Baricitinib (LY-3009104, INCB-028050)

This product is for research use only, not for human use. We do not sell to patients.

For small sizes, please check our retail website as below: www.invivochem.com

Size	Price	Stock
1g	$390	In Stock
2g	$590	In Stock
5g	$1490	In Stock

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Cat #: V0338 CAS #: 1187594-09-7 (free base); Purity ≥ 98%

Description: Baricitinib, (also known as LY3009104 or INCB028050; trade name: Olumiant), is a potent, selective, ATP competitive and orally bioavailable inhibitor of tyrosine-protein kinase JAK1 (Janus kinase) or JAK2 with anti-inflammatory activity.

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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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	371.42
Molecular Formula	C16H17N7O2S
CAS No.	1187594-09-7 (free base);
Storage	-20℃ for 3 years in powder formr
Storage	-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
Synonyms	Olumiant; Baricitinib; LY-3009104; INCB 028050; LY3009104; LY 3009104; INCB028050; INCB-028050;

Protocol	In Vitro	In cell-based assays, Baricitinib (INCB028050) 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.
Protocol	In Vivo	Baricitinib (INCB028050) 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	1mg	5mg	10mg	20mg
1mM	2.6924 mL	13.4618 mL	26.9237 mL	53.8474 mL
5mM	0.5385 mL	2.6924 mL	5.3847 mL	10.7695 mL
10mM	0.2692 mL	1.3462 mL	2.6924 mL	5.3847 mL
20mM	0.1346 mL	0.6731 mL	1.3462 mL	2.6924 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

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)

Volume_(start)

Concentration_(final)

Volume_(final)

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.