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.
Biological Activity
Description
In Vitro
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. Further protocols information, click here.
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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.
In Vivo
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.
Protocols
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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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
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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