产品说明书

Losartan

Print
Chemical Structure| 114798-26-4 同义名 : 洛沙坦 ;DuP-753
CAS号 : 114798-26-4
货号 : A254713
分子式 : C22H23ClN6O
纯度 : 98%
分子量 : 422.911
MDL号 : MFCD00865831
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(248.28 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
动物实验配方：
生物活性
靶点

  • AT1 receptor

    AT1 receptor, IC50:20 nM
描述 Losartan, a small-molecule angiotensin II type 1 receptor antagonist used to treat hypertension[3]. The concentration that inhibits 50% of the binding of angiotensin II (IC50) is 20 nM[4]. In vitro, losartan effectively limited the fibrotic potential of RDEB fibroblasts, as measured by cell contractility[3]. In vivo, Losartan was filtered to a final concentration of 0.6 g/L, providing an estimated daily dose of 40-60 mg/kg/day. Losartan treatment prevented significant retinal ganglion cell loss and significantly lowered blood pressure. Losartan inhibited effects of glaucoma[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00447603 Hypertension Phase 3 Terminated(Achieving site read... 展开 >>iness and enrolling the trial within a reasonable time) 收起 << - -
NCT01198249 Essential Hypertension Phase 1 Completed - Korea, Republic of ... 展开 >> Severance Hospital Seoul, Korea, Republic of, 120-752 收起 <<
NCT02183701 Hypertension Phase 3 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.36mL

0.47mL

0.24mL

11.82mL

2.36mL

1.18mL

23.65mL

4.73mL

2.36mL
参考文献

[1]Burnier M. Angiotensin II type 1 receptor blockers. Circulation. 2001 Feb 13;103(6):904-12.

[2]Strawn WB, Chappell MC, et al. Inhibition of early atherogenesis by losartan in monkeys with diet-induced hypercholesterolemia. Circulation. 2000 Apr 4;101(13):1586-93.

[3]Nyström A, Thriene K, Mittapalli V, Kern JS, Kiritsi D, Dengjel J, Bruckner-Tuderman L. Losartan ameliorates dystrophic epidermolysis bullosa and uncovers new disease mechanisms. EMBO Mol Med. 2015 Sep;7(9):1211-28. doi: 10.15252/emmm.201505061. PMID: 26194911; PMCID: PMC4568953.

[4]Burnier M. Angiotensin II type 1 receptor blockers. Circulation. 2001 Feb 13;103(6):904-12. doi: 10.1161/01.cir.103.6.904. PMID: 11171802.

[5]Quigley HA, Pitha IF, Welsbie DS, Nguyen C, Steinhart MR, Nguyen TD, Pease ME, Oglesby EN, Berlinicke CA, Mitchell KL, Kim J, Jefferys JJ, Kimball EC. Losartan Treatment Protects Retinal Ganglion Cells and Alters Scleral Remodeling in Experimental Glaucoma. PLoS One. 2015 Oct 27;10(10):e0141137. doi: 10.1371/journal.pone.0141137. PMID: 26505191; PMCID: PMC4624713.