LNP-911
LNP-911 is a ligand for the I1 imidazoline receptor. LNP-911 allosterically modulates I1Rs and enhances the effect of agonists on Forskolin (HY-15371)-stimulated cAMP accumulation. LNP-911 exists mainly as a stable imine tautomer. After radioiodination, LNP-911 serves as a selective high-affinity radioligand for characterization studies of I1Rs in membrane preparations. LNP-911 can be used in hypertension-related research.
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- CAS 番号: 497180-72-0
- 分子式: C11H12ClIN2
- 分子量:334.58
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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
生物活性
製品説明
体外実験
LNP-911 (10-10-10-3 M; 60 min) exhibits low affinity for human α2A, α2B and α2C adrenergic receptors expressed on CHO cell membranes, with Ki values ranging from 1750 nM to ≥10,000 nM; it shows low affinity for I2 binding sites in rabbit kidney cell membranes (Ki = 25,428 nM)[1].
LNP-911 (10-10-10-3 M; 30 min) binds to I1 imidazoline receptors on PC-12 cell membranes, with a high-affinity Ki value of 0.2 nM (accounting for 38% of binding sites) and a low-affinity Ki value of 10000 nM[1].
[125I]-labeled LNP-911 (0.05-6.6 nM; 60 min) binds to a single high-affinity site on PC-12 cell membranes, with a Kd value of 1.4 nM and a Bmax value of 398 fmol/mg protein[1].
LNP‑911 acts as an allosteric potentiator in PC‑12 cells, dose‑dependently enhancing the inhibitory effect of I1 receptor agonists on forskolin‑stimulated cAMP production and exerting no independent influence on cAMP levels[1].
LNP-911 binds with high affinity to I1-imidazoline receptors on PC12 cell membranes, with Ki values of 1.4 nM (using [125I]LNP 911 as the radioligand)[2].
LNP-911 exists mainly as a stable non-planar imine tautomer (IIB) in both gas and aqueous phases[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
化学情報
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CAS 番号 497180-72-0
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分子量 334.58
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分子式 C11H12ClIN2
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SMILES
CC1CCC(NC2=CC=C(I)C=C2Cl)=N1
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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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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
[1]. Greney H, et al. [125I]2-(2-chloro-4-iodo-phenylamino)-5-methyl-pyrroline (LNP 911), a high-affinity radioligand selective for I1 imidazoline receptors. Molecular pharmacology. 2002 Jul;62(1):181-91. [Content Brief]
[3]. Remko M, et al. Theoretical study of structure, pKa, lipophilicity, solubility, absorption, and polar surface area of some centrally acting antihypertensives. Bioorganic & medicinal chemistry. 2006 Mar 15;14(6):1715-28. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
LNP-911 関連分類
HY-188067 関連分類
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