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My CartCAS：863031-21-4
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 863031-21-4 |
| Name | Azilsartan Medoxomil |
| Molecular Formula | C30H24N4O8 |
| Molecular Weight | 568.53 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 1308068-626-2 |
| MDL | MFCD19443688 |
| SMILES | O=C(C1=C2C(N=C(OCC)N2CC3=CC=C(C4=CC=CC=C4C5=NC(ON5)=O)C=C3)=CC=C1)OCC6=C(C)OC(O6)=O |
| Target Point | Angiotensin Receptor（AT1 receptor） |
| Passage | GPCR & G Protein |
| Background | Azilsartan Medoxomil is a potent angiotensin II type 1 (AT1) receptor antagonist that inhibits RAAS with >10,000-fold selectivity over AT2 |
| Biological Activity | Azilsartan Medoxomil (TAK-491)是一种有效的angiotensin II type 1 (AT1) receptor（血管紧张素II 1型受体）拮抗剂，抑制RAAS比作用于AT2选择性高10，000倍以上，用于治疗高血压。[1-2] |
| In Vitro | Azilsartan medoxomil是一种前药，在肠道和血浆中通过酯水解能够迅速转化为活性部分，azilsartan(TAK-536)。 在血管平滑肌和肾上腺中，Azilsartan选择性阻断血管紧张素II与AT1(1型血管紧张素II)受体的结合，从而促进血管舒张并降低醛固酮的效果。[2] Azilsartan是AT1受体的高选择性拮抗剂，IC50为2.6 nM，对AT1受体的亲和力是AT2受体的10，000多倍，并且对其它心脏受体或离子通道没有亲和力。Azilsartan的抑制作用在游离化合物冲洗后仍然存在(IC50值为7.4 nM)。Azilsartan也会抑制血管紧张素II诱导的肌醇-1-磷酸(IP1)在细胞水平测定中的积累，IC50值为9.2 nM，并且这种作用耐冲洗(IC50值为81.3 nM)。[1] |
| Animal Experiment | 人类AT1表达质粒转染24小时后，通过改变培养基中饥饿缓冲液(1 mM CaCl2，0.5 mM MgCl2，4.2 mM KCl，146 mM NaCl，5.5 mM 葡萄糖，和10 mM HEPES，pH 7.3)使细胞饥饿。随后，溶解在饥饿缓冲液中的5微升/孔的测试化合物以指示浓度加入到细胞中，并将其按指示时间预处理。饥饿处理2小时后，LiCl加入到终浓度为50 mM，含有或不含血管紧张素II 10 nM，细胞在37°C下按照指示时间进一步培育。冲刷实验中，在血管紧张素II刺激前，用100微升/孔的饥饿缓冲液清洗细胞以除去未结合的化合物。[1] |
| Data Literature Source | [1] Ojima M，et al. J Pharmacol Exp Ther，2011，336(3)，801-808. [2] Zaiken K，et al. Clin Ther，2011，33(11)，1577-1589. |
| Unit | Bottle |
| Specification | 5mg 10mg 20mg |
Azilsartan Medoxomil是一种有效的angiotensin II type 1 (AT1) receptor（血管紧张素II 1型受体）拮抗剂，抑制RAAS比作用于AT2选择性高10，000倍以上
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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