SML1958
Bay 60-6583
≥98% (HPLC)
别名:
2-[[6-氨基-3,5-二氰基-4- [4-（环丙基甲氧基）苯基] -2-吡啶基]硫代]-乙酰胺, BAY606583, BR 4887, BR4887, Bay 60-6,583, Bay 606583
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关于此项目
经验公式（希尔记法）:
C19H17N5O2S
化学文摘社编号:
分子量:
379.44
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Quality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 20 mg/mL, clear
storage temp.
2-8°C
SMILES string
NC1=C(C#N)C(C2=CC=C(OCC3CC3)C=C2)=C(C#N)C(SCC(N)=O)=N1
InChI
1S/C19H17N5O2S/c20-7-14-17(12-3-5-13(6-4-12)26-9-11-1-2-11)15(8-21)19(24-18(14)23)27-10-16(22)25/h3-6,11H,1-2,9-10H2,(H2,22,25)(H2,23,24)
InChI key
ZTYHZMAZUWOXNC-UHFFFAOYSA-N
Biochem/physiol Actions
BAY 60-6583是一种有效的腺苷受体A2b（A2bR）的部分激动剂（抑制0.3 nM [3H] PSB-603与人/小鼠/大鼠A2bR结合的Ki = 114/136/100 nM），可在转染后表达人A2bR（EC50〜100 nM）的CHO中选择性诱导cAMP依赖性转录活性，但在表达A1R或A2aR的CHO中无效，其对人/大鼠/小鼠A2aR没有亲和力。BAY 60-6583还显示出对A1R（抑制1 nM [3H]CCPA与人/小鼠/大鼠A1R结合的 Ki= 387/351/514 nM；对100 nM CCPA诱导的hA1R β-抑制蛋白募集过程的抑制IC50 = 7.4 μM）和A3R（抑制10 nM [3H]NECA与人/小鼠/大鼠的A3R结合的 Ki= 223/3920/2750 nM；对30 nM Cl-IB-MECA诱导的hA3R β-抑制蛋白募集过程的抑制IC50 = 6.7 μM）的低亲和性拮抗活性。BAY 60-6583已通过i.p.（0.1-80 mg/kg）或i.v.（0.2-2 mg/kg）广泛应用于动物体内，以研究A2bR介导的生物反应。
对A1R & A3R具有低亲和力拮抗活性的有效腺苷受体A2bR部分激动剂。
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Atsushi Kuno et al.
Journal of molecular and cellular cardiology, 43(3), 262-271 (2007-07-17)
Although protein kinase C (PKC) plays a key role in ischemic preconditioning (IPC), the actual mechanism of that protection is unknown. We recently found that protection from IPC requires activation of adenosine receptors during early reperfusion. We, therefore, hypothesized that
Tobias Eckle et al.
Circulation, 115(12), 1581-1590 (2007-03-14)
Ecto-5'-nucleotidase (CD73)-dependent adenosine generation has been implicated in tissue protection during acute injury. Once generated, adenosine can activate cell-surface adenosine receptors (A1 AR, A2A AR, A2B AR, A3 AR). In the present study, we define the contribution of adenosine to
Mohamad Wessam Alnouri et al.
Purinergic signalling, 11(3), 389-407 (2015-07-02)
Adenosine receptors (ARs) have emerged as new drug targets. The majority of data on affinity/potency and selectivity of AR ligands described in the literature has been obtained for the human species. However, preclinical studies are mostly performed in mouse or
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| SML1958-5MG | 04061832086101 |
| SML1958-25MG | 04061832086095 |