S23515
S23515 is a highly selective I1 imidazoline receptor (I1R) agonist with a Ki value of 6.4 nM. S23515 modulates central cardiovascular functions, induces hypotension and bradycardia, shows no affinity for α-adrenergic receptors, and cannot cross the blood-brain barrier. S23515 inhibits oxidosqualene-lanosterol cyclase (OSC) and cholesterol synthesis, induces the production of (24S,25)-Epoxycholesterol (HY-W040150), and upregulates the expression of ABCA1 and ABCG1 in human macrophages. S23515 is applicable to research related to dyslipidemia and hypertension.
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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。
- CAS 番号: 359715-57-4
- 分子式: C10H11BrN2O2
- 分子量:271.11
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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
生物活性
製品説明
体外実験
S23515 (25 μM; 2 h) specifically inhibits the synthesis of cholesterol and cholesteryl esters (but not triglyceride synthesis) in primary rat hepatocytes[1].
S23515 (5-100 μM; 2 h) inhibits oxidosqualene:lanosterol cyclase activity in primary rat hepatocytes, with an IC50 of 8 μM for inhibiting intracellular cholesterol synthesis and an IC50 of 10 μM for inhibiting secreted cholesterol[1].
S23515 (1-100 μM; 6 h) stimulates (24S,25)-Epoxycholesterol synthesis in primary rat hepatocytes in a biphasic manner, with the production peaking at 12-25 μM after 6 h of treatment[1].
S23515 (100 μM; 24 h) inhibits the activity of oxidosqualene:lanosterol cyclase and promotes (24S,25)-Epoxycholesterol in differentiated human THP-1 macrophages[1].
S23515 (100 μM; 24 h) upregulates the mRNA expression of ABCA1, ABCG1 and LDLr in differentiated human THP-1 macrophages[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:differentiated human THP-1 macrophages
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Concentration:100 μM
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Incubation Time:24 h
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Result:Increased ABCA1 mRNA expression to 168% of control, with statistically significant change.
Increased ABCG1 mRNA expression to 330% of control, with statistically significant change.
Increased LDLr mRNA expression to 380% of control, with statistically significant change.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Zika strain (male, 2.5 to 3.5 kg, anaesthetized)[2]
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Dosage:3 μg/kg; 10 μg/kg; 30 μg/kg; 100 μg/kg; 300 μg/kg
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Administration:i.c.; single injection; sequential injection (3 μg/kg followed by 0.5 mg/kg α-methylnorepinephrine after 10 minutes)
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Result:Induced a dose-dependent decrease in mean arterial pressure (MAP) and heart rate (HR).
At 300 μg/kg, reduced MAP from 96 mmHg to 70 mmHg, and reduced HR from 290 beats/min to 243 beats/min.
Caused significant hypotension at doses ≥ 30 μg/kg and significant bradycardia at doses ≥ 10 μg/kg.
化学情報
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CAS 番号 359715-57-4
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分子量 271.11
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分子式 C10H11BrN2O2
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SMILES
BrC1=C(OCC2OC(N)=NC2)C=CC=C1
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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.
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)
S23515 関連分類
HY-188066 関連分類
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Keywords
- S23515
- 359715-57-4
- S 23515
- S-23515
- Imidazoline Receptor
- Squalene Monooxygenase
- human HepG2 hepatoma cells
- α-adrenoceptors
- I1 imidazoline receptor
- blood-brain barrier
- primary rat hepatocytes
- primary human hepatocytes
- human macrophages
- primary cynomolgus hepatocytes
- differentiated human THP-1 macrophages
- oxidosqualene:lanosterol cyclase
- Inhibitor
- inhibitor
- inhibit