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Dyclonine HCl

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Chemical Structure| 536-43-6 同义名 : Dyclocaine hydrochloride;Dyclonine (hydrochloride);Tanaclone;Dyclothane;Dyclone;Dyclocaine HCl;Dyclonine hydrochloride
CAS号 : 536-43-6
货号 : A162451
分子式 : C18H28ClNO2
纯度 : 98%
分子量 : 325.873
MDL号 : MFCD00035386
存储条件:

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 25 mg/mL(76.72 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 50 mg/mL(153.43 mM),配合低频超声助溶

动物实验配方:
生物活性
描述 Dyclonine hydrochloride is the hydrochloride salt of Dyclonine. It reversibly binds to activated sodium channels in the neuron membrane, thereby decreasing the neuronal membrane’s permeability to sodium ions. This results in a transient and reversible loss of sensation in a localized area of body. It is recently reported to act as a covalent inhibitor for aldehyde dehydrogenases (ALDHs). Dyclonine hydrochloride (50 µM; 24 h) sensitizes cancer cells to deficiency of cysteine and GSH. Dyclonine hydrochloride (5 mg/kg; i.p.; single daily for 24 days) sensitizes the involucrin+ differentiated tumor cells to sulfasalazine treatment in vivo. 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[3].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03352700 Bowel Preparation Scale ... 展开 >> the Amount of Air Bubble Adenoma Detection Rate 收起 << Phase 4 Not yet recruiting February 1, 2018 China ... 展开 >> Changhai Hospital, Second Military Medical University Shanghai, China, 200433 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.07mL

0.61mL

0.31mL

15.34mL

3.07mL

1.53mL

30.69mL

6.14mL

3.07mL

参考文献

[1]Gargiulo AV, Burns GM, Huck CP. Dyclonine hydrochloride--a topical agent for managing pain. Ill Dent J. 1992 Jul-Aug;61(4):303-4.

[2]Florestano HJ, Bahler ME. Antimicrobial properties of dyclonine hydrochloride, a new topical anesthetic. J Am Pharm Assoc Am Pharm Assoc (Baltim), 1956. 45(5): p. 320-5.

[3]Okazaki S, Shintani S, Hirata Y, et al. Synthetic lethality of the ALDH3A1 inhibitor dyclonine and xCT inhibitors in glutathione deficiency-resistant cancer cells. Oncotarget. 2018;9(73):33832-33843.