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YM-341619

Cat. No. M31278
YM-341619 Structure
Synonym:

AS1617612

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Biological Activity

YM-341619 (AS1617612) is a potent, orally active STAT6 inhibitor with an IC50 value of 0.70 nM. It can be used in studies related to allergic diseases (e.g., asthma and atopic rhinitis) by selectively inhibiting the differentiation of CD4(+) T cells into the Th2 subpopulation, and thereby inhibiting the ability to inhibit allergen-induced Th2 responses.

Chemical Information
Molecular Weight 458.45
Formula C22H21F3N6O2
CAS Number 643082-52-4
Form Solid
Solubility (25°C) DMSO 50 mg/mL
Storage -20°C
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Ibrahim Sulaiman, et al. Pulm Pharmacol Ther. Molecularly targeted therapies for asthma: Current development, challenges and potential clinical translation

[2] Keiko Ohga, et al. Eur J Pharmacol. YM-341619 suppresses the differentiation of spleen T cells into Th2 cells in vitro, eosinophilia, and airway hyperresponsiveness in rat allergic models

[3] Shinya Nagashima, et al. Bioorg Med Chem. Identification of 4-benzylamino-2-[(4-morpholin-4-ylphenyl)amino]pyrimidine-5-carboxamide derivatives as potent and orally bioavailable STAT6 inhibitors

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  Catalog
Abmole Inhibitor Catalog




Keywords: YM-341619, AS1617612 supplier, STAT, inhibitors, activators


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