中文名 | 缬沙坦 |
英文名 | Valsartan |
别名 | 缬沙坦 缬沙坦相关物A (R)-缬沙坦 缬沙坦EP杂质A 缬沙坦相关物质A 盐酸氨溴索杂质D 缬沙坦(标准品) 缬沙坦相关化合物A 缬沙坦USP相关物质A 原研CGP 49309 缬沙坦(盐酸氨溴索杂质D) 缬沙坦溶液, 100PPM 缬沙坦, 一种非肽类血管紧张素II AT1受体拮抗剂 N-(1-戊酰基)-N-[4-[2-(1H-四氮唑-5-基)苯基]苄基]-L-缬氨酸 N-戊酰基-N-[[2'-(1H-四唑-5-基)[1,1'-联苯]-4-基]甲基]-D-缬氨酸 N-((2'-(1H-四唑-5-基)-[1,1'-联苯]-3-基)甲基)-N-戊酰基-L-缬氨酸 N-(1-氧代戊基)-N-[[2'-(1H-四氮唑-5-基)[1,1'-联苯]-3-基]甲基]-L-缬氨酸 (R)-2-(N-((2'-(1H-四唑-5-基)-[1,1'-联苯]-4-基)甲基)戊氨基)-3 - 甲基丁酸 |
英文别名 | Valsartan ent-Valsartan VALSARTAN IMP C Valsartan(Diovan) Valsartan R-enantiomer Valsartan Related Compound A Ambroxol Hydrochloride Imp.D (R)-2-(N-((2'-(1H-tetrazol-5-yl) N-pentanoyl-N-{[2'-(2H-tetrazol-5-yl)biphenyl-4-yl]methyl}valine (S)-N-Valeryl-N-([2'-(1H-tetrazole-5-yl)biphen-4-yl]methyl)valine N-pentanoyl-N-{[2'-(2H-tetrazol-5-yl)biphenyl-4-yl]methyl}-L-valine N-pentanoyl-N-{[2'-(2H-tetrazol-5-yl)biphenyl-4-yl]methyl}-D-valine N-((2'-(1H-Tetrazol-5-yl)-[1,1'-biphenyl]-3-yl)methyl)-N-pentanoyl-L-valine N-(1-Oxopentyl)-N-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-3-yl]methyl]-L-valine N-(1-OXOPENTYL)-N-[[2'-(1H-TETRAZOL-5-YL)[1,1'-BIPHENYL]-4-YL]METHYL]-L-VALINE L-Valine, N-(1-oxopentyl)-N-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]- L-VALINE,N-(1-OXOPENTYL)-N-[[2''-(1H-TETRAZOL-5-YL)[1,1''-BIPHENYL]-3-YL]METHYL]- (R)-2-[N-[[2'-(5-Tetrazolyl)-4-biphenylyl]methyl]pentanamido]-3-methylbutanoic Acid D-Valine, N-(1-oxopentyl)-N-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]- (9CI) L-Valine, N-(1-oxopentyl)-N-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-3-yl]methyl]- (9CI) 3-Methyl-2-[pentanoyl-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]amino]-butanoic aci 3-methyl-2-[pentanoyl-[[4-[2-(2h-tetrazol-5-yl)phenyl]phenyl]methyl]amino]-butanoic acid (S)-2-(N-((2'-(1H-Tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic aci (R)-2-(N-((2'-(1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid (S)-N-(1-carboxy-2-methyl-prop-1-yl)-N-pentanoyl-N-[(2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl]amine |
CAS | 137862-53-4 137863-60-6 137862-87-4 |
EINECS | 1592732-453-0 |
化学式 | C24H29N5O3 |
分子量 | 435.52 |
InChI | InChI=1/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-/m1/s1 |
InChIKey | ACWBQPMHZXGDFX-QFIPXVFZSA-N |
密度 | 1.212±0.06 g/cm3(Predicted) |
熔点 | 116-117°C |
沸点 | 684.9±65.0 °C(Predicted) |
闪点 | 368°C |
水溶性 | 84.99mg/L(25 ºC) |
蒸汽压 | 1.06E-19mmHg at 25°C |
溶解度 | DMSO: ≥ 20 mg/mL |
折射率 | 1.586 |
酸度系数 | 3.56±0.10(Predicted) |
存储条件 | 2-8°C |
稳定性 | 吸湿性 |
敏感性 | Easily absorbing moisture |
外观 | 粉末 |
颜色 | white to tan |
Merck | 14,9916 |
物化性质 | 从二异丙醚结晶,熔点116--117℃。 |
MDL号 | MFCD00865840 |
体外研究 | Valsartan剂量依赖性抑制血管紧张素II诱导的血管收缩,降低高血压的肾素依赖性模型的血压。Valsartan是至少一样有效的ACE抑制剂,利尿剂,β-阻断剂和钙拮抗剂。 |
体内研究 | Valsartan导致改善的葡萄糖耐受性,降低的空腹血糖水平,并降低西式饮食小鼠中血清胰岛素水平。Valsartan治疗抑制西式饮食诱导的促炎症的血清细胞因子干扰素γ和单核细胞趋化蛋白1的增加。在小鼠的胰岛中,Valsartan增强线粒体功能并防止西式饮食诱导的葡萄糖刺激的胰岛素分泌的降低。在孤立的脂肪细胞,Valsartan阻断或减弱西方饮食引起的几个关键的炎症信号表达的变化:白细胞介素12p40,白细胞介素12p35,肿瘤坏死因子-α,干扰素-γ,脂连蛋白,血小板12-脂氧合酶,胶原6,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治疗促进胰岛素诱导的IRS-1的磷酸化,IRS-1和磷酸肌醇3-激酶(PI3-k)的P85调节亚基的结合,PI3-K活性,和GLUT4易位到质膜。Valsartan也降低了肿瘤坏死因子-α(TNF-α)在KK-AY小鼠的骨骼肌表达和超氧化。 |
危险品标志 | Xi - 刺激性物品 |
风险术语 | 36/37/38 - 刺激眼睛、呼吸系统和皮肤。 |
安全术语 | S26 - 不慎与眼睛接触后,请立即用大量清水冲洗并征求医生意见。 S37/39 - 戴适当的手套和护目镜或面具。 |
WGK Germany | 3 |
RTECS | YV9455000 |
海关编号 | 29339900 |
上游原料 | 2'-氰基联苯-4-醛 正戊酰氯 氰基硼氢化钠 三正丁基叠氮化锡 5-(2-溴苯基)-1-三苯甲基-1H-四氮唑 缬沙坦氰基类似物甲基酯 |
参考资料 展开查看 | 1. Niu, Guanghao, et al. "Marein ameliorates Ang II/hypoxia‐induced abnormal glucolipid metabolism by modulating the HIF‐1α/PPARα/γ pathway in H9c2 cells." Drug Development Research 82.4 (2021): 523-532.https://doi.org/10.1002/ddr.21770 2. Niu, Guanghao, et al. "Marein ameliorates Ang II/hypoxia‐induced abnormal glucolipid metabolism by modulating the HIF‐1α/PPARα/γ pathway in H9c2 cells." Drug Development Research 82.4 (2021): 523-532.https://doi.org/10.1002/ddr.21770 3. Zhu, Zeng-Yan, et al. "Apigenin-induced HIF-1α inhibitory effect improves abnormal glucolipid metabolism in AngⅡ/hypoxia-stimulated or HIF-1α-overexpressed H9c2 cells." Phytomedicine 62 (2019): 152713.https://doi.org/10.1016/j.phymed.2018.10.010 |
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