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Cat. No.: HY-188066

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S23515

S23515 is a highly selective I₁ imidazoline receptor (I₁R) agonist with a K_i 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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CAS No.: 359715-57-4
Formule: C₁₀H₁₁BrN₂O₂
Masse moléculaire:271.11

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

S23515 Chemical Structure

CAS No.: 359715-57-4

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- In Vitro
- In Vivo
Chemical Information
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Activité biologique

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.

Real Time qPCR^[1]

Cell Line:

differentiated human THP-1 macrophages
Concentration:

100 μM
Incubation Time:

24 h
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

S23515 (3-300 μg/kg; i.c.; single injection; sequential injection) induces a dose-dependent hypotension and bradycardia in anaesthetized normotensive rabbits, with a maximal 27% reduction in MAP, and interacts synergistically with α-methylnorepinephrine^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Zika strain (male, 2.5 to 3.5 kg, anaesthetized)^[2]
Dosage:

3 μg/kg; 10 μg/kg; 30 μg/kg; 100 μg/kg; 300 μg/kg
Administration:

i.c.; single injection; sequential injection (3 μg/kg followed by 0.5 mg/kg α-methylnorepinephrine after 10 minutes)
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.

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Chemical Information

CAS No. 359715-57-4
Masse moléculaire 271.11
Formule C₁₀H₁₁BrN₂O₂
SMILES

BrC1=C(OCC2OC(N)=NC2)C=CC=C1
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Venteclef N, et al. The imidazoline-like drug S23515 affects lipid metabolism in hepatocyte by inhibiting the oxidosqualene: lanosterol cyclase activity. Biochemical pharmacology. 2005 Apr 01;69(7):1041-8.

[2]. Bruban V, et al. Respective contributions of alpha-adrenergic and non-adrenergic mechanisms in the hypotensive effect of imidazoline-like drugs. British journal of pharmacology. 2001 May;133(2):261-6.

[3]. Bousquet P, et al. I(1) imidazoline receptors involved in cardiovascular regulation: where are we and where are we going? Ann N Y Acad Sci. 2003 Dec;1009:228-33.
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How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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