Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Momelotinib sulfate is an ATP-competitive JAK1/JAK2 inhibitor (IC50: 11 nM/18 nM). It has 10-fold selectivity versus JAK3.
パッケージサイズ | 在庫状況 | 単価(税別) |
---|---|---|
2 mg | 約 5 days | ¥ 10,500 |
5 mg | 約5 days | ¥ 18,000 |
1 mL * 10 mM (in DMSO) | 約5 days | ¥ 26,000 |
ターゲット&IC50 | JAK2:18 nM, JAK1:11 nM, JAK3:155 nM |
In vivo | Administering Momelotinib sulfate at doses of 50 and 100 mg/kg had minimal impact on peripheral blood counts over 8 weeks. The median peak plasma concentrations reached 7.1 μM and 32.1μM for the lower and higher doses, respectively, with a 2-hour half-life. Trough levels were observed at 10nM (25 mg/kg) and 900nM (50 mg/kg) 12 hours post-administration. The compound demonstrated high plasma concentrations after oral intake (Cmax= 40.4 μM; Tmax=4 h), suggesting high oral bioavailability. This is likely due to its low blood clearance rate (6.3 mL/min/kg), indicating reduced hepatic first-pass metabolism. In a study, by day 34 post-transplantation, white blood cell counts and hematocrit values in Balb/c mice exceeded the normal range by more than one standard deviation (SD). Subsequent treatment with 25 mg/kg or 50 mg/kg Momelotinib sulfate, or a vehicle control, initiated a rapid decrease in white cell counts within six days and a decrease in hematocrit after 20 days, showing the drug's efficacy in modulating hematologic parameters. |
別名 | CYT387 sulfate salt |
分子量 | 610.62 |
分子式 | C23H26N6O10S2 |
CAS No. | 1056636-06-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 6.2 mg/mL (10.15 mM)
You can also refer to dose conversion for different animals. 詳細
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Momelotinib sulfate 1056636-06-6 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells JAK CYT387 sulfate salt Momelotinib Sulfate CYT387 Sulfate CYT 387 Sulfate CYT-387 Sulfate Inhibitor inhibitor inhibit