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Tilorone 2HCl

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Chemical Structure| 27591-69-1 同义名 : 盐酸替洛隆 ;Tilorone (hydrochloride);Tilorone dihydrochloride;NSC 143969
CAS号 : 27591-69-1
货号 : A632643
分子式 : C25H36Cl2N2O3
纯度 : 98%
分子量 : 483.471
MDL号 : MFCD00134071
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 12 mg/mL(24.82 mM)，配合低频超声助溶，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: 100 mg/mL(206.84 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 Tilorone dihydrochloride (tilorone) is a small-molecule, orally bioavailable drug. Tilorone was shown to have 52% human plasma protein binding with excellent plasma stability and a mouse liver microsome half-life of 48 min. Dose range-finding studies in mice demonstrated a maximum tolerated single dose of 100 mg/kg of body weight. Tilorone doses of 25 and 50 mg/kg proved efficacious in protecting 90% of mice from a lethal challenge with mouse-adapted with once-daily intraperitoneal (i.p.) dosing for 8 days[3]. RT-PCR analysis showed that tilorone dihydrochloride induced upregulation and downregulation in expression of Bax and Bcl-2, respectively[4]. Furthermore, the synthesized tilorone dihydrochloride exhibited an obvious effect on induction of interferon-α (IFN-α) in mice within 12 h, and the peak level was observed until 24 h[5]. Moreover, tilorone treatment resulted in decreased PC3 cell growth and invasion; PC3 cells with inactive CDK5 (Cyclin-dependent kinase 5) were inhibited more effectively[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.07mL

0.41mL

0.21mL

10.34mL

2.07mL

1.03mL

20.68mL

4.14mL

2.07mL
参考文献

[1]Wissing MD, Dadon T, et al. Small-molecule screening of PC3 prostate cancer cells identifies tilorone dihydrochloride to selectively inhibit cell growth based on cyclin-dependent kinase 5 expression. Oncol Rep. 2014 Jul;32(1):419-24.

[2]Tokumaru T. The mode of inhibition of herpes simplex and vesicular stomatitis ocular viral infections in the rabbit and hamster by an interferon inducer tilorone dihydrochloride. Res Commun Chem Pathol Pharmacol. 1975 Jun;11(2):289-301.

[3]Ekins S, Lingerfelt MA, Comer JE, Freiberg AN, Mirsalis JC, O'Loughlin K, Harutyunyan A, McFarlane C, Green CE, Madrid PB. Efficacy of Tilorone Dihydrochloride against Ebola Virus Infection. Antimicrob Agents Chemother. 2018 Jan 25;62(2):e01711-17

[4]Alem M, Shahbazfar AA, Zare P, Tayefi-Nasrabadi H. The effects of coadministration of tilorone dihydrochloride and culture supernatants from Lactobacillus reuteri on the mouse hepatoma cell line. J Cancer Res Ther. 2019 Jan-Mar;15(1):176-184

[5]Zhang J, Yao Q, Liu Z. An Effective Synthesis Method for Tilorone Dihydrochloride with Obvious IFN-α Inducing Activity. Molecules. 2015 Dec 2;20(12):21458-63

[6]Wissing MD, Dadon T, Kim E, Piontek KB, Shim JS, Kaelber NS, Liu JO, Kachhap SK, Nelkin BD. Small-molecule screening of PC3 prostate cancer cells identifies tilorone dihydrochloride to selectively inhibit cell growth based on cyclin-dependent kinase 5 expression. Oncol Rep. 2014 Jul;32(1):419-24