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500mg | $290 | Check With Us |
1g | $470 | Check With Us |
5g | $1185 | Check With Us |
Cat #: V0096 CAS #: 1187595-84-1 Purity ≥ 98%
Description: Baricitinib phosphate, the phosphate salt of Baricitinib which is also known as LY3009104 or INCB028050 or trade name Olumiant, is a potent, selective, ATP competitive and orally bioavailable inhibitor of tyrosine-protein kinase JAK1 or JAK2.
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Molecular Weight (MW) | 469.41 |
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Molecular Formula | C16H20N7O6PS |
CAS No. | 1187595-84-1 |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent | |
Solubility In Vitro | DMSO: >30 mg/mLr |
Water: N/Ar | |
Ethanol: N/A | |
Solubility In Vivo | 0.5% CMC+0.25% Tween 80: 30 mg/mL |
SMILES Code | N#CCC1(N2N=CC(C3=C4C(NC=C4)=NC=N3)=C2)CN(S(=O)(CC)=O)C1.O=P(O)(O)O |
Synonyms | trade name Olumiant; LY3009104 phosphate; LY-3009104; LY 3009104; INCB028050 phosphate; INCB-028050; INCB 028050; Baricitinib phosphate. |
Protocol | In Vitro | In cell-based assays, Baricitinib phosphate (INCB028050 phosphate) proves to be a potent inhibitor of JAK signaling and function. In PBMCs, Baricitinib inhibits IL-6-stimulated phosphorylation of the canonical substrate STAT3 (pSTAT3) and subsequent production of the chemokine MCP-1 with IC50 values of 44 nM and 40 nM, respectively. In isolated naive T-cells, INCB028050 also inhibits pSTAT3 stimulated by IL-23 (IC50=20 nM). Importantly, this inhibition prevented the production of two pathogenic cytokines (IL-17 and IL-22) produced by Th17 cells-a subtype of helper T cells with demonstrable inflammatory and pathogenic properties-with an IC50 value of 50 nM. In stark contrast, the structurally similar but ineffective JAK1/2 inhibitors INCB027753 and INCB029843 has no significant effect in any of these assays systems when tested at concentrations up to 10 μM. |
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In Vivo | Baricitinib phosphate (INCB028050 phosphate) treatment, compares with vehicle, inhibits the increase in hind paw volumes during the 2 wk of treatment by 50% at a dose of 1 mg/kg and >95% at doses of 3 or 10 mg/kg. Because baseline paw volume measurements are taken on treatment day 0-in animals with significant signs of disease-it is possible to have >100% inhibition in animals showing marked improvement in swelling. |
Solvent volume to be added | Mass (the weight of a compound) | |||
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Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 2.1303 mL | 10.6517 mL | 21.3033 mL | 42.6067 mL |
5mM | 0.4261 mL | 2.1303 mL | 4.2607 mL | 8.5213 mL |
10mM | 0.2130 mL | 1.0652 mL | 2.1303 mL | 4.2607 mL |
20mM | 0.1065 mL | 0.5326 mL | 1.0652 mL | 2.1303 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.