GP 1a

Name: GP 1a
Brand: TargetMol
SKU: T41231
Price: 428 CNY
Availability: InStock
Rating: 5 (10 reviews)

一键复制产品信息

很棒

纯度: 99.96%

货号 T41231Cas号 511532-96-0

GP 1a 是cannabinoid receptor 2（CB2）的强效激动剂（EC50=7.1),是在cAMP、GTPγS 和β-arrestin 招募试验中显示的。GP 1a 对CB2受体的选择性约为CB1受体的30倍，且在体外增加HL-60细胞的P-ERK1/2表达。GP 1a 对皮肤伤口愈合有益。GP 1a 可抑制炎症和纤维生成，同时促进上皮的重新形成。

为众多的药物研发团队赋能，

让新药发现更简单！

GP 1a

一键复制产品信息

很棒

纯度: 99.96%

货号 T41231Cas号 511532-96-0

规格	价格	库存
1 mg	¥ 428	现货
5 mg	¥ 928	现货
10 mg	¥ 1,460	现货
25 mg	¥ 2,890	现货
50 mg	¥ 4,190	现货
100 mg	¥ 5,960	现货
500 mg	¥ 11,900	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

该分子属于定制产品。TargetMol拥有优秀的合成团队，经验和能力，可以为您提供高性价比的产品。如您有任何问题，欢迎咨询，我们将竭诚为您服务。

实验操作小课堂

常见问题解答

选择批次:

纯度: 99.96%

联系我们获取更多批次信息

资源下载:

COA HNMR LCMS 产品操作手册

产品介绍

GP 1a AI Summary

GP 1a exhibits a very high affinity for the CB2 receptor, with a Ki value of 0.037 nM in both spleen and brain tissues of CD1 mice, and a substantially lower affinity for the CB1 receptor (Ki = 363.0 nM). This results in a remarkable selectivity ratio (Ki) of 9810.0, reflecting a strong preference for CB2 over CB1 receptors. At a concentration of 10 nM, it significantly increases ERK1/2 phosphorylation activity in HL60 cells, indicating potent intrinsic activity at the CB2 receptor (83.0%). GP 1a also demonstrates inhibitory activities in various bioassays, including: - Tyrosyl-DNA Phosphodiesterase (TDP1) with a potency of 22387.2 nM - Bacillus subtilis Sfp phosphopantetheinyl transferase (PPTase) with a potency of 15848.9 nM - Fructose-1,6-bisphosphate Aldolase from Giardia Lamblia with a potency of 17740.7 nM - ROR gamma transcriptional activity with a potency of 35481.3 nM - GCN5L2 with a potency of 3981.1 nM - Binding or entry into cells for Lassa Virus and Marburg Virus with potencies of 35481.3 nM Moreover, GP 1a demonstrates antiviral activity. It inhibits SARS-CoV-2 induced cytotoxicity in Caco-2 cells and VERO-6 cells at a concentration of 10 μM after 48 hours. It also shows 10.99% inhibition of SARS-CoV-2 3CL-Pro protease at 20 μM and exhibits minor inhibitory activity against human HDAC6. Overall, GP 1a’s highly selective interaction with the CB2 receptor, combined with its diverse bioactivity profile, including antiviral and enzyme inhibition effects, marks it as a compound of significant pharmacological potential..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述

GP 1a is a potent agonist of cannabinoid receptor 2 (CB2) (EC50=7.1), as shown in cAMP, GTPγS and β-arrestin recruitment assays. GP 1a is approximately 30-fold more selective for CB2 receptors than CB1 receptors and increases P-ERK1/2 expression in HL-60 cells in vitro. GP 1a is beneficial for skin wound healing. GP 1a inhibits inflammation and fibrogenesis while promoting epithelial re-formation.

化学信息

分子量	441.35
分子式	C₂₃H₂₂Cl₂N₄O
CAS No.	511532-96-0
Smiles	C(NN1CCCCC1)(=O)C=2C3=C(N(N2)C4=C(Cl)C=C(Cl)C=C4)C=5C(C3)=CC(C)=CC5
颜色	White
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: 90 mg/mL (203.92 mM), Sonication is recommended.

DMSO: 90 mg/mL (203.92 mM), Sonication is recommended.

溶液配制表

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2658 mL	11.3289 mL	22.6578 mL	113.2888 mL
5 mM	0.4532 mL	2.2658 mL	4.5316 mL	22.6578 mL
10 mM	0.2266 mL	1.1329 mL	2.2658 mL	11.3289 mL
20 mM	0.1133 mL	0.5664 mL	1.1329 mL	5.6644 mL
50 mM	0.0453 mL	0.2266 mL	0.4532 mL	2.2658 mL
100 mM	0.0227 mL	0.1133 mL	0.2266 mL	1.1329 mL