Derenofylline (SLV 320) is a potent, selective and orally active adenosine A1 receptor antagonist, with Ki values of 1 nM, 200 nM and 398 nM for human A1, A3 and A2A receptors respectively. Derenofylline suppresses cardiac fibrosis and attenuates albuminuria without affecting blood pressure in rats[1].
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产品名称 | Adenosine Receptor ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
ZM241385 | ✔ | 99%+ | |||||||||||||||||
Istradefylline |
+++
Adenosine A2A receptor, Ki: 2.2 nM |
98% | |||||||||||||||||
Reversine |
+
human A3 adenosine receptor, Ki: 0.66 μM |
98% | |||||||||||||||||
SCH58261 |
++++
bovine A2a, Ki: 2.0 nM rat A2a, Ki: 2.3 nM |
99%+ | |||||||||||||||||
A2A receptor antagonist 1 |
++
A1R, Ki: 264 nM A2AR, Ki: 4 nM |
99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Derenofylline (SLV 320) is a potent, selective, and orally active adenosine A1 receptor antagonist, with Ki values of 1 nM, 200 nM, and 398 nM for human A1, A3, and A2A receptors, respectively. Derenofylline mitigates cardiac fibrosis and reduces albuminuria in rats without affecting blood pressure [1]. |
Animal study | Derenofylline (0.3-10 mg/kg, orally administered) mitigates adenosine-induced bradycardia in rats [1].Derenofylline (10 mg/kg/d, oral administration, 12 weeks) diminishes myocardial fibrosis in 5/6 nephrectomy rats without altering blood pressure [1].Derenofylline (0.1-5 mg/kg, intravenous injection) does not induce major hemodynamic effects (heart rate and blood pressure) [1]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT00568009 | - | Terminated(additional enrolmen... 展开 >>t criteria made patients' recruitment not feasible anymore) 收起 << | November 2008 | - | |
NCT00160134 | Congestive Heart Failure | Phase 2 | Completed | - | Germany ... 展开 >> Site 1 Bad Nauheim, Germany 收起 << |
NCT00744341 | Acute Decompensated Heart Fail... 展开 >>ure; Renal Dysfunction 收起 << | Phase 2 | Terminated(This study was stop... 展开 >>ped 29OCT2009 due to strategic drug development considerations) 收起 << | - | - |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
3.24mL 0.65mL 0.32mL |
16.21mL 3.24mL 1.62mL |
32.43mL 6.49mL 3.24mL |
CAS号 | 251945-92-3 |
分子式 | C18H20N4O |
分子量 | 308.38 |
SMILES Code | O[C@H]1CC[C@H](NC2=C3C(NC=C3)=NC(C4=CC=CC=C4)=N2)CC1 |
MDL No. | MFCD12756289 |
别名 | Slv 320 |
运输 | 蓝冰 |
InChI Key | RBZNJGHIKXAKQE-UHFFFAOYSA-N |
Pubchem ID | 9953065 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place, sealed in dry, 2-8°C |
溶解方案 |
请根据您的动物给药指南选择适当的溶解方案。 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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