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缬沙坦, AT 1 受体拮抗剂

高选择性,有效,竞争性AT 1受体拮抗剂
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货号 (SKU) 包装规格 是否现货 价格 数量
V129241-1g
1g 现货 Stock Image
V129241-5g
5g 现货 Stock Image
V129241-25g
25g 现货 Stock Image
V129241-100g
100g 现货 Stock Image

基本描述

别名 缬沙坦 | N-(1-氧代戊基)-N-[[2'-(2H-四唑-5-基)[1,1'-联苯]-4-基]甲基]-L-缬氨酸
英文别名 HSDB 7519 | Valsartan [USAN:USP:INN:BAN] | 80M03YXJ7I | Tareg | VALSARTAN (USP-RS) | MLS001424088 | VALSARTAN [INN] | ENTRESTO COMPONENT VALSARTAN | Spectrum_001796 | Miten | VALSARTAN [MART.] | VALSARTAN [VANDF] | VALSARTAN [EMA EPAR] | VALSARTAN [HSDB]
规格或纯度 Moligand™, ≥98%(HPLC)
英文名称 Valsartan
生化机理 缬沙坦是一种血管紧张素II 1型(AT1)受体拮抗剂和抗高血压药。缬沙坦可以防止由血压突然升高导致的心脏病发作和中风。 缬沙坦可降低心脏病发作幸存者的心肌梗死相关并发症。高度选择性,有效的竞争性AT 1受体拮抗剂(K i = 2.38 nM)。在体内显示出降压作用。显示中央和外围效果。口服具有活性
储存温度 -20°C储存
运输条件 超低温冰袋运输
作用类型 拮抗剂
作用机制 AT 1 受体拮抗剂
备注 需要更多关于溶解度,用法和处理的建议吗?请访问我们的常见问题(FAQ)页面以获取更多详细信息。
产品介绍

Valsartan是一种血管紧张素II受体拮抗剂,IC50在39.5到116 μM之间。使用缬沙坦治疗小鼠,以研究Ang II依赖性途径对醛固酮相关作用的影响。

Valsartan is an angiotensin II receptor antagonist with IC50 of ranging from 39.5 to 116 μM. Valsartan is an orally active specific angiotensin II receptor blocker used for the treatment of hypertension
A nonpeptide angiotensin II AT1 receptor antagonist.

纯度 ≥98%(HPLC)

产品属性

ALogP 4.4

关联靶点(人)

AGTR1 Tclin 1型血管紧张素II受体(Type-1 angiotensin II receptor) (3 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
PDE5A Tclin Phosphodiesterase 5A (5113 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ABL1 Tclin Tyrosine-protein kinase ABL (18331 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
EGFR Tclin Epidermal growth factor receptor erbB1 (33727 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CA2 Tclin Carbonic anhydrase II (17698 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ESR1 Tclin Estrogen receptor alpha (17718 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HMGCR Tclin HMG-CoA reductase (2475 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NR3C1 Tclin Glucocorticoid receptor (14987 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
INSR Tclin Insulin receptor (5558 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PGR Tclin Progesterone receptor (8562 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRB2 Tclin Beta-2 adrenergic receptor (11824 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CHRM2 Tclin Muscarinic acetylcholine receptor M2 (10671 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRB1 Tclin Beta-1 adrenergic receptor (6630 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR1A Tclin Serotonin 1a (5-HT1a) receptor (14969 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRA2A Tclin Alpha-2a adrenergic receptor (9450 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AR Tclin Androgen Receptor (11781 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CHRM1 Tclin Muscarinic acetylcholine receptor M1 (12690 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ACE Tclin Angiotensin-converting enzyme (1423 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DRD2 Tclin Dopamine D2 receptor (23596 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MAOA Tclin Monoamine oxidase A (11911 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CNR1 Tclin Cannabinoid CB1 receptor (20913 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DRD1 Tclin Dopamine D1 receptor (9720 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DRD4 Tchem Dopamine D4 receptor (7907 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ACHE Tclin Acetylcholinesterase (18204 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PTGS1 Tclin Cyclooxygenase-1 (9233 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLC6A2 Tclin Norepinephrine transporter (10102 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HRH2 Tclin Histamine H2 receptor (5428 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRA1D Tclin Alpha-1d adrenergic receptor (4171 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR1B Tclin Serotonin 1b (5-HT1b) receptor (2801 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR2A Tclin Serotonin 2a (5-HT2a) receptor (14758 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR2C Tclin Serotonin 2c (5-HT2c) receptor (11471 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADORA1 Tclin Adenosine A1 receptor (17603 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AGTR1 Tclin Type-1 angiotensin II receptor (5176 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CALCR Tclin Calcitonin receptor (2215 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLC6A4 Tclin Serotonin transporter (12625 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRA1A Tclin Alpha-1a adrenergic receptor (8359 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PTGS2 Tclin Cyclooxygenase-2 (13999 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HRH1 Tclin Histamine H1 receptor (7573 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRA1B Tclin Alpha-1b adrenergic receptor (2912 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OPRM1 Tclin Mu opioid receptor (19785 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DRD3 Tclin Dopamine D3 receptor (14368 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AVPR1A Tclin Vasopressin V1a receptor (5412 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OPRD1 Tclin Delta opioid receptor (15096 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OPRK1 Tclin Kappa opioid receptor (16155 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLC6A3 Tclin Dopamine transporter (10535 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
KCNH2 Tclin HERG (29587 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR4 Tclin Serotonin 4 (5-HT4) receptor (2068 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ESR2 Tclin Estrogen receptor beta (9272 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYSLTR1 Tclin Cysteinyl leukotriene receptor 1 (2118 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ERBB2 Tclin Receptor protein-tyrosine kinase erbB-2 (7851 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CHRM4 Tclin Muscarinic acetylcholine receptor M4 (6041 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

