CGS 21680

产品信息

Adenosine is a neuromodulator maintaining adequate oxygen and energy supply throughout the body which is mediated by two specific cell-surface receptors known as A1 and A2. The 2 receptors are intense investigating targets for new drug developments in the treatment of hypertension and epilepsy^[6]. CGS 21680 is an adenosine receptors with IC50 values of 22 nM for A2 and 3.1 mM for A1 and with high affinity for brain striatal. CGS 21680 also showed 140-fold selective for A2 without effect on binding to 17 other adenosine receptor ligand sites. The drug increased coronary flow in a rat model^[2]. CGS 21680 could bind to A2 with high affinity (Kd = 15.5 nM), which was greatest in striatal membranes, consistent with a selective interaction in a pharmacological profile and high positive correlation between the pharmacological profile of adenosine ligands to inhibit the binding to A2 receptor^[7]. CGS 21680 was a weak agonist on A1 receptor mediated events in hippocampal slices and also not helpful of stimulating the formation of cAMP with an EC50 of only 110 nM, suggesting that CGS 21680 is selective at the high affinity adenosine for A2a receptor in striatum^[8].

CAS号	120225-54-9
分子式	C23H29N7O6
主要靶点	Adenosine Receptor
主要通路	GPCR/G Protein
分子量	499.5197
MDL NO	MFCD00078573
Pubchem ID	3086599
纯度	99.35%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件	粉末 -20°C 3年 液体 -80°C 1年
运输条件	Shipped in cold pack
别名

靶点

Target	Activity
Adenosine Receptor A2	IC50=22nM
Adenosine Receptor A1	IC50=3080nM

动物研究

剂量	Mice: 0.5 mg/kg[3] (i.p.) Rat: 0.5 mg/kg - 40 mg/kg[4] (s.c.)
给药途径	i.p., s.c.