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Baricitinib phosphate (LY-3009104, INCB-028050, Olumiant)

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Baricitinib phosphate (LY-3009104, INCB-028050, Olumiant)
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500mg$290Check With Us
1g$470Check With Us
5g$1185Check 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.

References: Fridman JS, et al. Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050. J Immunol. 2010 May 1;184(9):5298-307.

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Molecular Weight (MW)469.41
Molecular FormulaC16H20N7O6PS
CAS No.1187595-84-1
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: >30 mg/mLr
Water: N/Ar
Ethanol: N/A
Solubility In Vivo0.5% CMC+0.25% Tween 80: 30 mg/mL
SMILES CodeN#CCC1(N2N=CC(C3=C4C(NC=C4)=NC=N3)=C2)CN(S(=O)(CC)=O)C1.O=P(O)(O)O
Synonymstrade name Olumiant; LY3009104 phosphate; LY-3009104; LY 3009104; INCB028050 phosphate; INCB-028050; INCB 028050; Baricitinib phosphate.
ProtocolIn VitroIn 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.
In VivoBaricitinib 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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.1303 mL10.6517 mL21.3033 mL42.6067 mL
5mM0.4261 mL2.1303 mL4.2607 mL8.5213 mL
10mM0.2130 mL1.0652 mL2.1303 mL4.2607 mL
20mM0.1065 mL0.5326 mL1.0652 mL2.1303 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (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.