| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| 5g |
|
||
| Other Sizes |
|
Purity: ≥98%
Bupivacaine HCl (AH250; HSDB7790; SKY0402; AH-250; Win-11318; HSDB-7790; SKY-0402; Marcaine), the hydrochloride salt of Bupivacaine, is a potent inhibitor of cAMP production that also binds to the intracellular portion of voltage-gated sodium channels and blocks sodium influx into nerve cells. Bupivacaine is a medication used to freeze tissue in a specific area. It is administered by injecting it into the area, around a nerve that supplies the area, or into the spinal canal's epidural space. It is available mixed with a small amount of epinephrine to make it last longer. Bupivacaine binds to the intracellular portion of voltage-gated sodium channels and blocks sodium influx into nerve cells, which prevents depolarization.
| ln Vitro |
In the spinal dorsal horn, an area intimately associated with central sensitization, bupivacaine hydrochloride blocks NMDA receptor-mediated synaptic transmission [1]. Bupivacaine hydrochloride shifts the half-maximal activation/deactivation membrane potential toward a slightly more negative membrane potential, which has an impact on the voltage dependence of channel activation and steady-state inactivation. The SCN5A channel has an IC50 of 2.18±0.16 μM for bupivacaine hydrochloride, which indicates a slight sensitivity in the inactive state[2]. With an IC50 of 16.5 μM, bupivacaine hydrochloride dose-dependently and reversibly inhibits SK2 channels [3].
|
||
|---|---|---|---|
| ln Vivo |
|
||
| Cell Assay |
Cell Viability Assay[3]
Cell Types: HEK 293 cells transfected with the SK2 gene (transfected cells were named SK2 cells) Tested Concentrations: 10, 100, 1000 µM Incubation Duration: Experimental Results: The IC50 value was 16.5 µM. |
||
| Animal Protocol |
|
||
| References |
[1]. Casati A, et, al. Bupivacaine, levobupivacaine and ropivacaine: are they clinically different? Best Pract Res Clin Anaesthesiol. 2005 Jun;19(2):247-68.
[2]. Dan J, et, al. Inhibition of gastric cancer by local anesthetic bupivacaine through multiple mechanisms independent of sodium channel blockade. Biomed Pharmacother. 2018 Jul;103:823-828. |
| Molecular Formula |
C18H28N2O.HCL
|
|
|---|---|---|
| Molecular Weight |
324.89
|
|
| CAS # |
18010-40-7
|
|
| Related CAS # |
Bupivacaine;38396-39-3;Bupivacaine hydrochloride monohydrate;73360-54-0
|
|
| SMILES |
O=C(C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])N1C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H])N([H])C1C(C([H])([H])[H])=C([H])C([H])=C([H])C=1C([H])([H])[H]
|
|
| InChi Key |
SIEYLFHKZGLBNX-UHFFFAOYSA-N
|
|
| InChi Code |
InChI=1S/C18H28N2O.ClH/c1-4-5-12-20-13-7-6-11-16(20)18(21)19-17-14(2)9-8-10-15(17)3;/h8-10,16H,4-7,11-13H2,1-3H3,(H,19,21);1H
|
|
| Chemical Name |
1-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide hydrochloride
|
|
| Synonyms |
|
|
| 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)
|
| Solubility (In Vitro) |
|
|---|
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0780 mL | 15.3898 mL | 30.7796 mL | |
| 5 mM | 0.6156 mL | 3.0780 mL | 6.1559 mL | |
| 10 mM | 0.3078 mL | 1.5390 mL | 3.0780 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA