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Chemical Structure| 104931-56-8 Chemical Structure| 104931-56-8

Structure of Tranilast sodium
CAS No.: 104931-56-8

Chemical Structure| 104931-56-8

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Tranilast is an antiallergic agent.

Synonyms: MK-341 sodium; SB 252218 sodium

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Product Details of Tranilast sodium

CAS No. :104931-56-8
Formula : C18H16NNaO5
M.W : 349.31
SMILES Code : O=C([O-])C1=CC=CC=C1NC(/C=C/C2=CC=C(OC)C(OC)=C2)=O.[Na+]
Synonyms :
MK-341 sodium; SB 252218 sodium
MDL No. :MFCD14584862
InChI Key :KZGHWWBBHZLTTA-VRTOBVRTSA-M
Pubchem ID :23669590

Safety of Tranilast sodium

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P264-P270-P301+P312-P330-P501

Related Pathways of Tranilast sodium

GPCR

Isoform Comparison

Biological Activity

Description
Tranilast sodium (MK-341 sodium) serves as an anti-atopic agent and is effective in suppressing the production of prostaglandin D2 (PGD2) with an IC50 of 0.1 mM. This compound is known for its anti-inflammatory and immunomodulatory effects[1].

In Vitro:

Cell Line
Concentration Treated Time Description References
Human lung adenocarcinoma CAFs 0.01 mg/ml 6, 24, and 48 hours Reduced TGF-β1 protein concentration and mRNA expression PMC9684407
4T1-derived CAFs 0.01 and 10 mg/ml 24 and 48 hours Suppressed TGF-β expression PMC9684407
CAFs 200μM and 400μM 2 days Tranilast inhibited CAFs viability and proliferation, and down-regulated IL-8 mRNA levels. PMC7923322
SH-SY5Y neuroblastoma cells 2.5 μM - 10 μM 24 hours To evaluate the NMD-activating effect of Tranilast, which efficiently reactivated NMD activity and suppressed GFP-GR36 or (G4C2)36-induced apoptosis PMC6487333

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c and C57BL/6 mice 4T1 and E0771 breast cancer models Intravenous injection 2 mg/kg (daily) and 4 mg/kg (every other day) Daily or every other day for 6 days Optimized TME mechanomodulation and tumor perfusion, reduced tumor stiffness, improved vascular perfusion PMC9684407
Mice 4T1 and E0771 mouse breast cancer models Oral 200 mg/kg Daily Tranilast reduced collagen and hyaluronan content and increased the fraction of perfused vessels, thereby improving perfusion and oxygenation and reducing hypoxic regions. PMC7856901
BALB/c nude mice Subcutaneous inoculation model of 5-8F cells mixed with CAFs Orthotopic injection 200μM Once daily for three days Tranilast inhibited the CAF-induced proliferation of NPC cells in vivo and restored tumor sensitivity to radiation. PMC7923322
BALB/c and C57BL/6 female mice 4T1 and E0771 triple-negative breast cancer models Oral (Tranilast), intraperitoneal (Doxorubicin), intravenous (Doxil) 200 mg/kg Tranilast daily oral, Doxorubicin intraperitoneal every 3 days, Doxil intravenous weekly, until tumor volume reached 1200mm3 or animal death Combination of tranilast with Doxil caused a pronounced reduction in extracellular matrix components and an increase in the intratumoral vessel diameter and pericyte coverage, indicators of TME normalization. These modifications resulted in a significant increase in tumor perfusion and oxygenation and enhanced treatment efficacy as indicated by the notable reduction in tumor size. Tranilast further normalized the immune TME by restoring the infiltration of T cells and increasing the fraction of T cells that migrate away from immunosuppressive cancer-associated fibroblasts. PMC6993226
C57BL/6 mice Abdominal aortic banding model Oral 100 mg/kg 11 weeks To investigate the effects of Tranilast on cardiac hypertrophy and function, results showed that Tranilast significantly limited the development of cardiac hypertrophy, prevented the fall in left ventricular function and ventricular dilatation PMC2193589
Drosophila PR36 or GFP-GR36-expressing Drosophila model Oral (added to food) 10 μM Continuous administration starting from larval stage To evaluate the protective effect of Tranilast against PR36 or GFP-GR36-induced neurotoxicity, which significantly improved survival rate and motor function in flies PMC6487333

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.86mL

0.57mL

0.29mL

14.31mL

2.86mL

1.43mL

28.63mL

5.73mL

2.86mL

References

 

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