|3-(4-(2-((6-氨基-9-((2R,3R,4S,5S)-5-(乙基氨基甲酰基)-3,4-二羟基四氢呋喃-2-基)-9H-嘌呤-2-基)氨基)乙基)苯基)丙酸盐酸盐|CsnPharm

CAS No.: 124431-80-7

CGS 21680 HCl/CGS 21680 盐酸盐 Catalog No. CSN18682

Synonyms: CGS 21680 (hydrochloride);CGS-21680;CGS-21680 HCl

CGS 21680 HCl is A2A adenosine receptor agonist with Ki value of 27 nM, which can be used to distinguish A2A- and A2B-mediated effect and shows affinity for both A1 and A3 adenosine receptors.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述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^[7]. 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 Hydrochloride is a hydrochloride form of CGS 21680. 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^[1]. 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].

动物研究

剂量

Mice: 0.5 mg/kg^[3] (i.p.) Rat: 0.065 mg/kg - 0.125 mg/kg^[4] (i.p.); 0.03 mg/kg - 0.3 mg/kg^[5] (s.c.)

给药途径

i.p., s.c.

动物药代数据

Animal	Rats^[6]
Dose	0.3 mg/kg (i.v.) 3.0 mg/kg (p.o.)
Administration	i.v. p.o.
F	140% (p.o.)
B	558 ng/ml (i.v.)
T_max	13 min (p.o.)
MRT	11 min (i.v.)
A	6827 ng/ml (i.v.)
CL_p	0.83 L/kg/h (i.v.)
T_1/2β	15 min (i.v.)
C_max	94 ng/ml (p.o.)
V_β	0.27 L/kg (i.v.)
T_1/2α	1.8 min (i.v.)
AUC	485 h·ng/ml (i.v.) 67 h·ng/ml (p.o.)

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8657 mL
- 9.3287 mL
- 18.6574 mL
- 5 mM
- 0.3731 mL
- 1.8657 mL
- 3.7315 mL
- 10 mM
- 0.1866 mL
- 0.9329 mL
- 1.8657 mL

技术信息

CAS号

124431-80-7

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H30ClN7O6

运输

蓝冰

分子量

535.98

别名

CGS 21680 (hydrochloride);CGS-21680;CGS-21680 HCl;CGS-21680 hydrochloride

溶解度

DMSO	50.0 mg/mL (93.3 mM)
Water	insoluble

动物实验配方

30% propylene glycol+5% Tween 80+65% water

30 mg/mL

suspension

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