MDL-19744A
MDL-19744A is an orally active and selective α1-adrenergic receptor antagonist, with rat α1-adrenergic receptor IC50 of 8 nM. MDL-19744A increases renal blood flow, dose-related decreases mean arterial blood pressure, increases urinary sodium excretion, and mediates renal vasodilation. MDL-19744A can be used for the research of hypertension.
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- CAS 番号: 97233-26-6
- 分子式: C21H25NO3S
- 分子量:371.49
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- 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
Adrenergic 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
IC50 & Target
[1]|
α1-adrenergic receptor |
体外実験
MDL-19744A (Compound 1) potently and selectively inhibits α1-adrenergic receptor binding in rat cerebrocortex tissue, with an IC50 of 8 nM for α1 receptors[1].
MDL-19744A (30 min) potently antagonizes α1-adrenergic receptor-mediated vasoconstriction in isolated rabbit aortic strips, with a pA2 of 8.13[1].
MDL-19744A (3 μM) is inactive as a β-adrenergic receptor blocker in isolated guinea pig ventricles[1].
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
MDL-19744A (0.03-3 mg/kg; i.v.; single dose) produces decreases in mean arterial blood pressure in anesthetized normotensive dogs, with an ED15 for hypotension of 0.08 mg/kg and a maximal mean arterial blood pressure reduction of -47 mmHg at 1 mg/kg i.v[1].
MDL-19744A (0.01-1 mg/kg; i.v.; cumulative dose) produces dose-dependent increases in renal blood flow and increases in urinary sodium excretion in anesthetized normotensive dogs[1].
MDL-19744A (0.1-3 mg/kg; i.v.; single dose) selectively antagonizes α1-adrenergic receptors in pithed rats, shifting Phenylephrine (HY-B0769)-induced pressor responses at 0.1-1.0 mg/kg i.v. while only weakly affecting α2-mediated responses at 3.0 mg/kg i.v[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:spontaneously hypertensive rats (SHR) (conscious)[1]
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Dosage:30 mg/kg
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Administration:p.o.; single dose
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Result:Produced a maximal decrease in mean arterial blood pressure of -70 mmHg.
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Animal Model:normotensive dogs (anesthetized)[1]
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Dosage:0.01 mg/kg; 0.03 mg/kg; 0.1 mg/kg; 0.3 mg/kg; 1.0 mg/kg
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Administration:i.v.; cumulative dose
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Result:Produced a 9% increase in renal blood flow and a -5% change in mean arterial blood pressure at 0.01 mg/kg cumulative dose.
Produced a 17% increase in renal blood flow and a -9% change in mean arterial blood pressure at 0.03 mg/kg cumulative dose.
Produced a 27% increase in renal blood flow and a -15% change in mean arterial blood pressure at 0.1 mg/kg cumulative dose.
Produced a 34% increase in renal blood flow, a -23% change in mean arterial blood pressure, and increased urinary sodium excretion from a baseline of 42 to 104 µequiv/min at 0.3 mg/kg cumulative dose.
Produced a 42% increase in renal blood flow and a -32% change in mean arterial blood pressure at 1.0 mg/kg cumulative dose.
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Animal Model:rats[1]
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Dosage:0.1 mg/kg; 0.3 mg/kg; 1.0 mg/kg; 3 mg/kg
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Administration:i.v.; single dose
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Result:Shifted the Phenylephrine-induced diastolic blood pressure dose-response curve (DR2 = 0.07, 0.02 mg/kg) at doses of 0.1-1.0 mg/kg.
Weakly affected α2-mediated responses at 3.0 mg/kg i.v.
化学情報
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CAS 番号 97233-26-6
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分子量 371.49
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分子式 C21H25NO3S
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SMILES
O=C1C2=C(SC(C)=C2)CC[C@H]1CN[C@@H]3[C@@H]([C@H](CC3)OC4=CC=CC=C4)O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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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.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
MDL-19744A 関連分類
HY-183954 関連分類
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