货号:A561984 同义名: DuP-753 potassium;Losartan (potassium salt)
Losartan potassium (DuP-753 potassium) 作为血管紧张素II受体1型(AT1)拮抗剂,竞争性抑制血管紧张素II与AT1的结合,IC50为20 nM。
There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
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描述 | The numerous effects of Angiotensin II (AII), including its roles in vasoconstriction, secretion of aldosterone and vasopressin, cellular proliferation, and hypertrophy are dominantly mediated through the activation of the angiotensin type 1 (AT1) receptor, a member of the superfamily of G protein-coupled receptors [5]. Losartan Potassium is an AII receptor antagonist that competitively binds the AT1 receptor with IC50 of 20 nM [6]. Male cynomolgus monkeys were given losartan (180 mg/d, n=6) or vehicle (n=8) for 6 weeks. Losartan caused significant (P<0.05) increases in plasma AII and angiotensin-(1-7). Compared with vehicle-treated controls, losartan reduced the extent of fatty streak in the aorta, the coronary arteries, and the carotid arteries by approximately 50% (P<0.05). A significant (P<0.05) reduction in the susceptibility of low-density lipoprotein (LDL) to in vitro oxidation, serum levels of monocyte chemoattractant protein-1, and circulating monocyte CD11b expression were also associated with losartan treatment [7]. |
Dose | Mice[3]: 0.1 mg/kg - 5 mg/kg (i.p.); 3 mg/kg, 30 mg/kg (p.o.) Rat[4]: 10 mg/kg (p.o.) | ||||||||||||||
Administration | i.p., p.o. | ||||||||||||||
Pharmacokinetics |
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NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT00763893 | Marfan Syndrome | Phase 3 | Terminated(A similar publicati... 展开 >>on has been released, suggesting a beneficial effect of sartans, and only 15 patients remained to be seen for their visit at 36 months.) 收起 << | - | France ... 展开 >> Hôpital Bichat Paris, France, 75018 收起 << |
NCT01224860 | Renal Transplant | Phase 2 | Completed | - | Italy ... 展开 >> Mario negri Institute - Clinical Research Center for Rare Diseases Ranica, Bergamo, Italy, 24020 收起 << |
NCT01620788 | Hypertension | Phase 3 | Not yet recruiting | March 2019 | - |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.17mL 0.43mL 0.22mL |
10.85mL 2.17mL 1.08mL |
21.69mL 4.34mL 2.17mL |
CAS号 | 124750-99-8 |
分子式 | C22H22ClKN6O |
分子量 | 461.001 |
别名 | DuP-753 potassium;Losartan (potassium salt);MK 954;DuP 753 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,Room Temperature |
溶解度 |
DMSO: 105 mg/mL(227.77 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO H2O: 50 mg/mL(108.46 mM),配合低频超声助溶 |
动物实验配方 |