CAS |
124750-99-8 |
Chinese Name |
氯沙坦钾 |
English Name |
Losartan Potassium |
Synonyms |
氯沙坦钾;科素亚钾盐;氯沙坦钾盐;洛沙坦钾; |
Molecular Formula |
C22H22CIKN6O |
Molecular Weight |
461 |
Solubility |
Soluble in DMSO ≥25mg/mL |
Purity |
HPLC≥98% |
Appearance |
White to off-white Solid |
Storage |
Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
EC |
EINECS 200-287-4 |
MDL |
MFCD02092704 |
SMILES |
OCC1=C(Cl)N=C(CCCC)N1CC2=CC=C(C3=CC=CC=C3C4=N[N-]N=N4)C=C2.[K+] |
InChIKey |
OXCMYAYHXIHQOA-UHFFFAOYSA-N |
InChI |
InChI=1S/C22H22ClN6O.K/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;/q-1;+1 |
PubChem CID |
11751549 |
Target Point |
Angiotensin Receptor |
Passage |
GPCR & G Protein |
Background |
It is an angiotensin II receptor type 1 (AT1) antagonist. |
Biological Activity |
Losartan potassium是血管紧张素II受体1型 (AT1)拮抗剂,与血管紧张素II与AT1的结合竞争,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 |
50mg 10mM*1mL in DMSO 100mg |