4,8-DiMeIQx - CAS:95896-78-9

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4,8-DiMeIQx (Synonyms:2-氨基-3,4,8-三甲基-3H-咪唑[4,5-f]喹喔啉;2-Amino-3,4,8-trimethyl-3H-imidazo[4,5-f]quinoxaline)

目录号 : KP14008 CAS No. : 95896-78-9 纯度 : 98%

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4,8-DiMeIQx 是一种具有口服活性的诱变剂、选择性多巴胺能神经毒物和 DNA 损伤剂。4,8-DiMeIQx 可从烹制后的牛肉、香肠、猪肉和鸡肉中分离。4,8-DiMeIQx 可在有无 S9 混合液的条件下诱导鼠伤寒沙门氏菌 TA98 发生回复突变，并在大鼠肝脏中体内形成 DNA 加合物。4,8-DiMeIQx 对多巴胺能神经元具有选择性神经毒性。4,8-DiMeIQx 对非多巴胺能神经元无活性。4,8-DiMeIQx 可用于帕金森病和结直肠癌的相关研究。

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5mg		In-stock

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生物活性

4,8-DiMeIQx is an orally active mutagen, selective dopaminergic neurotoxicant, and DNA damaging agent. 4,8-DiMeIQx can be isolated from cooked beef, sausage, pork, and chicken. 4,8-DiMeIQx induces reverse mutations in *Salmonella typhimurium* TA98 in the presence or absence of S9 mix, and forms DNA adducts in vivo in rat liver. 4,8-DiMeIQx exhibits selective neurotoxicity toward dopaminergic neurons. 4,8-DiMeIQx shows no activity against non-dopaminergic neurons. 4,8-DiMeIQx can be used in studies related to Parkinson's disease and colorectal cancer.

体外研究

4,8-DiMeIQx (1 μg per assay) showed mutagenicity to Salmonella typhimurium TA98 treated with S9 mixture, inducing 206000 revertant mutant colonies per microgram, accounting for 9% of the total mutagenicity of bacterial grade extracts.

4,8-DiMeIQx (100 nM-5 μM; 24 h) exhibits selective neurotoxicity on dopaminergic neurons in E17 primary midbrain cultures, with a threshold dose of 100 nM. Significant loss of dopaminergic neurons was observed at all test concentrations between 100 nM and 5 μ M, while non dopaminergic neurons were not affected.

4,8-DiMeIQx (100 nM -5 μM; 24 h) did not cause significant changes in axonal density of dopaminergic or non dopaminergic neurons after incubation at a concentration of 100 nM -5 μ M in the E17 primary midbrain culture system for 24 h.

体内研究

4,8-DiMeIQx (50 mg/kg; oral administration; Single time DNA adducts can be formed in the liver, with N2- (2 '- deoxyguanosin-8-yl) -4,8-DiMeIQx being the main adduct, accounting for approximately 60% of the total adducts; After a single oral dose of 50 mg/kg for 72 hours, the relative adduct level was 3.54 × 10-5.
4,8-DiMeIQx (0.5 mg per animal; oral administration; After oral administration to male AGUS rats, radioactive substances were mainly excreted through urine within 24 hours, and BNF induced intestinal enzyme activity increased fecal excretion; The main metabolites include hydroxylated and acylated forms, and their mutagenic activity differs from that of chiral compounds.

Animal Model:	Wistar (male, 8 weeks old, 250 g)
Dosage:	50 mg/kg
Administration:	p.o.; single dose
Result:	Identified three DNA adducts in liver DNA. Accounted for ~60% of total measured radioactivity via the major adduct N2 -(2'- deoxyguanosin-8-yl)-4,8-DiMeIQx. Had a relative adduct level of 3.54×10-5 for the major adduct. Had relative adduct levels of 1.43×10-5 and 1.30×10-5 for the two minor adducts. Matched the in vivo adduct pattern seen in in vitro modified calf thymus DNA.

分子式

C₁₂H₁₃N₅

分子量

227.265

CAS号

95896-78-9

中文名称

2-氨基-3,4,8-三甲基-3H-咪唑[4,5-f]喹喔啉

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

2-8°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

纯度： 98%

Data Sheet

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