购物车

您的购物车当前为空

GS 39783

Name: GS 39783
Brand: TargetMol
SKU: T22813
Price: 227 CNY
Availability: InStock
Rating: 5 (10 reviews)

一键复制产品信息

很棒

纯度: 99.92%

货号 T22813Cas号 39069-52-8

GS 39783 是 GABABR 的正变构调节剂 (PAM)，可降低酒精的动机特性,减少精神兴奋剂的条件强化和条件性奖励。

为众多的药物研发团队赋能，

让新药发现更简单！

GS 39783

一键复制产品信息

很棒

纯度: 99.92%

货号 T22813Cas号 39069-52-8

GS 39783 是 GABABR 的正变构调节剂 (PAM)，可降低酒精的动机特性,减少精神兴奋剂的条件强化和条件性奖励。

规格	价格	库存
1 mg	¥ 227	现货
5 mg	¥ 548	现货
10 mg	¥ 833	现货
25 mg	¥ 1,590	现货
50 mg	¥ 2,590	现货
100 mg	¥ 3,670	现货

库存状态实时更新，以官网显示为准，现货产品可直接加购物车下单

大包装 & 定制

加入购物车

TargetMol的所有产品仅用作科学研究或药证申报，不能被用于人体，我们不向个人提供产品和服务。请您遵守承诺用途，不得违反法律法规规定用于任何其他用途。

实验操作小课堂

常见问题解答

选择批次:

纯度: 99.92%

联系我们获取更多批次信息

资源下载:

COA HNMR HPLC 产品操作手册

产品介绍

GS 39783 AI Summary

GS 39783 exhibits a diverse range of bioactivities across various assays and biological systems. It acts as a positive allosteric modulator of GABAB receptors, particularly GABA-B1 and GABA-B1b, expressed in CHO-K1 cells and rat cortical membranes, showing an EC50 of 741.31 nM and modulation efficacy between 132.0% and 192.0%. Additionally, it modulates GABA activity, with a recorded Emax of 146.0% when co-administered with 1 µM GABA. The compound also displays inhibition of critical enzymes and interactions: - Menin-MLL interaction in leukemia (potency: 39810.7 nM) - Tyrosyl-DNA Phosphodiesterase (TDP1) (potency: 891.3 nM) - Cytochrome P450 enzymes (2C19 and 2C9) (potencies: 5011.9 nM and 1995.3 nM, respectively) - USP1/UAF1 (potency: 15848.9 nM) - Anthrax Lethal Toxin Internalization (potency: 10000.0 nM) Its antiviral capabilities are demonstrated by inhibiting SARS-CoV-2 induced cytotoxicity in Caco-2 and VERO-6 cells, though with varying degrees of efficacy. Additionally, the compound inhibits SARS-CoV-2 3CL-Pro protease at 20 µM. In hypnotic assays with DBA mice, GS 39783 increases the pentobarbital-induced duration and reduces onset time of the loss of the righting reflex. However, it shows cytotoxicity in mouse NIH/3T3 cells with an IC50 of 60000.0 nM. In GPCR beta-arrestin recruitment assays, it exhibits varying degrees of modulation across multiple targets, implicating potential effects on diverse receptor systems. Moreover, thermal shift assays suggest both stabilizing and destabilizing effects on protein structures, indicating complex interactions with protein domains. Lastly, GS 39783 displays inhibition of human HDAC6 activity, with a higher inhibition percentage using commercial substrates (47.7%) compared to custom ones (5.72%), and depending on cell type, it shows differential impacts on cell viability: generally promoting growth in HEK293T cells, mixed effects in U2OS cells, and varying effects in human fibroblast cells..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	GS 39783 is a positive allosteric modulator (PAM) of GABABR, which reduces the motivational properties of alcohol and the conditioned reinforcement and conditional reward of psychostimulants.

化学信息

分子量	337.44
分子式	C₁₅H₂₃N₅O₂S
CAS No.	39069-52-8
Smiles	N(C=1C(N(=O)=O)=C(NC2CCCC2)N=C(SC)N1)C3CCCC3
密度	1.31g/cm3
颜色	Yellow
物理性状	Solid

储存&溶解度

存储

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

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 20 mg/mL (59.27 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.93 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	2.9635 mL	14.8174 mL	29.6349 mL	148.1745 mL
5 mM	0.5927 mL	2.9635 mL	5.9270 mL	29.6349 mL
10 mM	0.2963 mL	1.4817 mL	2.9635 mL	14.8174 mL
20 mM	0.1482 mL	0.7409 mL	1.4817 mL	7.4087 mL
50 mM	0.0593 mL	0.2963 mL	0.5927 mL	2.9635 mL