购物车
您的购物车当前为空
Valsartan
一键复制产品信息
很棒纯度: 99.76%
货号 T6716Cas号 137862-53-4
别名 缬沙坦, Tareg, Diovan, CGP 48933
Valsartan (CGP 48933) 是一种血管紧张素 II 受体拮抗剂，有用于高血压和心力衰竭的研究潜力。
其他形式的 “Valsartan”:
Valsartan
一键复制产品信息 很棒纯度: 99.76%
货号 T6716 别名 缬沙坦, Tareg, Diovan, CGP 48933Cas号 137862-53-4
Valsartan (CGP 48933) 是一种血管紧张素 II 受体拮抗剂，有用于高血压和心力衰竭的研究潜力。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 127 | 现货 | |
| 5 mg | ¥ 257 | 现货 | |
| 10 mg | ¥ 397 | 现货 | |
| 25 mg | ¥ 782 | 现货 | |
| 50 mg | ¥ 1,320 | 现货 | |
| 100 mg | ¥ 1,990 | 现货 | |
| 200 mg | ¥ 2,970 | 现货 | |
| 1 mL x 10 mM (in DMSO) | ¥ 246 | 现货 |
库存状态实时更新，以官网显示为准，现货产品可直接加购物车下单
大包装 & 定制
加入购物车
TargetMol的所有产品仅用作科学研究或药证申报，不能被用于人体，我们不向个人提供产品和服务。请您遵守承诺用途，不得违反法律法规规定用于任何其他用途。
产品介绍
Valsartan AI Summary
Valsartan exhibits a variety of pharmacokinetic and pharmacodynamic properties, demonstrating its potential as a pharmacologically active agent. The compound shows high affinity and potent inhibitory activity against the Angiotensin II receptor, type 1 (AT1), with IC50 values ranging from 1.4 to 2.7 nM in different experimental setups. It has an inhibition constant (Ki) of approximately 3.0 nM and demonstrates significant efficacy in reducing angiotensin II-induced pressor responses, underscoring its potential as an anti-hypertensive agent.
The compound has a half-life (T1/2) of approximately 6.1 hours and exhibits notable renal (CL_renal = 4.8 ml s^-1) and total clearance (CLtotal = 37.0 ml s^-1) rates, indicating efficient elimination from the body. Its low permeability across hexadecane membranes at pH 6.8 with a Log Pe of -5.0 cm s^-1, and slightly higher permeability at a pH range of 4-8 (Log Pe = -4.5 cm s^-1), suggest limited absorption in different pH environments, complemented by moderate gastrointestinal absorption of 55%.
Pharmacokinetically, Valsartan shows a low fraction unbound in plasma (Fu = 0.04), moderate oral bioavailability (25%), and a volume of distribution (Vdss) of 0.22 L/kg, reflecting its strong binding to plasma proteins and its pharmacological stability. It also exhibits mild to moderate impacts on liver enzyme activities, including elevated levels of SGOT, SGPT, and slight hepatotoxicity, signified by serum activity increases.
Additionally, the compound has shown variable antiviral activities, including limited inhibition of SARS-CoV-2 replication and cytotoxicity in Vero E6 and Caco-2 cells, as well as antibacterial effects against multiple bacterial strains with varying inhibition rates.
In multiple formats, Valsartan has demonstrated to be a versatile compound with significant therapeutic potential in cardiovascular diseases, and possibly other areas, given its comprehensive pharmacokinetic profile, inhibitory potency, and bioactivity spectrum against various targets. It also has implications for drug metabolism pathways, influencing key liver enzymes and transporters like OATP2B1, OATP1B1, and OATP1B3..
Note: Summary generated by AI. Data source: ChEMBL 
生物活性
化学信息
储存&溶解度
| 产品描述 | Valsartan (CGP 48933) is a tetrazole derivative and angiotensin II type 1 receptor blocker that is used to treat hypertension. |
| 体外活性 | Valsartan可促进胰岛素诱导的IRS-1的磷酸化,IRS-1与PI3K的P85调节亚基的结合,PI3-K活性及GLUT4易位到质膜.Valsartan可改善的葡萄糖耐受性,降低空腹血糖水平及西式饮食小鼠中血清胰岛素水平.在小鼠的胰岛中,Valsartan可使线粒体功能增强并防止西式饮食诱导的葡萄糖刺激的胰岛素分泌的降低.Valsartan阻断或减弱孤立脂肪细胞中西方饮食引起的几个关键的炎症信号表达的变化：IL-12p35,IL-12p40,TNF-α,IFN-γ,血小板12-脂氧合酶,胶原6,脂连蛋白,诱导型NO合成酶和AT1R. Valsartan显著增加胰岛素介导的2-[3H]脱氧-D-葡萄糖（2- [3H],DG）摄入到骨骼肌并减弱葡萄糖负荷后葡萄糖和胰岛素的浓度和血浆葡萄糖浓度.Valsartan也降低了TNF-α在KK-AY小鼠骨骼肌的表达和超氧化. |
| 体内活性 | Valsartan是有效的利尿剂,ACE抑制剂,钙拮抗剂和β-阻断剂。Valsartan剂量依赖性抑制对血管紧张素II诱导的血管有收缩作用,降低高血压的肾素依赖性模型的血压。 |
| 别名 | 缬沙坦, Tareg, Diovan, CGP 48933 |
| 分子量 | 435.52 |
| 分子式 | C24H29N5O3 |
| CAS No. | 137862-53-4 |
| Smiles | C(N([C@@H]([C@H](C)C)C(O)=O)C(CCCC)=O)C1=CC=C(C2=C(C=CC=C2)C=3NN=NN3)C=C1 |
| 密度 | 1.212g/cm3 |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | H2O: < 1 mg/mL (insoluble or slightly soluble)  DMSO: 250 mg/mL (574.03 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+90% Corn Oil: 2 mg/mL (4.59 mM), Sonication is recommeded. 请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。 | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
| ||||||||||||||||||||||||||||||||||||
计算器
体内实验配液计算器
请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：
比如您的给药剂量是10 mg/kg，每只动物体重20g，给药体积100 μL， 一共给药动物10只，您使用的配方为5%
DMSO + 30%PEG300 + 5%Tween 80 + 60%Saline/PBS/ddH2O， 那么您的工作液浓度为2mg/mL。 以上为“体内实验配液计算器”的使用方法举例，并不是具体某个化合物的推荐配制方式，请根据您的实验动物和给药方式选择适当的溶解方案。
剂量转换
对于不同动物的给药剂量换算，您也可以参考 更多
预览
Related Tags: buy Valsartan | purchase Valsartan | Valsartan cost | order Valsartan | Valsartan chemical structure | Valsartan in vivo | Valsartan in vitro | Valsartan formula | Valsartan molecular weight
嗨！有任何问题？点我咨询
版权所有©2015-2026 TargetMol Chemicals Inc.保留所有权利.
沪ICP备20019793号-4 | 沪公网安备 31010602006700号
| 沪(静)应急管危经许[2024]203441