所有图片(1)
别名:
4-[(4-trans-Hydroxycyclohexyl)amino]-2-phenyl-7H-pyrrolo[2,3-d]pyrimidine, Derenofylline, SLV 320, SLV-320, trans-4-[(2-Phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclohexanol
经验公式（希尔记法）:
C18H20N4O
推荐产品
质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
O[C@H]1CC[C@@H](CC1)NC2=NC(C3=CC=CC=C3)=NC4=C2C=CN4
InChI
1S/C18H20N4O/c23-14-8-6-13(7-9-14)20-18-15-10-11-19-17(15)21-16(22-18)12-4-2-1-3-5-12/h1-5,10-11,13-14,23H,6-9H2,(H2,19,20,21,22)
InChI key
RBZNJGHIKXAKQE-UHFFFAOYSA-N
生化/生理作用
SLV320 is an orally active, high-affinity adenosine receptor A1 antagonist (pKi = 9.0 against 3H-DPCPX for binding human A1R and 8.6 against 3H-CCPA for binding rat A1R) that exhibits higher A1R-selectivity than DPCPX over other adenosine receptor subtypes (Fold-selectivity/subtypes = 200/hA3, 398/hA2a, 3981/hA2b). SLV320 displays much reduced or little affinity toward a panel of 94 other receptors and no inhibitory activity against PDE1-6 (IC50 ≥1 μM). SLV320 selectively reduces A1R-mediated bradycardia (ED50 = 0.49 mg/kg via p.o. or 0.25 mg/kg via i.v. 10 min prior to 100 μg/kg adenosine i.v. challenge), but not A2R-dependent hypotension (up to 2 mg/kg) among adenosin-challenged rats. When administered via food intake, SLV320 efficacy is demonstrated in experimental models of chronic renal failure (CRF; 10 mg/kg/day) and liver cirrhosis (5.1 mg/kg/day p.o.) in rats in vivo.
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
Jian Zhou et al.
American journal of respiratory cell and molecular biology, 48(3), 299-305 (2012-12-12)
Epithelial injury and airway hyperresponsiveness are prominent features of asthma. We have previously demonstrated that laser ablation of single epithelial cells immediately induces global airway constriction through Ca(2+)-dependent smooth muscle shortening. The response is mediated by soluble mediators released from
Berthold Hocher et al.
PloS one, 6(3), e17891-e17891 (2011-03-23)
Liver cirrhosis is often complicated by an impaired renal excretion of water and sodium. Diuretics tend to further deteriorate renal function. It is unknown whether chronic selective adenosine A(1) receptor blockade, via inhibition of the hepatorenal reflex and the tubuloglomerular
P Kalk et al.
British journal of pharmacology, 151(7), 1025-1032 (2007-06-15)
Myocardial fibrosis is an unwanted effect associated with chronic renal failure. The adenosine system is involved in cardiac and renal function. Therefore, we investigated the novel selective adenosine A(1) receptor antagonist SLV320 focusing on its potential in preventing cardiomyopathy in
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