YM-341619

YM-341619 (AS1617612) is a potent and orally active STAT6 inhibitor with an IC50 of 0.70 nM. YM-341619 inhibits Th2 differentiation in mouse spleen T cells induced by IL-4 (IC50=0.28 nM) without affecting Th1 cell differentiation. YM-341619 is a promising compound for the the research of allergic diseases, such as allergic asthma.

Product information

CAS Number: 643082-52-4

Molecular Weight: 458.44

Formula: C22H21F3N6O2

Chemical Name: 2-{[4-(morpholin-4-yl)phenyl]amino}-4-{[(2,3,6-trifluorophenyl)methyl]amino}pyrimidine-5-carboxamide

Smiles: NC(=O)C1=CN=C(NC2C=CC(=CC=2)N2CCOCC2)N=C1NCC1C(F)=CC=C(F)C=1F

InChiKey: IUUUCMFTTBSFIT-UHFFFAOYSA-N

InChi: InChI=1S/C22H21F3N6O2/c23-17-5-6-18(24)19(25)15(17)11-27-21-16(20(26)32)12-28-22(30-21)29-13-1-3-14(4-2-13)31-7-9-33-10-8-31/h1-6,12H,7-11H2,(H2,26,32)(H2,27,28,29,30)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

YM-341619 (0.1-100 nM; pretreatment 30 min before IL-4) inhibits IL-4-increased STAT6 luciferase gene activity in a concentration dependent manner, exhibiting an IC50 value of 1.5 nM in FW4 cells. YM-341619 (0.1-10 nM; pretreatment 30 min before IL-4) concentration-dependently decreases the production of IL-4 and the expression of GATA-3 mRNA in T cells cultured with IL-4. And it has no effects on the production of IFN-γ or the expression of T-bet (a Th1 transcription factor) mRNA in T cells cultured with IL-12.

In Vivo:

YM-341619 (intravenous injection; 1 mg/kg) exhibits CLtot, t1/2, Vd values of 36.1 mL/min/kg, 1.0 hour, 3117 mL/kg, respectively. And it exhibits Cmax, Tmax, AUC, and F% values of 80 ng/mL, 0.5h, 114 ng h/mL and 25%, respectively in 8-week-old female balb/c mice. YM-341619 (oral administration; 0.003-0.03 mg/kg) suppresses the IgE level in a dose-dependent manner, but not the IgG2a level, and the ED50 value of YM-341619 for the suppression of IgE production is 0.026 mg/kg. YM-341619 tends to decrease IL-4 production and decrease IL-13 production in a dose-dependent manner (both 57%), but does not affect IFN-γ production in DNP-Ascaris-sensitized rats.

Products are for research use only. Not for human use.