2. Metabolic Enzyme/Protease
  3. Phospholipase
  4. ASM-IN-1

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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ASM-IN-1 Chemical Structure

ASM-IN-1 Chemical Structure

CAS No. : 2913151-46-7

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5 mg USD 240 In-stock
10 mg USD 435 In-stock
25 mg USD 890 In-stock
50 mg USD 1560 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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[1].

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.

ASM-IN-1 Related Antibodies

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
T1/2 (h) 0.20 ± 0.04 0.83 ± 0.32
Tmax (h) 0.083 ± 0.00 0.083 ± 0.00
Cmax (ng/mL) 787 ± 64.7 2763 ± 485
AUC0-t (h·ng/mL) 227 ± 14.3 805 ± 76.7
AUC0-∞ (h·ng/mL) 228 ± 15.1 809 ± 75.1
Vz (mL/kg) 1277 ± 216
CL (mL/h/kg) 4390 ± 291
MRT0-t (h) 0.077 ± 0.012 0.32 ± 0.078
MRT0-∞ (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.
Molecular Weight

390.19

Formula

C16H12BrN3O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5629 mL 12.8143 mL 25.6285 mL
5 mM 0.5126 mL 2.5629 mL 5.1257 mL
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

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

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:

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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% 
+
%
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%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ASM-IN-12913151-46-7Phospholipaseorally activeantiatheroscleroticanti-inflammatoryIL-6TNF-αMCP-1HUVECsInhibitorinhibitorinhibit

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