2. GPCR/G Protein Neuronal Signaling Metabolic Enzyme/Protease
  3. mAChR Phosphodiesterase (PDE)
  4. Irsogladine

Irsogladine  (Synonyms: Dicloguamine)

Cat. No.: HY-B0327 Purity: 99.97%
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Irsogladine is a PDE4 inhibitor and muscarinic acetylcholine receptor binder.

For research use only. We do not sell to patients.

Irsogladine Chemical Structure

Irsogladine Chemical Structure

CAS No. : 57381-26-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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 USD 55 In-stock
Solution
10 mM * 1 mL in DMSO USD 55 In-stock
Solid
500 mg USD 50 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Irsogladine:

Irsogladine Related Antibodies

Top Publications Citing Use of Products

View All mAChR Isoform Specific Products:

View All Isoforms
mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

View All Phosphodiesterase (PDE) Isoform Specific Products:

View All Isoforms
PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Irsogladine is a PDE4 inhibitor and muscarinic acetylcholine receptor binder. Target: PDE4; mACHR Irsogladine treatment (300 and 500 mg/kg/day) resulted in a dose-dependent reduction of angiogenesis in wild-type mice by 21 and 45.3% (P < 0.02, P < 0.001), in tPA-deficient mice by 42.6 and 46% (P < 0.001, P < 0.001), and in uPA-deficient mice by 27.2 and 46% (P < 0.05, p < 0.001), respectively. Irsogladine inhibits bFGF-induced angiogenesis in wild-type, tPA-knockout, and uPA-knockout mice [1]. Irsogladine up-regulates GJIC between PC cells via regulation of the PKA pathway. It also suggests a useful adjuvant of Irsogladine to pancreatic cancer therapy [2]. irsogladine produces the increase of intracellular cAMP content via non-selective inhibition of PDE isozymes, which may be a key mechanism involved in its gastroprotective actions [3].

IC50 & Target

PDE4

 

Clinical Trial
Molecular Weight

256.09

Formula

C9H7Cl2N5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NC1=NC(N)=NC(C2=CC(Cl)=CC=C2Cl)=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 120 mg/mL (468.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.9049 mL 19.5244 mL 39.0488 mL
5 mM 0.7810 mL 3.9049 mL 7.8098 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: 3 mg/mL (11.71 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 3 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 3 mg/mL (11.71 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

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.9049 mL 19.5244 mL 39.0488 mL 97.6219 mL
5 mM 0.7810 mL 3.9049 mL 7.8098 mL 19.5244 mL
10 mM 0.3905 mL 1.9524 mL 3.9049 mL 9.7622 mL
15 mM 0.2603 mL 1.3016 mL 2.6033 mL 6.5081 mL
20 mM 0.1952 mL 0.9762 mL 1.9524 mL 4.8811 mL
25 mM 0.1562 mL 0.7810 mL 1.5620 mL 3.9049 mL
30 mM 0.1302 mL 0.6508 mL 1.3016 mL 3.2541 mL
40 mM 0.0976 mL 0.4881 mL 0.9762 mL 2.4405 mL
50 mM 0.0781 mL 0.3905 mL 0.7810 mL 1.9524 mL
60 mM 0.0651 mL 0.3254 mL 0.6508 mL 1.6270 mL
80 mM 0.0488 mL 0.2441 mL 0.4881 mL 1.2203 mL
100 mM 0.0390 mL 0.1952 mL 0.3905 mL 0.9762 mL
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Irsogladine 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:

Irsogladine57381-26-7DicloguaminemAChRPhosphodiesterase (PDE)Muscarinic acetylcholine receptorInhibitorinhibitorinhibit

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