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My CartCAS：114798-26-4
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 | 114798-26-4 |
| Name | Losartan |
| Molecular Formula | C22H23ClN6O |
| Molecular Weight | 422.91 |
| 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 601-329-8 |
| MDL | MFCD00865831 |
| SMILES | OCC1=C(Cl)N=C(CCCC)N1CC2=CC=C(C3=CC=CC=C3C4=NNN=N4)C=C2 |
| InChIKey | PSIFNNKUMBGKDQ-UHFFFAOYSA-N |
| InChI | InChI=1S/C22H23ClN6O/c1-2-3-8-20-24-21(23)19(14-30)29(20)13-15-9-11-16(12-10-15)17-6-4-5-7-18(17)22-25-27-28-26-22/h4-7,9-12,30H,2-3,8,13-14H2,1H3,(H,25,26,27,28) |
| PubChem CID | 3961 |
| Target Point | Angiotensin Receptor |
| Passage | GPCR & G Protein |
| Background | Losartan is an angiotensin II receptor antagonist that competes with angiotensin II for binding to the AT1 receptor. |
| Biological Activity | Losartan 是血管紧张素II受体拮抗剂，与血管紧张素II竞争性结合AT1受体，IC50为20 nM。[1-5] |
| In Vitro | 氯沙坦与血管紧张素II与AT1受体的结合竞争。抑制50％血管紧张素II结合的浓度(IC50)为20 nM [1]。氯沙坦(40μM)影响ISC，但阻止ANGII对ISC的影响[2]。氯沙坦显著降低Ang II介导的子宫内膜癌细胞的增殖。与单独使用每种药物相比，氯沙坦和抗miR-155的组合具有显著更高的抗增殖作用[3]。 |
| In Vivo | 与安慰剂治疗的Fbn1C1039G/+动物相比，氯沙坦(0.6g/L，po)处理的Fbn1C1039G/+小鼠显示远端空气口径减少。滴定氯沙坦和普萘洛尔的剂量以达到相当的血液动力学效果。对pSmad2核染色的分析显示氯沙坦拮抗Fbn1C1039G/+小鼠的主动脉壁中的TGF-β信号传导。氯沙坦可以改善肺部的疾病表现，这一事件与改善血液动力学无关[4]。氯沙坦(10 mg/kg，动脉内注射)使血液中的血管紧张素水平增加4到6倍。氯沙坦(10 mg/kg，ip)使血浆肾素水平增加100倍;血浆血管紧张素原水平降低至对照的24％;和血浆醛固酮水平没有变化[5]。 |
| Cell Experiment | MTT测定用于测量细胞增殖和活力。对于测定，将每孔200μL培养基中的5000个细胞接种在96孔板中。在孵育过夜以允许细胞附着后，通过抽吸除去培养基。加入无血清培养基中1mg/mL浓度的MTT，然后在37℃下孵育4小时。除去MTT溶液后，加入100μLDMSO以溶解甲crystals晶体。然后使用酶标仪测量570nm处和600nm处的吸光度作为参考。因此，吸光度的差异与细胞存活的程度有关。 |
| Animal Experiment | 雌性Fbn1C1039G/+小鼠与野生型雄性小鼠进行定时交配。在交配后14.5d，怀孕的雌性Fbn1C1039G/+小鼠用口服氯沙坦(饮用水中0.6g/L; n = 10)，普萘洛尔(0.5g/L; n = 6)或安慰剂(n = 12)治疗。 。在整个哺乳期和断奶后持续治疗至10个月大。使用上述技术处死小鼠并检查。普萘洛尔用于与氯沙坦进行比较，因为β-肾上腺素能受体阻断是目前虽然有争议的调节标准，用于调节MFS中主动脉根的异常生长。从7周龄开始，野生型和Fbn1C1039G/+小鼠用口服氯沙坦(饮用水中0.6 g/L; n = 5)，普萘洛尔(0.5 g/L; n = 7)或安慰剂(n = 10)。小鼠继续口服治疗6个月，然后处死。 |
| Data Literature Source | [1]. Burnier，M. Angiotensin II type 1 receptor blockers. Circulation，2001. 103(6): p. 904-12. [2]. Ashry，O.，et al. Evidence for expression and function of angiotensin II receptor type 1 in pulmonary epithelial cells. Respir Physiol Neurobiol，2014. [3]. Choi，C.H.，et al. Angiotensin II type I receptor and miR-155 in endometrial cancers: synergistic antiproliferative effects of anti-miR-155 and losartan on endometrial cancer cells. Gynecol Oncol，2012. 126(1): p. 124-31. [4]. Habashi，J.P.，et al. Losartan，an AT1 antagonist，prevents aortic aneurysm in a mouse model of Marfan syndrome. Science，2006. 312(5770): p. 117-21. [5]. Campbell，D.J.，et al. Effects of losartan on angiotensin and bradykinin peptides and angiotensin-converting enzyme. J Cardiovasc Pharmacol，1995. 26(2): p. 233-40. |
| Unit | Bottle |
| Specification | 100mg 200mg 500mg 1g |
Losartan 是血管紧张素II受体拮抗剂，与血管紧张素II竞争性结合AT1受体。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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