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Chemical Structure| 57381-26-7 Chemical Structure| 57381-26-7

Structure of Irsogladine
CAS No.: 57381-26-7

Chemical Structure| 57381-26-7

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Irsogladine is a PDE4 inhibitor and muscarinic acetylcholine receptor binder.

Synonyms: Dicloguamine

4.5 *For Research Use Only !

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Product Details of Irsogladine

CAS No. :57381-26-7
Formula : C9H7Cl2N5
M.W : 256.09
SMILES Code : ClC1=C(C2=NC(N)=NC(N)=N2)C=C(Cl)C=C1
Synonyms :
Dicloguamine
MDL No. :MFCD00866871
InChI Key :ATCGGEJZONJOCL-UHFFFAOYSA-N
Pubchem ID :3752

Safety of Irsogladine

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H312-H332
Precautionary Statements:P280

Isoform Comparison

Biological Activity

Target
  • AChR

  • PDE

In Vitro:

Cell Line
Concentration Treated Time Description References
HCT-15 cells 100 μM and 200 μM 24 hours To evaluate the effects of irsogladine maleate on NF-κB transcriptional activity. Results showed that 100 μM and 200 μM irsogladine maleate decreased NF-κB transcriptional activity by 22% and 29%, respectively. Oncotarget. 2016 Feb 23;7(8):8640-52
Human induced pluripotent stem cell-derived 2D monolayer crypt-villus structural small intestine (2D-hiPSC-SI) 16 µg/mL 48 hours To evaluate the effect of Irsogladine on 2D-hiPSC-SI under normal conditions, results showed that Irsogladine significantly increased Mki67 and Muc2 mRNA expression. Medicina (Kaunas). 2022 Dec 31;59(1):92
RAW 264.7 macrophages 100 and 10 μM 24 hours To evaluate the effects on cAMP levels, cytokine release, ROS and NO production in LPS-stimulated RAW 264.7 macrophages. Results showed that compounds 1 and 2 increased cAMP levels, reduced TNF-α and IL-1β release, and decreased ROS production. Inflamm Res. 2017 Jan;66(1):79-95

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6-ApcMin/+ mice Familial adenomatous polyposis model Dietary administration 5 ppm and 50 ppm 8 weeks To evaluate the inhibitory effects of irsogladine maleate on intestinal polyp formation. Results showed that 5 ppm and 50 ppm irsogladine maleate reduced the number of intestinal polyps to 69% and 66% of the untreated control value, respectively. Additionally, mRNA levels of NF-κB downstream targets, such as IL-1β and IL-6, were significantly decreased, and the levels of oxidative stress-related markers, reactive carbonyl species, in the livers of Min mice were clearly reduced. Oncotarget. 2016 Feb 23;7(8):8640-52
Male Hos: Donryu rats Indomethacin-induced gastric mucosal injury model Oral 1 mg/kg, 3 mg/kg, 10 mg/kg Single dose, lasted for 4 hours To investigate the mucosal protective effect and the mechanisms of action of the anti-ulcer drug irsogladine maleate in gastric injury induced by indomethacin in rats. Results showed that irsogladine maleate significantly reduced the number and severity of gastric mucosal lesions and decreased the levels of proinflammatory cytokines (TNF-α, IL-1β, IL-8) and MPO in gastric mucosa. World J Gastroenterol. 2008 Aug 14;14(30):4784-90
ICR mice Ethanol/HCl-induced gastric ulcer model Oral 1 mg/kg and 10 mg/kg Pretreatment 1 hour before IM significantly reduced the extent of ethanol/HCl mixture-induced gastric ulceration, exhibiting dose-related gastroprotection. Korean J Intern Med. 2021 Jan;36(1):67-75

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.90mL

0.78mL

0.39mL

19.52mL

3.90mL

1.95mL

39.05mL

7.81mL

3.90mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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