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Dyclonine hydrochloride
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。
Dyclonine hydrochloride图片
CAS NO:536-43-6
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
500mg电议
5 g电议
10 g电议
50 g电议

产品名称
盐酸达克罗宁
Dyclocaine hydrochloride
产品介绍
Dyclonine (Dyclocaine) hydrochloride 是一种口服有效的ALDH共价抑制剂 (可穿过血脑屏障),其对ALDH2ALDH3A1IC50分别为 35 和 76 μM. Dyclonine hydrochloride 具有靶向癌细胞的增敏活性和抗菌活性。Dyclonine hydrochloride 还是一种局部麻醉剂,能阻断各种神经冲动或刺激的传导,抑制触觉和痛觉。
生物活性

Dyclonine (Dyclocaine) hydrochloride is an orally effectiveALDHcovalent inhibitor (crosses blood-brain barrier), with anIC50of 35 μM forALDH2and 76 μM forALDH3A1. Dyclonine hydrochloride has sensitizing activities for targetedcancercells and antibacterial. Dyclonine hydrochloride is also a local anesthetic that blocks the transmission of various nerve impulses or stimuli and inhibits the sensation of touch and pain[1][2][3].

IC50& Target[3]

ALDH2

35 μM (IC50)

ALDH3

76 μM (IC50)

体外研究
(In Vitro)

Dyclonine hydrochloride (50 μM; 24 h) sensitizes cancer cells to deficiency of cysteine and GSH[1].
Dyclonine hydrochloride (0-2048 μg/mL; 24 or 48 h) shows significant bactericidal and fungicidal activity[2].

Cell Viability Assay[1]

Cell Line:HSC-4 cells
Concentration:50 μM
Incubation Time:24 h
Result:Inhibited ALDH activity and induced 4-HNE accumulation in GSH-depleted cancer cells.

Cell Viability Assay[2]

Cell Line:S. aureus,B. subtilis,E. coli,T. mentagrophyte
Concentration:0-2048 μg/mL
Incubation Time:24 h (for bacterial), 48 h (for fungi)
Result:Showed good antibacterial and antifungal activity, with minimum microbicidal concentration of 0.006%, 0.025%, 0.012% and 0.025% forS. aureus,B. subtilis,E. coli,T. mentagrophyte, separately.
体内研究
(In Vivo)

Dyclonine hydrochloride (5 mg/kg; i.p.; single daily for 24 days) sensitizes the involucrin+differentiated tumor cells to sulfasalazine treatment in vivo[1].
Dyclonine hydrochloride (5 mg/kg; i.p.; single daily for 21 days) suppress the growth of tumors formed by ALDH3A1-expressing gastric cancer stemlike cells when combines with sulfasalazine[1].

Animal Model:Athymic nude mice (HSC-2 cells implanted model)[1].
Dosage:5 mg/kg
Administration:Intraperitoneal injection; single daily for 24 days (combine with sulfasalazine).
Result:Attenuated the formation of tumors by HSC-2 cells implanted in nude mice when combined with sulfasalazine.
Animal Model:C57BL6 mice (K19-Wnt1/C2mE-KP cells implanted model)[1].
Dosage:5 mg/kg
Administration:Intraperitoneal injection; single daily for 21 days (combine with sulfasalazine).
Result:Enhanced the antitumor effect of sulfasalazine on HNSCC tumors consisting of CD44vhigh stemlike tumor cells and involucrin+differentiated tumor cells.
分子量

325.87

性状

Solid

Formula

C18H28ClNO2

CAS 号

536-43-6

中文名称

盐酸达克罗宁

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

H2O : 50 mg/mL(153.44 mM;Need ultrasonic)

DMSO : ≥ 25 mg/mL(76.72 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.0687 mL15.3435 mL30.6871 mL
5 mM0.6137 mL3.0687 mL6.1374 mL
10 mM0.3069 mL1.5344 mL3.0687 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储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.5 mg/mL (7.67 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.67 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.5 mg/mL (7.67 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.67 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (7.67 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.67 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。