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Meticrane

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Chemical Structure| 1084-65-7 同义名 : 蒲硫杂茶磺胺
CAS号 : 1084-65-7
货号 : A692089
分子式 : C10H13NO4S2
纯度 : 99%+
分子量 : 275.344
MDL号 : MFCD00079454
存储条件:

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 50 mg/mL(181.59 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

动物实验配方:
生物活性
描述 Meticrane is a diuretic and a potent peripheral-type benzodiazepine receptor (PBR) inhibitor (IC50= 1 μM). Meticrane inhibits the reabsorption of sodium and chloride ions in the distal convoluted tubule. Meticrane is used to treat essential hypertension[3]. Meticrane is highly ranked in the connectivity map (cMap) analysis, and it does not have any known anti-cancer or immune-stimulating effect. Co-treatment with Meticrane significantly enhances treatment efficacy of CTLA-4 blockade[4]. In vitro assays performed in presence of 6-hydroxycoumarin and meticrane, among the highly affinity predicted binders, confirmed a dose-dependent inhibition (17-81%) of patulin production by 6-hydroxycoumarin (10 µM-1 mM concentration range), whereas the approved drug meticrane inhibited patulin production by 43% already at 10 µM. Furthermore, 6-hydroxycoumarin and meticrane caused a 60 and 41% reduction of patulin production, respectively, in vivo on apples at 100 µg/wound[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.63mL

0.73mL

0.36mL

18.16mL

3.63mL

1.82mL

36.32mL

7.26mL

3.63mL

参考文献

[1]Boissier JR, Hirtz J, et al. [Resorption, distribution, excretion and metabolism in rat of a new diuretic: meticrane] . Ann Pharm Fr. 1970 Jul-Aug;28(7):497-509. French.

[2]Linquette M, Decoulx M. [Clinical trial of a new diuretic: meticrane] . Lille Med. 1968 Jan;13(1):Suppl:13-6.

[3]Boissier JR, Hirtz J, Dumont C, Gérardin A. Résorption, distribution, excrétion et métabolisme chez le rat d'un nouveau diurétique: le métricrane [Resorption, distribution, excretion and metabolism in rat of a new diuretic: meticrane]. Ann Pharm Fr. 1970 Jul-Aug;28(7):497-509. French

[4]Lesterhuis WJ, Rinaldi C, Jones A, Rozali EN, Dick IM, Khong A, Boon L, Robinson BW, Nowak AK, Bosco A, Lake RA. Network analysis of immunotherapy-induced regressing tumours identifies novel synergistic drug combinations. Sci Rep. 2015 Jul 21;5:12298

[5]Tragni V, Cotugno P, De Grassi A, Cavalluzzi MM, Mincuzzi A, Lentini G, Sanzani SM, Ippolito A, Pierri CL. Targeting Penicillium expansum GMC Oxidoreductase with High Affinity Small Molecules for Reducing Patulin Production. Biology (Basel). 2020 Dec 31;10(1):21