Irsogladine

Alias: MN1695; MN 1695; Gaslon; MN-1695;Irsogladine maleate;
Cat No.:V0796 Purity: ≥98%
Irsogladine (MN1695; MN 1695; Gaslon; MN-1695; Dicloguamine),a mucosal protective drug, is a novel and potent PDE4 inhibitor and muscarinic acetylcholine receptor binder with anti-ulceric activity.
Irsogladine Chemical Structure CAS No.: 57381-26-7
Product category: PDE
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
500mg
1g
2g
Other Sizes

Other Forms of Irsogladine:

  • Irsogladine maleate
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Irsogladine (MN1695; MN 1695; Gaslon; MN-1695; Dicloguamine), a mucosal protective drug, is a novel and potent PDE4 inhibitor and muscarinic acetylcholine receptor binder with anti-ulceric activity. It is used as an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding. 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%.

Biological Activity I Assay Protocols (From Reference)
ln Vitro

In vitro activity: 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. 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

ln Vivo
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.
Animal Protocol
300 and 500 mg/kg
Mice
References
J Surg Res.1998 Jul 1;77(2):126-31;Pancreas.2002 Nov;25(4):373-7.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C9H7CL2N5
Molecular Weight
256.09
CAS #
57381-26-7
Related CAS #
Irsogladine maleate;84504-69-8
SMILES
ClC1C([H])=C([H])C(=C([H])C=1C1N=C(N([H])[H])N=C(N([H])[H])N=1)Cl
Chemical Name
6-(2,5-dichlorophenyl)-1,3,5-triazine-2,4-diamine
Synonyms
MN1695; MN 1695; Gaslon; MN-1695;Irsogladine maleate;
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 2 mg/mL (7.8 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
Solubility (In Vivo)
Solubility in Formulation 1: 3 mg/mL (11.71 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 3 mg/mL (11.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 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
10 mM 0.3905 mL 1.9524 mL 3.9049 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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g/mol

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02581696 Completed Drug: Lafutidine
Drug: Irsogladine maleate
Peptic Ulcer Boryung Pharmaceutical Co., Ltd August 2015 Phase 1
NCT02759224 Completed Drug: Lafutidine
Drug: Irsogladine maleate
Gastric Ulcer Boryung Pharmaceutical Co., Ltd April 15, 2016 Phase 1
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