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.
For research use only. We do not sell to patients.
- CAS No.: 359715-57-4
- Formula: C10H11BrN2O2
- Molecular Weight:271.11
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Storage:
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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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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.
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.
Chemical Information
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CAS No. 359715-57-4
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Molecular Weight 271.11
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Formula C10H11BrN2O2
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SMILES
BrC1=C(OCC2OC(N)=NC2)C=CC=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
S23515 Related Classifications
HY-188066 Related Classifications
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- 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