|6-甲酰基-5,11-二氢吲哚并[3,2-B]咔唑|CsnPharm

CAS No.: 172922-91-7

FICZ Catalog No. CSN10150

Synonyms: 6-Formylindolo[3,2-b]carbazole

FICZ is a tryptophan-derived, high affinity Ah receptor ligand and an efficient inducer of CYP1A1 gene expression in short time incubation (0.5 h) experiments. It is also a potent aryl hydrocarbon receptor (AHR) agonist, and also has the qualities of a perfect substrate for mammalian CYP1 enzymes.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述The aryl hydrocarbon receptor (AHR) is a transcription factor that regulates gene expressions in response to endogenous and exogenous signals. FICZ is a high potency AHR agonist with a K_d value of 0.07 nM^[3]. The 24-h treatment with 100 nM FICZ significantly induced EROD activity in wild-type mouse hepatoma Hepa-1 cells. FICZ at the concentration of 1 nM increased the mRNA level of CYP1A1 in wild-type cells, but the induction was transient and declined 3h after the treatment. In c37 cells, FICA-induced CYP1A1 mRNA expression was sustained^[4]. In human liver microsomes, a 20-min preincubation with a mixture of CYP1A1/1A2 and CYP1B1 antibodies almost completely blocked (93%) the NADPH-dependent FICZ metabolism. In HepG2 cells treated with 5 nM FICZ, the addition of 5 μM αNF attenuated the complete depletion of intracellular levels of FICZ as compared to non-αNF treated cells. CYP1A1 catalyzes the hydroxylation of FICZ with extremely high efficiency (K_cat/K_m = 8.1 × 10⁷M^-1s^-1^[5]. In a mouse model of mite-induced chronic dermatitis, treatment with FICZ ointment at the dose of 10^-3 mM for 2 weeks significantly improved the dermatitis compared to control mice^[6].
动物研究
剂量
Mice: 50 μg/kg - 10 mg/kg^[3] (i.p.), 0.15 mg/kg^[4] (i.p.) Rat: 0.1 mg/kg^[5] (i.g.)

给药途径
i.p., i.g.
参考文献

动物研究
剂量	Mice: 50 μg/kg - 10 mg/kg^[3] (i.p.), 0.15 mg/kg^[4] (i.p.) Rat: 0.1 mg/kg^[5] (i.g.)
给药途径	i.p., i.g.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.5173 mL
- 17.5864 mL
- 35.1727 mL
- 5 mM
- 0.7035 mL
- 3.5173 mL
- 7.0345 mL
- 10 mM
- 0.3517 mL
- 1.7586 mL
- 3.5173 mL

技术信息

CAS号

172922-91-7

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H12N2O

运输

蓝冰

分子量

284.31

别名

6-Formylindolo[3,2-b]carbazole

溶解度

DMSO	56.0 mg/mL (197.0 mM)
Water	Insoluble
Ethanol	Insoluble

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FICZ Catalog No. CSN10150

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