EXP3179
Based on 1 Customer Validation
EXP3179 (Losartan Carboxaldehyde) is a metabolite of Losartan (HY-17512). EXP3179 binds to AT1R with an affinity of 20 nM and blocks ANGII-induced AT1R signaling, inhibiting ERK1/2 activation. EXP3179 reduces NADPH oxidase activity. EXP3179 inhibits Phenylephrine (HY-B0769)-induced aortic contraction through an endothelium-dependent, NO-dependent mechanism. EXP3179 dose-dependently inhibits type I collagen-induced platelet aggregation and activation through GPVI binding, reducing platelet adhesion to the injured site. EXP3179 lowers blood pressure in normotensive and spontaneously hypertensive rats and mice. EXP3179 can be used for research on type 2 diabetes, hypertensive heart disease, hypertension, thrombosis, and coronary artery disease.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 98.09%
- CAS 番号: 114798-36-6
- 分子式: C22H21ClN6O
- 分子量:420.89
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
Angiotensin Receptor アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
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AT1 Receptor |
ERK1 |
ERK2 |
体外実験
EXP3179, as a metabolite of Losartan (HY-17512), reduces NADPH oxidase activity in circulating leukocytes[2].
EXP3179 (25 μM) blocks ANGII-AT1R signaling in HEK-AT1R cells[3].
EXP3179 (25 μM) completely blocks ANGII-induced ERK1/2 phosphorylation in primary rASMCs at 25 μM[3].
EXP3179 (500 μM) dose-dependently inhibits type I collagen-induced platelet aggregation and activation, with a significant effect at 500 μM[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
体内実験
EXP3179 (10 mg/kg; intravenous injection) significantly reduces systolic and diastolic blood pressure in spontaneously hypertensive rats within 30 min[3].
EXP3179 significantly reduces platelet adhesion at the site of vascular injury in a mouse carotid artery injury model[4].
EXP3179 (subcutaneous injection) does not mediate the antitumor effect of Losartan in orthotopic PDAC tumor-bearing mice; instead, the antitumor activity is mediated by EXP3174[7].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Spontaneously hypertensive (male, 10 months old)[3]
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Dosage:10 mg/kg
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Administration:i.v. (single injection)
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Result:Caused a profound decrease in SBP and DBP by 103 and 64 mmHg, respectively, within 30 min after injection.
化学情報
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CAS 番号 114798-36-6
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性状 Solid
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分子量 420.89
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分子式 C22H21ClN6O
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Color White to off-white
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SMILES
[H]N1N=NN=C1C2=CC=CC=C2C3=CC=C(C=C3)CN4C(C([H])=O)=C(N=C4CCCC)Cl
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別名
Losartan Carboxaldehyde; DuP 167
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
DMSO : 125 mg/mL (296.99 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.94 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
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Research Protocol for Cardiovascular Diseases
Cardiovascular disease can be modeled as maladaptive cardiac remodeling, where ischemic injury or pressure overload activates inflammatory signaling, fibroblast activation, extracellular-matrix deposition, cardiomyocyte hypertrophy, vascular remodeling, and progressive ventricular dysfunction. The TGF-β/SMAD axis is a central profibrotic pathway after myocardial injury and pressure overload, while innate immune and cytokine pathways regulate leukocyte recruitment, scar formation, and adverse remodeling. Key unresolved questions include which inflammatory signals are reparative versus harmful, when fibrosis is protective versus maladaptive, and whether pathway inhibition improves function without weakening necessary infarct healing or compensatory remodeling.
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Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
純度とドキュメンテーション
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3759 mL | 11.8796 mL | 23.7592 mL | 59.3979 mL |
| 5 mM | 0.4752 mL | 2.3759 mL | 4.7518 mL | 11.8796 mL | |
| 10 mM | 0.2376 mL | 1.1880 mL | 2.3759 mL | 5.9398 mL | |
| 15 mM | 0.1584 mL | 0.7920 mL | 1.5839 mL | 3.9599 mL | |
| 20 mM | 0.1188 mL | 0.5940 mL | 1.1880 mL | 2.9699 mL | |
| 25 mM | 0.0950 mL | 0.4752 mL | 0.9504 mL | 2.3759 mL | |
| 30 mM | 0.0792 mL | 0.3960 mL | 0.7920 mL | 1.9799 mL | |
| 40 mM | 0.0594 mL | 0.2970 mL | 0.5940 mL | 1.4849 mL | |
| 50 mM | 0.0475 mL | 0.2376 mL | 0.4752 mL | 1.1880 mL | |
| 60 mM | 0.0396 mL | 0.1980 mL | 0.3960 mL | 0.9900 mL | |
| 80 mM | 0.0297 mL | 0.1485 mL | 0.2970 mL | 0.7425 mL | |
| 100 mM | 0.0238 mL | 0.1188 mL | 0.2376 mL | 0.5940 mL |
EXP3179 関連分類
HY-114950 関連分類
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Keywords
- EXP3179
- 114798-36-6
- Losartan Carboxaldehyde
- DuP 167
- EXP 3179
- EXP-3179
- DuP167
- DuP 167
- DuP-167
- Drug Metabolite
- Angiotensin Receptor
- ERK
- NADPH Oxidase
- NO Synthase
- Glycoprotein VI
- NADPH oxidase
- primary rASMC
- AT1R antagonist
- GPVI antagonist
- ANGII-induced ERK1/2 phosphorylation
- collagen type I-induced human platelet aggregation
- 3T3-L1 adipocyte differentiation
- HEK-AT1R cells
- PPARγ modulator
- losartan metabolite
- Inhibitor
- inhibitor
- inhibit