proparacaine acts like bupivacaine or lidocaine and produces dose-related spinal blockades of motor function, proprioception and nociception.
| ln Vitro |
Proparacaine Hydrochloride (>588.93 μM; 4-28 hours) has a dose- and time-dependent cytotoxicity to HCS cells at concentrations in vitro[1]. Proparacaine Hydrochloride (294.47-18.85 mM; 4-12 hours) can induce apoptosis of HCS 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 [1]. Proparacaine hydrochloride causes disruption of the mitochondrial transmembrane potential as well as activation of caspase -2, -3, and -9[1]. 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[1].
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| ln Vivo |
When administered intranasally for seven days, proparacaine hydrochloride (75 μg/30 μL) dramatically reduces the amount of mast cells, goblet cells, and eosinophils in the nasal mucosa's lamina propria[2].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: HCS cells Tested Concentrations: 294.47 μM, 588.93 μM, 1.18 mM, 2.35 mM, 4.71 mM, 9.42 mM, 18.85 mM Incubation Duration: 4 hrs (hours), 8 hrs (hours), and 12 hrs (hours), 16 hrs (hours), 20 hrs (hours), 24 hrs (hours), 28 hrs (hours) Experimental Results: diminished the viability of HCS cells with concentration and time at concentrations above 588.93 μM. Apoptosis Analysis[1] Cell Types: HCS cells Tested Concentrations: 294.47 μM, 588.93 μM, 1.18 mM, 2.35 mM, 4.71 mM, 9.42 mM, 18.85 mM Incubation Duration: 4 hrs (hours), 8 hrs (hours), and 12 hrs (hours) Experimental Results: Induced apoptosis of HCS cells. Cell Cycle Analysis[1] Cell Types: HCS cells Tested Concentrations: 4.71 mM Incubation Duration: 4 hrs (hours), 8 hrs (hours), and 12 hrs (hours) Experimental Results: Arrested HCS cells at the G1 phase of the cell cycle. Western Blot Analysis[1] Cell Types: HCS cells Tested Concentrations: 4.71 mM Incubation Duration: 4 hrs (hours), 8 hrs (hours), and 12 hrs (hours) Experimental Results: Down-regulated the expression level of anti-apoptotic protein Bcl-xL and up-regulated the pro-apoptotic protein Bax, whereas Dramatically up-regulated the cytopl |
| Animal Protocol |
Animal/Disease Models: 7-week- old female balb/c (Bagg ALBino) mouse, allergic rhinitis model[2]
Doses: 75 μg/30 μL Route of Administration: Intranasal administration, for 7 days Experimental Results: Dramatically decreased nasal rubbing and sneezing. |
| References |
[1]. Wen Yi Fan, et al. Proparacaine induces cytotoxicity and mitochondria-dependent apoptosis in corneal stromal cells both in vitro and in vivo. Toxicol Res (Camb). 2016 Sep 1; 5(5): 1434-1444.
[2]. Hwan Soo Kim, et al. Effect of Proparacaine in a Mouse Model of Allergic Rhinitis. Clin Exp Otorhinolaryngol. 2017 Dec; 10(4): 325–331. |
| Molecular Formula |
C16H26N2O3.HCL
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| Molecular Weight |
330.85
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| CAS # |
5875-06-9
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| Related CAS # |
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| SMILES |
O=C(OCCN(CC)CC)C1=CC=C(OCCC)C(N)=C1.[H]Cl
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.56 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.56 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.56 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: Saline: 30 mg/mL Solubility in Formulation 5: 60 mg/mL (181.35 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0225 mL | 15.1126 mL | 30.2252 mL | |
| 5 mM | 0.6045 mL | 3.0225 mL | 6.0450 mL | |
| 10 mM | 0.3023 mL | 1.5113 mL | 3.0225 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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