关联靶点(其它种属)

Agtr2 Angiotensin II type 2 (AT-2) receptor (803 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Mc4r Melanocortin receptor 4 (1205 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Ltc4s Leukotriene C4 synthase (1 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Agtr1b Type-1B angiotensin II receptor (525 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Sigmar1 Sigma opioid receptor (160 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Npy1r Neuropeptide Y receptor type 1 (8 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Cckar Cholecystokinin A receptor (90 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Aplnr Apelin receptor (201 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Nos2 Nitric oxide synthase, inducible (3573 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Mapk1 MAP kinase ERK2 (650 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Hdac6 Histone deacetylase 6 (222 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Mmp9 Matrix metalloproteinase 9 (38 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Fgfr3 Fibroblast growth factor receptor 3 (21 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Agtr1 Type-1A angiotensin II receptor (520 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Pseudomonas aeruginosa (123386 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Klebsiella pneumoniae (43867 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Staphylococcus aureus (210822 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Acinetobacter baumannii (41033 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Escherichia coli (133304 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Cryptococcus neoformans (21258 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Candida albicans (78123 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Oryctolagus cuniculus (11301 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Rattus norvegicus (775804 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
NIH3T3 (5395 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Luciferin 4-monooxygenase (66902 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Gpr119 Glucose-dependent insulinotropic receptor (270 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Plasma (328 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Agtr1b Angiotensin II receptor (AT-1) type-1 (1480 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Liver microsome (341 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Glra2 Glycine receptor (1745 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SARS-CoV-2 (38078 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

作用机制

作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献

名称和识别符

EC号 604-045-2, 695-249-0
分子类型 小分子
IIUPAC Name (2S)-3-methyl-2-[pentanoyl-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]amino]butanoic acid
INCHI 1S/C24H29N5O3/c1-4-5-10-21(30)29(22(16(2)3)24(31)32)15-17-11-13-18(14-12-17)19-8-6-7-9-20(19)23-25-27-28-26-23/h6-9,11-14,16,22H,4-5,10,15H2,1-3H3,(H,31,32)(H,25,26,27,28)/t22-/m0/s1
InChi Key ACWBQPMHZXGDFX-QFIPXVFZSA-N
Smiles CCCCC(=O)N(CC1=CC=C(C=C1)C2=CC=CC=C2C3=NNN=N3)C(C(C)C)C(=O)O
Isomeric SMILES CCCCC(=O)N(CC1=CC=C(C=C1)C2=CC=CC=C2C3=NNN=N3)[C@@H](C(C)C)C(=O)O
关联CAS 137862-53-4
NSC Number 758927
MeSH Entry Terms 48933, CGP;CGP 48933;Diovan;Kalpress;Miten;N-valeryl-N-((2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl)valine;Nisis;Provas;Tareg;Vals;valsartan
分子量 435.52
Reaxy-Rn 24721853
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=24721853&ln=

化学和物理性质

溶解性 Soluble in Ethanol and Methanol
敏感性 对湿度敏感
比旋光度 -65°C
熔点 117°C
分子量 435.500 g/mol
XLogP3 4.400
氢键供体数Hydrogen Bond Donor Count 2
氢键受体数Hydrogen Bond Acceptor Count 6
可旋转键计数Rotatable Bond Count 10
精确质量Exact Mass 435.227 Da
单同位素质量Monoisotopic Mass 435.227 Da
拓扑极表面积Topological Polar Surface Area 112.000 Ų
重原子数Heavy Atom Count 32
形式电荷Formal Charge 0
复杂度Complexity 608.000
同位素原子数Isotope Atom Count 0
定义的原子立体中心计数Defined Atom Stereocenter Count 1
未定义的原子立体中心计数Undefined Atom Stereocenter Count 0
定义的键立体中心计数Defined Bond Stereocenter Count 0
未定义的键立体中心计数Undefined Bond Stereocenter Count 0
所有立体化学键的总数The total count of all stereochemical bonds 0
共价键合单元计数Covalently-Bonded Unit Count 1

安全和危险性(GHS)

