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AGI-43192

Name: AGI-43192
Brand: TargetMol
SKU: T9729
Price: 696 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.89%

货号 T9729Cas号 2377491-54-6

AGI-43192是一种有效的，可渗透进血脑屏障的蛋氨酸腺苷转移酶 2A (MAT2A) 抑制剂。AGI-43192抑制 s -腺苷蛋氨酸(SAM)生成代谢酶和蛋氨酸腺苷转移酶2A (MAT2A)，具有研究 SAM 调节在中枢神经系统 (CNS) 中的作用和治疗癌症疾病的潜力。

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AGI-43192

一键复制产品信息

很棒

纯度: 99.89%

货号 T9729Cas号 2377491-54-6

规格	价格	库存
1 mg	¥ 696	现货
5 mg	¥ 1,730	现货
10 mg	¥ 2,560	现货
25 mg	¥ 3,970	现货
50 mg	¥ 5,560	现货
100 mg	¥ 7,500	现货
500 mg	¥ 14,800	现货
1 mL x 10 mM (in DMSO)	¥ 1,900	现货

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COA LCMS HNMR 产品操作手册

产品介绍

AGI-43192 AI Summary

AGI-43192 is a bioactive compound exhibiting potent inhibition of MAT2A in MTAP-null human HCT-116 cells, with an IC50 of 14.0 nM and an Imax of 80.0%. It is involved in the transactivation of human PXR and induces CYP450 expression. The compound has good cell membrane permeability and an efflux ratio of 1.8. In mouse models, it has low brain penetration (brain-to-plasma ratio < 0.1) and is primarily hepatically cleared (extraction ratio of 0.245). It has a moderate volume of distribution at steady state (Vdss = 1.98 L.kg-1) and a mean residence time of 8.1 hours. The compound demonstrates high Cmax and AUC values in mice and significantly inhibits MAT2A in in vivo xenograft models, reducing tumor and brain SAM levels. It strongly binds to proteins in mouse plasma, with a low unbound fraction (Fu = 0.0028). Its potency is underscored by the plasma exposure required for SAM level reduction and its selectivity for tumor vs. brain reduction, as indicated by the free plasma IC50 ratio..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述

AGI-43192 is a potent methionine adenosine transferase 2A (MAT2A) inhibitor that penetrates the blood-brain barrier. AGI-43192 inhibits S-adenosine methionine (SAM) production metabolic enzyme and methionine adenosine transferase 2A (MAT2A), which has the potential to study the role of SAM regulation in the central nervous system (CNS) and the treatment of cancer diseases.

化学信息

分子量	484.86
分子式	C₂₃H₁₆ClF₃N₆O
CAS No.	2377491-54-6
Smiles	Cn1cc2cc(ccc2n1)-n1cc2cnc(NCC(F)(F)F)nc2c(-c2ccc(Cl)cc2)c1=O

储存&溶解度

存储

store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 45 mg/mL (92.81 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 8 mg/mL (16.5 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0625 mL	10.3123 mL	20.6245 mL	103.1226 mL
5 mM	0.4125 mL	2.0625 mL	4.1249 mL	20.6245 mL
10 mM	0.2062 mL	1.0312 mL	2.0625 mL	10.3123 mL
20 mM	0.1031 mL	0.5156 mL	1.0312 mL	5.1561 mL
50 mM	0.0412 mL	0.2062 mL	0.4125 mL	2.0625 mL