氯沙坦 - CAS:114798-26-4 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	氯沙坦促销
英文名称:	Losartan
别名:	洛沙坦 (2-butyl-4-chloro-1-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-imidazol-5-yl)methanol
CAS No:	114798-26-4	分子式:	C₂₂H₂₃ClN₆O	分子量:	422.91
CAS No:	114798-26-4
分子式:	C₂₂H₂₃ClN₆O
分子量:	422.91
MDL:	MFCD00865831

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L10019 氯沙坦 ≥95% (psaitong)

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熔点：

183.5-184.5 °C

包装规格：

1g 5g 25g in poly bottle

溶解性：

溶解在乙醇（100mM）和DMSO（100mM）。

产品描述：

基本信息

产品编号：	L10019
产品名称：	Losartan
CAS:	114798-26-4	储存条件	粉末	室温	四年

分子式：	C22H23ClN6O		溶于液体	-80℃	6个月
分子量：	422.91			-20℃	1个月
化学名：	2-butyl-4-chloro-1-[p-(o-1h-tetrazol-5-ylphenyl)benzyl]imidazole-5- methanol
Solubility (25°C)：
体外:	DMSO	82mg/mL (193.89mM)
	Ethanol	82mg/mL (193.89mM)
	Water	Insoluble
体内(现配现用):
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	2.3646mL	11.8228mL	23.6457mL
5mM	0.4729mL	2.3646mL	4.7291mL
10mM	0.2365mL	1.1823mL	2.3646mL
50mM	0.0473mL	0.2365mL	0.4729mL

生物活性

产品描述	一种血管紧张素II受体1型（AT1）的一种有效的非肽类拮抗剂。这种受体启动一个信号级联，导致血管收缩。这种受体的拮抗作用通过阻断血管紧张素Ⅱ的信号而引起血管舒张。
靶点	IC50:20nM (angiotensin II)
体外研究	Losartan competes with the binding of angiotensin II to AT1 receptors.The concentration that inhibits 50% of the binding of angiotensin II (IC50) is 20nM.Losartan (40μM) affects ISC but prevents the effect of ANGII on ISC.Losartan significantly reduces Ang II-mediated cell proliferation in endometrial cancer cells.The combination of losartan and anti-miR-155 has a significantly greater antiproliferative effect compared to each drug alone.
体内研究	Losartan (0.6g/L,p.o.) -treated Fbn1C1039G/+mice show a reduction in distal airspace caliber relative to placebo-treated Fbn1C1039G/+animals.The doses of losartan and propranolol are titrated to achieve comparable hemodynamic effects.Analysis of pSmad2 nuclear staining reveals that losartan antagonizes TGF-β signaling in the aortic wall of Fbn1C1039G/+mice.Losartan can improve disease manifestations in the lungs,an event that cannot plausibly relate to improved hemodynamics.Losartan (10mg/kg,intraarterial injection) increases blood angiotensin levels four-to sixfold.Losartan (10mg/kg,i.p.) increases plasma renin levels 100-fold;plasma angiotensinogen levels decreases to 24% of control;and plasma aldosterone levels are unchanged.

推荐实验方法(仅供参考)

细胞实验:

An MTT assay is used to measure cell proliferation and viability.For the assay,5000 cells in 200μL media per well are seeded in a 96 well plate.After overnight incubation to allow for cell attachment,the medium is removed by suction.MTT at 1mg/mL concentration in serum-free medium is added and then incubated for 4h at 37℃.After removal of MTT solution,100μL of DMSO is added to dissolve formazan crystals.Absorbance at 570nm and at 600nm as a reference is then measured using a microplate reader.The difference in absorbance is thus relative to the extent of cell survival.

动物实验:

Female Fbn1C1039G/+mice undergo timed matings with wild-type male mice.At 14.5d post-coitum,pregnant female Fbn1 C1039G/+mice are treated with oral losartan (0.6g/L in drinking water;n=10),propranolol (0.5g/L;n=6) or placebo (n=12).Therapy is continued throughout lactation and after weaning until 10 months of age.Mice are sacrificed and examined using the techniques described above.Propranolol is used for comparison with losartan because β-adrenergic receptor blockade is the current albeit controversial standard of care to modulate abnormal growth of the aortic root in MFS.Beginning at 7 weeks of age,wild-type and Fbn1C1039G/+mice are treated with oral losartan (0.6g/L in drinking water;n=5),propranolol (0.5g/L;n=7) or placebo (n=10).Mice are continued on oral therapy for 6 months and then sacrificed.

保存条件：

室温

UN码：

HazardClass：

危害声明：

安全说明：

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