象形图 GHS08
信号词 警告
危险声明

H361: 怀疑破坏生育力或未出生的孩子

H412: 对水生生物有害并具有长期持续影响

预防措施声明

P273: 避免释放到环境中。

P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。

P405: 密闭存放

P501: 将内容物/容器处理到。。。

P203: 使用前,获取、阅读并遵守所有安全说明。

P318: 如果暴露或担心,请就医。

WGK Germany 3
Merck Index 9916

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批号(Lot Number) 证书类型 货号
G2511094 分析证书 V129241
B2318250 分析证书 V129241
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K2127016 分析证书 V129241
K2127017 分析证书 V129241
E1526061 分析证书 V129241
J2418270 分析证书 V129241
B2318251 分析证书 V129241
H2407057 分析证书 V129241
G2216548 分析证书 V129241
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引用文献

1. Qinglin Wang, Hao Yuan, Xinyue Pan, Yiling Yang, Xiaosong Ma, Yahui Guo.  (2024)  Synthesis of silver nanoclusters using a double-stranded DNA template and its application for captopril detection.  JOURNAL OF FOOD COMPOSITION AND ANALYSIS,  126  (105825).  [10.1016/j.jfca.2023.105825]
2. Huimin Zhou, Zhiwei Qiu, Jin Zeng, Ruobin Dai, Zhiwei Wang.  (2023)  Ultra-permeable polyamide nanofiltration membrane modified by hydrophilic-hydrophobic alternated lignocellulosic nanofibrils for efficient water reuse.  JOURNAL OF MEMBRANE SCIENCE,  688  (122125).  [10.1016/j.memsci.2023.122125]
3. Zhiren Zou, Qiang Huang, Xiaobo Li, Xianzhi Liu, Lina Yin, Yunjie Zhao, Guang Liang, Wenqi Wu.  (2023)  Dissolution changes in drug-amino acid/biotin co-amorphous systems: Decreased/increased dissolution during storage without recrystallization.  EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES,  188  (106526).  [PMID:37442486] [10.1016/j.ejps.2023.106526]
4. Mingkang Zhang, Ruirui Cui, Yan Zhou, Yanrong Ma, Yongwen Jin, Lina Wang, Wen Kou, Xin’an Wu.  (2023)  Accumulation of Renal Fibrosis in Hyperuricemia Rats Is Attributed to the Recruitment of Mast Cells, Activation of the TGF-β1/Smad2/3 Pathway, and Aggravation of Oxidative Stress.  INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES,  24  (13): (10839).  [PMID:37446016] [10.3390/ijms241310839]
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8. Lin Chen, Li Ge, Qinghui Liang, Zhenbo Zhao, Kedi Yang.  (2022)  Eutectic solvents formed by (+)-DTTA and L-menthol as novel chiral recognition and separation media for enantioselective extraction of valsartan enantiomers.  JOURNAL OF MOLECULAR LIQUIDS,  368  (120818).  [10.1016/j.molliq.2022.120818]
9. Ke Lin, Wu Luo, Na Yang, Lan Su, Hao Zhou, Xiang Hu, Yi Wang, Zia A. Khan, Weijian Huang, Gaojun Wu, Guang Liang.  (2022)  Inhibition of MyD88 attenuates angiotensin II-induced hypertensive kidney disease via regulating renal inflammation.  INTERNATIONAL IMMUNOPHARMACOLOGY,  112  (109218).  [PMID:36116148] [10.1016/j.intimp.2022.109218]
10. Wang Yiran, Shi Jihua, Dai Dapeng, Cai Jianping, Wang Shuanghu, Hong Yun, Zhou Shan, Zhao Fangling, Zhou Quan, Geng Peiwu, Zhou Yunfang, Xu Xue, Luo Qingfeng.  (2022)  Evaluation of commonly used cardiovascular drugs in inhibiting vonoprazan metabolism in vitro and in vivo.  Frontiers in Pharmacology,  13  [PMID:36052128] [10.3389/fphar.2022.909168]
11. Yan Zhou, Mengmeng Wei, Mingkang Zhang, Jianping Zhang, Fabing Tang, Xin’an Wu.  (2022)  Adefovir accumulation in the renal interstitium triggers mast cell degranulation and promotes renal interstitial fibrosis.  TOXICOLOGY LETTERS,  359  (10).  [PMID:35114312] [10.1016/j.toxlet.2022.01.018]
12. Xiao Juan Liu, Yang Zhang, Xue Zhong Wang.  (2020)  Study on Co-Crystallization of LCZ696 Using In Situ ATR-FTIR and Imaging.  Crystals,  10  (10): (922).  [10.3390/cryst10100922]
13. Qi Liang, Xiaoying Fu, Jianfeng Zhang, Jiaxue Hao, Gangjun Feng, Jing Wang, Qian Li, Faizan Ahmad, Xinfeng Zhao.  (2020)  Immobilized angiotensin II type I receptor: A powerful method of high throughput screening for antihypertensive compound identification through binding interaction analysis.  JOURNAL OF CHROMATOGRAPHY A,  1620  (461003).  [PMID:32156458] [10.1016/j.chroma.2020.461003]
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