Bupivacaine HCl

製品コードS2454 バッチS245402

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₈H₂₈N₂O.HCl
	分子量	324.89	CAS No.	18010-40-7
Solubility (25°C)*	体外	DMSO	65 mg/mL (200.06 mM)
		Ethanol	65 mg/mL (200.06 mM)
		Water	23 mg/mL (70.79 mM)
* <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.

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生物活性

製品説明	Bupivacaine HCl binds to the intracellular portion of voltage-gated sodium channels and blocks sodium influx into nerve cells, used for treating cardiac arrhythmias.
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]

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参考

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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