Losartan Carboxaldehyde
(Synonyms: 氯沙坦甲醛,DuP-167|EXP3179) 目录号 : GC14013
A losartan metabolite with anti-inflammatory actions
Cas No.:114798-36-6
Sample solution is provided at 25 µL, 10mM.
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Losartan is an inhibitor of endothelial cyclooxygenase (COX)-2.
COX-2 produces prostaglandins that inhibit apoptosis and stimulate angiogenesis and invasiveness, and thus selective COX-2 inhibitors can reduce prostaglandin synthesis and restore apoptosis.
In vitro: Losartan is an intermediate aldehyde metabolite of losartan, the angiotensin II type 1 receptor antagonist. Losartan could not block angiotensin receptors, but inhibit the expression of endothelial cyclooxygenase (COX)-2, therefore exerting anti-inflammatory actions. Moreover, losartan at 1 μM was able to block the upregulation of ICAM-1 mRNA and COX-dependent generation of thromboxane A2 and prostaglandin F2α [1].
In vivo: In animal stufdy, losartan was infused for 10 days to rats on a normal sodium intake (NNa) and rats on a high sodium intake (HNa) to suppress endogenous Ang II. Although basal plasma renin activity was markedly suppressed in HNa rats compared with NNa rats, control arterial pressure was not different between NNa and HNa rats. Losartan could decrease arterial pressure from control levels in NNa rats on the first day of infusion but had no effect on arterial pressure in HNa rats. In addition, by day 10 of losartan infusion, arterial pressure had decreased further from control levels in NNa rats but remained unchanged compared with control in HNa rats [2].
Clinical trial: In patients with mild to moderate hypertension, losartan as monotherapy could lower blood pressure to a similar degree to enalapril, atenolol and felodipine. Losartan combined with hydrochlorothiazide could reduce blood pressure than either drug separately given. About 1/3 patients with severe hypertension have response to the combination product [3].
References:
[1] C. Kr mer, J. Sunkomat, J. Witte, et al. Angiotensin II receptor-independent antiinflammatory and antiaggregatory properties of losartan: Role of the active metabolite EXP3179. Circulation Research 90(7), 770-776 (2002).
[2] Collister JP, Hornfeldt BJ, Osborn JW. Hypotensive response to losartan in normal rats. Role of Ang II and the area postrema. Hypertension. 1996 Mar;27(3 Pt 2):598-606.
[3] Goa KL, Wagstaff AJ. Losartan potassium: a review of its pharmacology, clinical efficacy and tolerability in the management of hypertension. Drugs. 1996 May;51(5):820-45.
| Cas No. | 114798-36-6 | SDF | |
| 别名 | 氯沙坦甲醛,DuP-167|EXP3179 | ||
| 化学名 | 2-butyl-4-chloro-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1H-imidazole-5-carboxaldehyde | ||
| Canonical SMILES | [H]N1N=NN=C1C2=CC=CC=C2C3=CC=C(CN4C(C([H])=O)=C(Cl)N=C4CCCC)C=C3 | ||
| 分子式 | C22H21ClN6O | 分子量 | 420.9 |
| 溶解度 | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 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。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3759 mL | 11.8793 mL | 23.7586 mL |
| 5 mM | 0.4752 mL | 2.3759 mL | 4.7517 mL |
| 10 mM | 0.2376 mL | 1.1879 mL | 2.3759 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet