Size | Price | Stock | Qty |
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500mg |
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1g |
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2g |
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5g |
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10g |
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100g |
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Other Sizes |
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Purity: ≥98%
Procaine HCl (also known as Novocaine; Gerovital H3; Aminocaine), the HCl salt of Procaine, is a local anesthetic that acts as an inhibitor of sodium channel, NMDA receptor and nAChR with IC50 of 60 μM, 0.296 mM and 45.5 μM. Procaine is also an inhibitor of 5-HT3 with KD of 1.7 μM. Procaine acts mainly by inhibiting sodium influx through voltage gated sodium channels in the neuronal cell membrane of peripheral nerves. Procaine has also been shown to bind or antagonize the function of N-methyl-D-aspartate (NMDA) receptors as well as nicotinic acetylcholine receptors and the serotonin receptor-ion channel complex.
ln Vitro |
Procaine hydrochloride (0.01-100 microM) reduced the 5-HT3 receptor-mediated inward current in the whole-cell patch clamp recording. Procaine appears to produce a competitive inhibition on 5-HT3 receptors with a KD of 1.7 microM[1]. is a DNA-demethylating chemical that produces a 40% reduction in 5-methylcytosine DNA concentration as assessed by high-performance capillary electrophoresis or total DNA enzyme digestion. Procaine can also demethylate heavily hypermethylated CpG islands. Procaine also exhibits growth-inhibitory actions in malignant cancer cells, producing mitotic arrest[2]. Procaine serves as an excitant of limbic system cells, and that procaine changes synaptic transmission in some, but not all, output pathways from the amygdale[3].
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ln Vivo |
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Animal Protocol |
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References |
[1]. Fan, P. and F.F. Weight, Procaine impairs the function of 5-HT3 receptor-ion channel complex in rat sensory ganglion neurons. Neuropharmacology, 1994. 33(12): p. 1573-9.
[2]. Villar-Garea, A., et al., Procaine is a DNA-demethylating agent with growth-inhibitory effects in human cancer cells. Cancer Res, 2003. 63(16): p. 4984-9. [3]. Adamec, R.E. and C. Stark-Adamec, The effects of procaine HCl on population cellular and evoked response activity within the limbic system of the cat. Evidence for differential excitatory action of procaine in a variety of limbic circuits. Prog Neuropsychopharmacol Biol Psychiatry, 1987. 11(4): p. 345-64. |
Molecular Formula |
C13H20N2O2.HCL
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Molecular Weight |
272.77
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CAS # |
51-05-8
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Related CAS # |
Procaine;59-46-1;Procaine-d4 hydrochloride
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SMILES |
O(C(C1C([H])=C([H])C(=C([H])C=1[H])N([H])[H])=O)C([H])([H])C([H])([H])N(C([H])([H])C([H])([H])[H])C([H])([H])C([H])([H])[H]
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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: 130 mg/mL (476.59 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
 (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.6661 mL | 18.3305 mL | 36.6609 mL | |
5 mM | 0.7332 mL | 3.6661 mL | 7.3322 mL | |
10 mM | 0.3666 mL | 1.8330 mL | 3.6661 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.