Benzocaine - Sodium Channel - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBenzocaineCat. No.: HY-Y0258CAS No.: 94-09-7分式: CHNO分量: 165.19作靶点: Sodium Channel作通路: Membrane Transporter/Ion Channel储存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性数据体外实验 DMSO : 10

2、0 mg/mL (605.36 mM)H2O : 2 mg/mL (12.11 mM; ultrasonic and warming and heat to 60C)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 6.0536 mL 30.2682 mL 60.5364 mL5 mM 1.2107 mL 6.0536 mL 12.1073 mL10 mM 0.6054 mL 3.0268 mL 6.0536 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制

3、储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (15.13 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)

4、Solubility: 2.5 mg/mL (15.13 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (15.13 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 Benzocaine 与所有其它局部醉药 (LAs) 起，作电压门控Na+通道的共同受体，其在 +30 mV 下测得的IC50 值为0.8 mM。IC50 & Target IC50: 0.8

5、mM (Na+ channel) 1.体外研究 Benzocaine blocks 1 wild-type Na+ currents in a dose-dependent Manner. The Benzocaine concentrationthat inhibits 50% of Na+ currents (IC50) is estimated to be about 0.8 mM when a test potential of +30 mV isapplied. The slope of the h curve is also significantly reduced by ben

6、zocaine (from 6.6 to 9.9 mV). Mutationof 1-N1584A also significantly increases the potency of Benzocaine. At 1 mM, Benzocaine blocks about55% of wild-type Na+ current but about 95% of 1-N1584A mutant current. Benzocaine also appears to bindmore strongly to its LA receptor in the N1584A mutant than i

7、n the wild type 1. The inhibition of Ca2+ uptakeoccurres at lower Benzocaine concentration (IC50=40.31.2mM) than that affecting the enzymatic activity 2.体内研究 A common Benzocaine-containing anesthetic is topically applied to the following species: dogs, domesticshorthair cats, Long-Evans rats, Spragu

8、e-Dawley rats, ferrets, rhesus monkeys, cynomolgus monkeys, owlmonkeys, New Zealand White rabbits, miniature pigs, ICR mice, C3H mice, and C57BL/10SnJ mice. Allanimals, except mice and rats, receive a 2-second spray to the mucous membranes of the nasopharynx foran estimated dose of 56 mg. A 2-second

9、 spray to rodents oral mucous membranes delivers too great avolume of fluid for these animals. The study is repeated in dogs several months later to confirm lowresponse. Response to Benzocaine spray is observed in most animals tested, with response peakingbetween 15 and 30 minutes after dosing 3.REF

10、ERENCES1. Wang GK et al. A common local anesthetic receptor for benzocaine and etidocaine in voltage-gated mu1 Na+ channels. Pflugers Arch.1998 Jan;435(2):293-302.2. Di Croce D et al. Drug action of benzocaine on the sarcoplasmic reticulum Ca-ATPase from fast-twitch skeletal muscle. NaunynSchmiedebergs Arch Pharmacol. 2015 Nov;388(11):1163-70.3. Davis JA, et al. Benzocaine-induced methemoglobinemia attributed to topical application of the anesthetic in several laboratory animalspecies. Am J Vet Res. 1993 Aug;54(8):1322-6.McePdfHeightCaution: Product has not been