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2g |
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10g |
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25g |
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50g |
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100g |
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Other Sizes |
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Purity: ≥98%
Dibucaine HCl (also known as Cinchocaine), a sodium channel inhibitor, is one of the most potent and toxic of the long-acting local anesthetics. Dibucaine is the active ingredient in some topical hemorrhoid creams such as Proctosedyl. It is also a component of the veterinary drug Somulose, used for euthanasia of horses and cattle. Dibucaine HCl blocks both the initiation and conduction of nerve impulses by decreasing the neuronal membrane's permeability to sodium ions. This reversibly stabilizes the membrane and inhibits depolarization, resulting in the failure of a propagated action potential and subsequent conduction blockade.
ln Vitro |
Cruzipain expression levels are not decreased or the parasite's total proteolytic activity is not inhibited when dibucaine (cinchaine) decreases the breakdown of BSA-gold complexes in depots [1]. Within two minutes, the quaternary ammonium compound dibucaine reversibly suppresses SChE to very low levels. Inhibition works incredibly well. For BuTch, the IC(50) is 5.3 microM, and for AcTch, it is 3.8 microM. When compared to AcTch, the inhibition constant is linear mixed (competitive/non-competitive), with inhibition constants K(i) and K(I) of 0.66 and 2.5 microM, respectively. In contrast, the inhibition is competitive when compared to BuTch, with K(i) being 1.3 microM. Dibucaine's butoxy side chain is longer than AcTch's ethylene group and resembles the butyl group of BuTch [2].
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References |
[1]. Souto-Padron, T., A.P. Lima, and O. Ribeiro Rde, Effects of dibucaine on the endocytic/exocytic pathways in Trypanosoma cruzi. Parasitol Res, 2006. 99(4): p. 317-20.
[2]. Elamin, B., Dibucaine inhibition of serum cholinesterase. J Biochem Mol Biol, 2003. 36(2): p. 149-53. |
Molecular Formula |
C20H29N3O2
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Molecular Weight |
343.46
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Exact Mass |
343.22598
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CAS # |
85-79-0
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Related CAS # |
Dibucaine hydrochloride;61-12-1
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SMILES |
O(C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H])C1C([H])=C(C(N([H])C([H])([H])C([H])([H])N(C([H])([H])C([H])([H])[H])C([H])([H])C([H])([H])[H])=O)C2=C([H])C([H])=C([H])C([H])=C2N=1
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InChi Key |
PUFQVTATUTYEAL-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C20H29N3O2/c1-4-7-14-25-19-15-17(16-10-8-9-11-18(16)22-19)20(24)21-12-13-23(5-2)6-3/h8-11,15H,4-7,12-14H2,1-3H3,(H,21,24) SMILES
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Chemical Name |
2-butoxy-N-[2-(diethylamino)ethyl]quinoline-4-carboxamide
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Synonyms |
Dibucaine Cinchocaine Nupercainal Nupercaine Sovcaine Dibucaine Base
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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) |
DMSO : ~100 mg/mL (~291.15 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.28 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 (7.28 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.9115 mL | 14.5577 mL | 29.1155 mL | |
5 mM | 0.5823 mL | 2.9115 mL | 5.8231 mL | |
10 mM | 0.2912 mL | 1.4558 mL | 2.9115 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.