GLPBio

Losartan

Catalog No.: GC10249Purity:>98.50%
COASDSData Sheet
Losartan은 20nM의 IC50으로 AT1 수용체에 대한 안지오텐신 II의 결합과 경쟁하는 안지오텐신 II 수용체 길항제입니다.

제품은 연구용으로만 사용됩니다. 인체에 사용할 수 없으며 환자에게 판매하지 않습니다.

Losartan
Cas No.: 114798-26-4
10mM (in 1mL DMSO)In Stock
$35.00
1
500mgIn Stock
$28.00
1
1gIn Stock
$35.00
1
5gIn Stock
$84.00
1
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제품 설명 (Description)

Losartan is an angiotensin II receptor antagonist (IC50=20nM). Losartan works by selectively blocking the AT1 receptor of angiotensin II. Losartan can be used for the treatment of hypertension and diabetic nephropathy[1-4].

In vitro, pretreatment of Vero E6 cells with Losartan (1–100μM) for 1 hour, followed by infection with SARS-CoV-2 (MOI=0.01) and culture for 96 hours, Losartan significantly reduced viral nucleoprotein levels and inhibited viral replication[5]. Pretreatment of MV3 cells with Losartan (0.7μM) for 30 minutes, followed by treatment with ATII (100nM), Losartan significantly inhibited NHE1 activity in the cells[6].

In vivo, Losartan (5-50mg/kg; oral administration) was administered to Swiss mice with 5-FU-induced intestinal mucositis for 4 days. Losartan significantly prevented the 5-FU-induced intestinal mucositis effects[7]. Losartan (10mg/kg) was orally administered daily via drinking water to CD2F1 mice bearing C26 cells for 19 days. Losartan prevented tumor-induced muscle mass loss, reduced tumor weight, attenuated myocardial interleukin-6 expression, improved cardiomyocyte calcium signaling, and increased cardiomyocyte contraction speed, contractile function, and blood pressure in tumor-bearing mice[8].

References:
[1] Sica DA, Gehr TW, Ghosh S. Clinical pharmacokinetics of losartan. Clin Pharmacokinet. 2005;44(8):797-814.
[2] Burnier M. Angiotensin II type 1 receptor blockers. Circulation. 2001 Feb 13;103(6):904-12.
[3] Ashry O, Schnecko A, Clauss WG, et al. Evidence for expression and function of angiotensin II receptor type 1 in pulmonary epithelial cells. Respir Physiol Neurobiol. 2014 May 1;195:37-40.
[4] Saleh N, Cosarderelioglu C, Vajapey R, et al. Losartan Mitigates Oxidative Stress in the Brains of Aged and Inflamed IL-10-/- Mice. J Gerontol A Biol Sci Med Sci. 2022 Sep 1;77(9):1784-1788.
[5] Nejat R, Sadr AS, Freitas B, et al. Losartan Inhibits SARS-CoV-2 Replication in Vitro. J Pharm Pharm Sci. 2021;24:390-399.
[6] Olschewski DN, Hofschröer V, Nielsen N, et al. The Angiotensin II Type 1 Receptor Antagonist Losartan Affects NHE1-Dependent Melanoma Cell Behavior. Cell Physiol Biochem. 2018;45(6):2560-2576.
[7] Oliveira MMB, de Araújo AA, Ribeiro SB, et al. Losartan improves intestinal mucositis induced by 5-fluorouracil in mice. Sci Rep. 2021 Dec 1;11(1):23241.
[8] Stevens SC, Velten M, Youtz DJ, et al. Losartan treatment attenuates tumor-induced myocardial dysfunction. J Mol Cell Cardiol. 2015 Aug;85:37-47.

실험 프로토콜 (Protocol)

Cell experiment [1]:

Cell lines

Vero E6 cells (African green monkey kidney cell line)

Preparation Method

Vero E6 cells were plated at 2 x 10⁴ cells/well in a 96-well plate and incubated overnight at 37°C. Losartan was prepared in DMEM to concentrations from 1μM to 100μM. For pre-infection treatment, cells were preincubated with Losartan for 1 hour, then infected with SARS-CoV-2 at a MOI=0.01 for 1 hour. After infection, fresh Losartan-containing media was added. For post-infection treatment, cells were first infected with SARS-CoV-2 at a MOI=0.01 for 1 hour, then Losartan-containing media was added. Cells were incubated for 96 hours at 37°C, 5% CO₂.

Reaction Conditions

1-100μM; pre-incubation 1 hour, incubation 96 hours.

Applications

Losartan treatment showed a dose-dependent and significant reduction in SARS-CoV-2 replication. Pre-infection treatment reduced SARS-CoV-2 nuclear protein levels, and post-infection treatment decreased viral replication. The half-maximal effective concentration (EC₅₀) of Losartan was 13.7μM for pre-infection treatment and 41μM for post-infection treatment.

Animal experiment [2]:

Animal models

Swiss mice (Mus musculus)

Preparation Method

Intestinal mucositis was induced by a single intraperitoneal administration of 5-fluorouracil (5-FU; 450mg/kg). Losartan or saline was orally administered 30min before 5-FU injection and daily for 4 days. On the 4th day, animals were euthanized and segments of small intestine were collected for analysis.

Dosage form

5, 25 or 50mg/kg; oral administration; daily for 4 days.

Applications

Losartan prevented 5-FU-induced intestinal mucositis effects including histopathological damage (shortened villi, loss of crypt architecture, inflammatory cell infiltration), partially rescued body weight loss, prevented leukopenia, decreased pro-inflammatory cytokine levels (TNF-α and IL-1β), reduced oxidative stress markers (MDA and GSH), and modulated mRNA expression of NF-κB p65, TWEAK and Fn14.

References:
[1] Nejat R, Sadr AS, Freitas B, et al. Losartan Inhibits SARS-CoV-2 Replication in Vitro. J Pharm Pharm Sci. 2021;24:390-399.
[2] Oliveira MMB, de Araújo AA, Ribeiro SB, et al. Losartan improves intestinal mucositis induced by 5-fluorouracil in mice. Sci Rep. 2021 Dec 1;11(1):23241.

제품 문서 (Product Documents)

Purity:>98.50%Appearance:A solid
COASDSData Sheet

화학적 특성 (Chemical Properties)

CAS 번호
114798-26-4
화학명
[2-butyl-5-chloro-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazol-4-yl]methanol
SMILES
CCCCC1=NC(=C(N1CC2=CC=C(C=C2)C3=CC=CC=C3C4=NNN=N4)CO)Cl
분자식
C22H23ClN6O
분자량
422.91
용해도
≥ 84.6mg/mL in DMSO
보관
Store at -20°C
일반 주의사항
제품의 용해도 데이터에 따라 적절한 용매를 선택하십시오. 조제 후에는 반복적인 동결·해동을 피할 수 있도록 저장 용액을 소분하십시오.
저장 용액은 -80°C 보관 시 6개월 이내, -20°C 보관 시 1개월 이내에 사용하십시오.
용해도를 높이려면 튜브를 37°C로 데운 뒤 적절한 시간 동안 초음파 처리하십시오.
배송 조건
평가용 샘플은 아이스팩과 함께 배송됩니다. 그 외 용량은 실온 배송되며, 요청 시 아이스팩과 함께 배송할 수 있습니다.

계산 도구 (Calculators)몰 농도 / 희석 / 분자량 / 단위 변환 / 생체 내 제형 / 용해도

g/mol

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