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经验公式(希尔记法):
C15H20ClN5O4
化学文摘社编号:
分子量:
369.80
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
SMILES string
Clc1nc2[n](cnc2c(n1)NC4CCCC4)[C@@H]3O[C@@H]([C@H]([C@H]3O)O)CO
InChI
1S/C15H20ClN5O4/c16-15-19-12(18-7-3-1-2-4-7)9-13(20-15)21(6-17-9)14-11(24)10(23)8(5-22)25-14/h6-8,10-11,14,22-24H,1-5H2,(H,18,19,20)/t8-,10-,11-,14-/m1/s1
InChI key
XSMYYYQVWPZWIZ-IDTAVKCVSA-N
assay
≥99% (HPLC)
form
solid
potency
2.3 nM Ki
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
white
solubility
DMSO: 100 mM
water: 5 mM
shipped in
ambient
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Primary Target
A1
A1
Reversible: yes
Disclaimer
Toxicity: Standard Handling (A)
General description
An adenosine analog that acts as a selective, high affinity agonist for Adenosine A1 receptor (A1R) (Ki = 800 pM; 2.3 µM, 18.8 µM, and 42 nM for human A1, A2A, A2B, A3 respectively). Shown to be centrally active following systemic administration and exhibits anti-convulsive effects. Also reported to inhibit adenylate cyclase activity in rat fat cell membrane (IC50 = 33 nM). Diminishes respiratory rhythm, reduces heart rate, and enhances the activity of KATP channels. Reduces norepinephrine release by about 50% in untreated and pertussis toxin treated hearts.
Other Notes
Burgdorf, C. et al. 2005. J Cardiovasc Pharmacol.45, 1.
Klotz, K. N., et al. 2000. Naunyn Schmiedebergs Arch Pharmacol. 362, 382.
Mironov, S., et al. 1990. J Neurophysiol.81, 1.
Monopoli, A., et al. 1994.Arzneimittelforschung.44, 1305.
Concas, A., et al. 1993. J Pharmacol Exp Ther.267, 844.
Lohse, M. J., et al. 1988. Nauryn Schmiedebergs Arch Pharmacol.337, 687.
Coffin, V. L., et al. 1987. J Pharmacol Exp Ther.241, 76.
Klotz, K. N., et al. 2000. Naunyn Schmiedebergs Arch Pharmacol. 362, 382.
Mironov, S., et al. 1990. J Neurophysiol.81, 1.
Monopoli, A., et al. 1994.Arzneimittelforschung.44, 1305.
Concas, A., et al. 1993. J Pharmacol Exp Ther.267, 844.
Lohse, M. J., et al. 1988. Nauryn Schmiedebergs Arch Pharmacol.337, 687.
Coffin, V. L., et al. 1987. J Pharmacol Exp Ther.241, 76.
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
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