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Bupivacaine HCl(HSDB 7790)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Bupivacaine HCl(HSDB 7790)图片
CAS NO:18010-40-7
规格:≥98%
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议
1g电议
5g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)324.89
FormulaC18H28N2O.HCl
CAS No.18010-40-7
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 65 mg/mL (200.1 mM)
Water: 23 mg/mL (70.8 mM)
Ethanol: 65 mg/mL (200.1 mM)
Other info

Chemical Name: 1-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide hydrochloride

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

SMILES Code: O=C(C1N(CCCC)CCCC1)NC2=C(C)C=CC=C2C

Synonyms

Marcaine; AH-250; Win-11318; HSDB7790; SKY0402; AH 250; Win 11318; AH250; HSDB 7790; SKY 0402; HSDB-7790; SKY-0402; Win11318

实验参考方法
In Vitro

In vitro activity: Bupivacaine solution is cytotoxic to bovine articular chondrocytes and articular cartilage in vitro after only 15 to 30 minutes exposure. Bupivacaine acts in isolated mitochondria, as uncouplers between oxygen consumption and phosphorylation of adenosine diphosphate. 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. 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. Bupivacaine HCl also potently inhibits cAMP production with an IC50 of 2.3 μM.

In VivoBupivacaine 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.
Animal modelRats
Formulation & Dosage
References

Arthroscopy. 2006 Jul;22(7):693-9; Anesthesiology. 2002 Sep;97(3):710-6.