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Technical Data
| Formula | C18H28N2O.HCl |
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| Molecular Weight | 324.89 | CAS No. | 18010-40-7 | |
| Solubility (25°C)* | In vitro | DMSO | 65 mg/mL (200.06 mM) | |
| Ethanol | 65 mg/mL (200.06 mM) | |||
| Water | 23 mg/mL (70.79 mM) | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Preparing Stock Solutions
Biological Activity
| Description | Bupivacaine HCl binds to the intracellular portion of voltage-gated sodium channels and blocks sodium influx into nerve cells, used for treating cardiac arrhythmias. | |
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| Targets |
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| In vitro | Bupivacaine solution is cytotoxic to bovine articular chondrocytes and articular cartilage in vitro after only 15 to 30 minutes exposure. [1] Bupivacaine acts in isolated mitochondria, as uncouplers between oxygen consumption and phosphorylation of adenosine diphosphate. [2] Bupivacaine causes a concentration-dependent mitochondrial depolarization and pyridine nucleotide oxidation in isolated mitochondria, which are matched by an increased oxygen consumption at bupivacaine concentrations of 1.5 mm or less at pH 7.4, whereas respiration is inhibited at higher concentrations. Bupivacaine causes the opening of the permeability transition pore (PTP), a cyclosporin A-sensitive inner membrane channel that plays a key role in many forms of cell death. Bupivacaine causes mitochondrial depolarization and pyridine nucleotides oxidation that are matched by increased concentrations of cytosolic free Ca(2+), release of cytochrome c, and eventually, hypercontracture in intact flexor digitorum brevis fibers. [3] Bupivacaine inhibits GIRK channels within seconds of application, regardless of whether channels are activated through the muscarinic receptor or directly via coexpressed G protein G(beta)gamma subunits. Bupivacaine also inhibits alcohol-induced GIRK currents in the absence of functional pertussis toxin-sensitive G proteins. [4] Bupivacaine HCl also potently inhibits cAMP production with an IC50 of 2.3 μM.[6] | |
| In vivo | Bupivacaine does not only induce Ca2+ release from the sarcoplasmic reticulum (SR) in rats, but also inhibits Ca2+ uptake by the SR, which is mainly regulated by SR Ca2+ adenosine triphosphatase activity. [5] |
Protocol (from reference)
References
Selleck's Bupivacaine HCl has been cited by 4 publications
| Role of the G-Protein-Coupled Receptor Signaling Pathway in Insecticide Resistance. [ Int J Mol Sci, 2019, 20(17)] | PubMed: 31484301 |
| Butyric acid regulates progesterone and estradiol secretion via cAMP signaling pathway in porcine granulosa cells [Lu N J Steroid Biochem Mol Biol, 2017, 172:89-97] | PubMed: 28602959 |
| A G-protein-coupled receptor regulation pathway in cytochrome P450-mediated permethrin-resistance in mosquitoes, Culex quinquefasciatus [ Sci Rep, 2015, 5:17772] | PubMed: 26656663 |
| Targeting thyroid hormone receptor beta in triple-negative breast cancer. [ Breast Cancer Res Treat, 2015, 150(3):535-45] | PubMed: 25820519 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.