Art. -Nr.: HY-149120

ASM-IN-1

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ASM-IN-1 is a potent and orally active acid sphingomyelinase (ASM) inhibitor with an IC₅₀ value of 1.5 µM. ASM-IN-1 reduces lipid plaques in the aortic arch and aorta and reduces plasma ceramide concentration and Ox-LDL levels. ASM-IN-1 shows antiatherosclerotic and anti-inflammatory activity.

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Reinheit: 98.65%
CAS. Nr.: 2913151-46-7
Formel: C₁₆H₁₂BrN₃O₄
Molecular Weight:390.19

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

ASM-IN-1 Chemical Structure

CAS. Nr.: 2913151-46-7

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Phospholipase Isoform-spezifische Produkte anzeigen :

In Vitro

ASM-IN-1 (compound 4i) (0-20 µM) dose not affect cell growth in HUVECs^[1].
ASM-IN-1 (0, 1, 5 µM) reduces the expressions of IL-6 and TNF-α with LPS stimulated in a dose-dependent manner, decreases the expression of MCP-1 mRNA in HUVECs^[1].
ASM-IN-1 (5 µM) reduces Ox-LDL-stimulated MCP-1 mRNA expression and restore IL-6 mRNA to a normal level^[1].

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

Cell Cytotoxicity Assay^[1]

Cell Line:

HUVECs
Concentration:

0.5, 1, 5, 10, 20 µM
Incubation Time:

24, 48 h
Result:

Showed no affect on cell growth.

In Vivo

ASM-IN-1 (1 mg/kg for i.v.; 10 mg/kg for p.o.) shows good pharmacokinetic properties with good oral bioavailability of 35.42% in ICR mice^[1].
ASM-IN-1 (6, 12, 40 mg/kg; i.p.; twice a day for 8 weeks) antiatherosclerotic activity by inhibiting ASM in mice^[1].
Pharmacokinetic Parameters of ASM-IN-1 in ICR mice^[1].

parameter	iv	po
T_1/2 (h)	0.20 ± 0.04	0.83 ± 0.32
T_max (h)	0.083 ± 0.00	0.083 ± 0.00
C_max (ng/mL)	787 ± 64.7	2763 ± 485
AUC_0-t (h·ng/mL)	227 ± 14.3	805 ± 76.7
AUC_0-∞ (h·ng/mL)	228 ± 15.1	809 ± 75.1
V_z (mL/kg)	1277 ± 216
CL (mL/h/kg)	4390 ± 291
MRT_0-t (h)	0.077 ± 0.012	0.32 ± 0.078
MRT_0-∞ (h)	0.087 ± 0.019	0.35 ± 0.064
F (%)		35.42 ± 0.033%

ICR mice, 1 mg/kg iv ; 10 mg/kg po^[1]

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

Chemical Information

CAS. Nr. 2913151-46-7
Appearance Solid
Molecular Weight 390.19
Formel C₁₆H₁₂BrN₃O₄
Color White to off-white
SMILES

BrC1=CC=C(OCC2=CC=C(C3=NOC(C(NO)=O)=N3)C=C2)C=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 60 mg/mL (153.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5629 mL

12.8143 mL

25.6285 mL

5 mM

0.5126 mL

2.5629 mL

5.1257 mL

10 mM

0.2563 mL

1.2814 mL

2.5629 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 3 mg/mL (7.69 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Yang K, et al. Discovery of Novel N-Hydroxy-1,2,4-oxadiazole-5-formamides as ASM Direct Inhibitors for the Treatment of Atherosclerosis. J Med Chem. 2023 Feb 23;66(4):2681-2698. [Content Brief]

Help & FAQs

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5629 mL	12.8143 mL	25.6285 mL	64.0713 mL
	5 mM	0.5126 mL	2.5629 mL	5.1257 mL	12.8143 mL
	10 mM	0.2563 mL	1.2814 mL	2.5629 mL	6.4071 mL
	15 mM	0.1709 mL	0.8543 mL	1.7086 mL	4.2714 mL
	20 mM	0.1281 mL	0.6407 mL	1.2814 mL	3.2036 mL
	25 mM	0.1025 mL	0.5126 mL	1.0251 mL	2.5629 mL
	30 mM	0.0854 mL	0.4271 mL	0.8543 mL	2.1357 mL
	40 mM	0.0641 mL	0.3204 mL	0.6407 mL	1.6018 mL
	50 mM	0.0513 mL	0.2563 mL	0.5126 mL	1.2814 mL
	60 mM	0.0427 mL	0.2136 mL	0.4271 mL	1.0679 mL
	80 mM	0.0320 mL	0.1602 mL	0.3204 mL	0.8009 mL
	100 mM	0.0256 mL	0.1281 mL	0.2563 mL	0.6407 mL

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ASM-IN-1

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cardiovascular Disease Compound Library

Orally Active Compound Library

Lipid Metabolism Compound Library

Metabolic Enzyme Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle Phospholipase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ASM-IN-1

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cardiovascular Disease Compound Library

Orally Active Compound Library

Lipid Metabolism Compound Library

Metabolic Enzyme Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle Phospholipase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ASM-IN-1 Related Classifications

HY-149120 Related Classifications