2. Metabolic Enzyme/Protease
  3. HIF/HIF Prolyl-Hydroxylase
  4. ISM012-042

ISM012-042 is an orally active PHD1 and PHD2 inhibitor with IC50 values of 1.9 and 2.5 nM, respectively. ISM012-042 (2.5 μM) can protect Caco-2 cells from DSS-induced barrier disruption. In lipopolysaccharide (LPS)-induced mouse bone marrow-derived dendritic cells (BMDC), ISM012-042 has anti-inflammatory effects and can dose-dependently reduce the expression of IL-12 subunit IL-12p35 and TNF. ISM012-042 restores intestinal barrier function and alleviates intestinal inflammation in various experimental colitis models. ISM012-042 can be used for intestinal mucosal repair and research into immune diseases.

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ISM012-042

ISM012-042 Chemical Structure

CAS No. : 2924181-80-4

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ISM012-042 Related Antibodies

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Description

ISM012-042 is an orally active PHD1 and PHD2 inhibitor with IC50 values of 1.9 and 2.5 nM, respectively. ISM012-042 (2.5 μM) can protect Caco-2 cells from DSS-induced barrier disruption. In lipopolysaccharide (LPS)-induced mouse bone marrow-derived dendritic cells (BMDC), ISM012-042 has anti-inflammatory effects and can dose-dependently reduce the expression of IL-12 subunit IL-12p35 and TNF. ISM012-042 restores intestinal barrier function and alleviates intestinal inflammation in various experimental colitis models. ISM012-042 can be used for intestinal mucosal repair and research into immune diseases[1].

Molecular Weight

489.53

Formula

C25H27N7O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C)(OC(N1CCN(C2=CC=C3C(C=NC(C(NCC4=CN=C(C#N)C=C4)=O)=C3O)=N2)CC1)=O)C
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 : 25 mg/mL (51.07 mM; ultrasonic and warming and heat to 60°C; 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 2.0428 mL 10.2139 mL 20.4278 mL
5 mM 0.4086 mL 2.0428 mL 4.0856 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.11 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (5.11 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(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:
%
DMSO +
% 
+
%
Tween-80 +
%
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 2.0428 mL 10.2139 mL 20.4278 mL 51.0694 mL
5 mM 0.4086 mL 2.0428 mL 4.0856 mL 10.2139 mL
10 mM 0.2043 mL 1.0214 mL 2.0428 mL 5.1069 mL
15 mM 0.1362 mL 0.6809 mL 1.3619 mL 3.4046 mL
20 mM 0.1021 mL 0.5107 mL 1.0214 mL 2.5535 mL
25 mM 0.0817 mL 0.4086 mL 0.8171 mL 2.0428 mL
30 mM 0.0681 mL 0.3405 mL 0.6809 mL 1.7023 mL
40 mM 0.0511 mL 0.2553 mL 0.5107 mL 1.2767 mL
50 mM 0.0409 mL 0.2043 mL 0.4086 mL 1.0214 mL
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ISM012-042 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:

ISM012-0422924181-80-4HIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHInhibitorinhibitorinhibit

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