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氯沙坦 /Losartan {[allProObj[0].p_purity_real_show]}

货号:A254713 同义名: 洛沙坦 / DuP-753

Losartan是一种血管紧张素 II 受体拮抗剂,以 IC50 为 20 nM 竞争性抑制血管紧张素 II 与 AT1 受体结合。

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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+
Losartan 化学结构 CAS号:114798-26-4
Losartan 化学结构
CAS号:114798-26-4
Losartan 3D分子结构
CAS号:114798-26-4
Losartan 化学结构 CAS号:114798-26-4
Losartan 3D分子结构 CAS号:114798-26-4
规格 价格 会员价 库存 数量
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Losartan 纯度/质量文件 产品仅供科研

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Losartan 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].

Losartan 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 - -

Losartan 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.

Losartan 实验方案

计算器
存储液制备 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

Losartan 技术信息

CAS号114798-26-4
分子式C22H23ClN6O
分子量 422.911
别名 洛沙坦 ;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,2-8°C

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

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