Benzocaine - Sodium Channel - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBenzocaineCat. No.: HY-Y0258CAS No.: 94-09-7分式: CHNO分量: 165.19作靶點: Sodium Channel作通路: Membrane Transporter/Ion Channel儲存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性數(shù)據(jù)體外實驗 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制備儲備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制

3、儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (15.13 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)

4、Solubility: 2.5 mg/mL (15.13 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (15.13 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Benzocaine 與所有其它局部醉藥 (LAs) 起，作電壓門控Na+通道的共同受體，其在 +30 mV 下測得的IC50 值為0.8 mM。IC50 & Target IC50: 0.8

5、mM (Na+ channel) 1.體外研究 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.體內(nèi)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