规格 | 价格 | 库存 | 数量 |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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体外研究 (In Vitro) |
可溶性鸟苷酸环化酶(sGC)是一氧化氮(NO)信号通路中的关键酶[1]。 Riociguat 不仅通过细胞色素 P450 同工酶 3A4 (CYP3A4)、CYP2C8 和 CYP2J2 代谢为 BAY60-4552,还通过位于肝脏和肺部的 CYP1A1 代谢为 BAY60-4552[2]。
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体内研究 (In Vivo) |
GSK2181236A 和 BAY 60-4552 对高血压引起的终末器官损伤具有部分益处。在自发性高血压、易发生中风的大鼠中,低剂量的 BAY 60-4552 可减少尿量并提高生存率。高剂量还可以减少尿量,此外还可以减少微量白蛋白尿并减弱平均动脉压的增加。 BAY 60-4552 0.3 和 3 mg/kg/天的剂量均可将生存率提高 46% 和 69%。 BAY 60-4552(0.3 和 3.0 mg/kg/天)治疗七周,剂量依赖性地将尿量降低至 79±11 和 56±10 mL/天[1]。 BAY 60-4552 和伐地那非具有协同有益作用,因此可能挽救根治性前列腺切除术后 PDE5 抑制剂治疗失败的患者[3]。
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动物实验 |
Rats: Oral gavage of rats is performed two hours before ischemia with vehicle (0.5% HPMC, 5% DMSO, and 0.1% Tween 80; 10 mL/kg; n=14), GSK2181236A (0.1 or 1.0 mg/kg; n=11–14), or BAY 60-4552 (0.3 or 3.0 mg/kg; n=10–12). Both when ischemia first occurs and 24 hours after reperfusion, blood is drawn. For analysis, plasma is obtained[1].
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参考文献 |
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分子式 |
C19H17FN8O2
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分子量 |
408.38908
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精确质量 |
408.15
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元素分析 |
C, 55.88; H, 4.20; F, 4.65; N, 27.44; O, 7.84
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CAS号 |
625115-52-8
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外观&性状 |
Solid powder
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SMILES |
COC(=O)NC1=C(N=C(N=C1N)C2=NN(C3=C2C=CC=N3)CC4=CC=CC=C4F)N
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InChi Key |
FTQHGWIXJSSWOY-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C19H17FN8O2/c1-30-19(29)24-14-15(21)25-17(26-16(14)22)13-11-6-4-8-23-18(11)28(27-13)9-10-5-2-3-7-12(10)20/h2-8H,9H2,1H3,(H,24,29)(H4,21,22,25,26)
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化学名 |
methyl N-[4,6-diamino-2-[1-[(2-fluorophenyl)methyl]pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl]carbamate
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别名 |
Nelociguat; BAY604552; BAY-604552; BAY 604552; BAY60-4552; BAY 60-4552; BAY-60-4552
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HS Tariff Code |
2934.99.9001
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外) |
DMSO: < 1 mg/mL
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溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.09 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.09 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. 请根据您的实验动物和给药方式选择适当的溶解配方/方案: 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4486 mL | 12.2432 mL | 24.4864 mL | |
5 mM | 0.4897 mL | 2.4486 mL | 4.8973 mL | |
10 mM | 0.2449 mL | 1.2243 mL | 2.4486 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。
Effects of the sGC heme-site inhibitor ODQ on GSK2181236A- and BAY 60-4552-mediated P-VASP formation and vasodilation. Front Pharmacol . 2012 Jul 5:3:128. td> |
Effect of GSK2181236A and BAY 60-4552 on (A) heart rate and (B) mean arterial pressure (MAP) in normotensive Sprague Dawley rats. Front Pharmacol . 2012 Jul 5:3:128. td> |
Effect of GSK2181236A and BAY 60-4552 on cardiac ischemia/reperfusion injury in Sprague Dawley rats (n = 10–14 per group). Front Pharmacol . 2012 Jul 5:3:128. td> |
Chronic administration of GSK2181236A and BAY 60-4552 enhanced (A) survival and similarly, but not significantly, reduced (B) blood pressure in age-matched, radiotelemetered HSFD SHR-SPs. Front Pharmacol . 2012 Jul 5:3:128. td> |