Baricitinib
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MedKoo CAT#: 205893

CAS#: 1187594-09-7 (free base)

Description: Baricitinib, also known as INCB028050 or LY3009104, is a selective orally bioavailable JAK1/JAK2 inhibitor with nanomolar potency against JAK1 (5.9 nM) and JAK2 (5.7 nM). INCB028050 inhibits intracellular signaling of multiple proinflammatory cytokines including IL-6 and IL-23 at concentrations <50 nM. INCB028050 was also effective in multiple murine models of arthritis, with no evidence of suppression of humoral immunity or adverse hematologic effects. Baricitinib was approved for the treatment of rheumatoid arthritis (RA) in the United States.


Price and Availability

Size
Price

200mg
USD 150
5g
USD 1250
Size
Price

500mg
USD 250
10g
USD 1950
Size
Price

1g
USD 450
20g
USD 2950

Baricitinib, purity > 98%, is in stock. The same day shipping out after order is received. Note: the estimated shipping out time for order > 10g may be 2 weeks.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 205893
Name: Baricitinib
CAS#: 1187594-09-7 (free base)
Chemical Formula: C16H17N7O2S
Exact Mass: 371.11644
Molecular Weight: 371.41688
Elemental Analysis: C, 51.74; H, 4.61; N, 26.40; O, 8.62; S, 8.63


Related CAS #: 1187594-09-7 (free base)   1187595-84-1 (phosphate)    

Synonym: INCB028050; INCB-028050; INCB 028050; LY3009104; LY-3009104; LY 3009104; Baricitinib.

IUPAC/Chemical Name: 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(ethylsulfonyl)azetidin-3-yl)acetonitrile

InChi Key: XUZMWHLSFXCVMG-UHFFFAOYSA-N

InChi Code: InChI=1S/C16H17N7O2S/c1-2-26(24,25)22-9-16(10-22,4-5-17)23-8-12(7-21-23)14-13-3-6-18-15(13)20-11-19-14/h3,6-8,11H,2,4,9-10H2,1H3,(H,18,19,20)

SMILES Code: N#CCC1(N2N=CC(C3=C4C(NC=C4)=NC=N3)=C2)CN(S(=O)(CC)=O)C1


Technical Data

Appearance:
white solid powder

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

Safety Data Sheet (MSDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

Related CAS#
1187594-09-7 (Baricitinib free base)
1187595-84-1 (Baricitinib phosphate)


References

1: Jabbari A, Dai Z, Xing L, Cerise JE, Ramot Y, Berkun Y, Sanchez GA, Goldbach-Mansky R, Christiano AM, Clynes R, Zlotogorski A. Reversal of Alopecia Areata Following Treatment With the JAK1/2 Inhibitor Baricitinib. EBioMedicine. 2015 Feb 26;2(4):351-5. doi: 10.1016/j.ebiom.2015.02.015. eCollection 2015 Apr. PubMed PMID: 26137574; PubMed Central PMCID: PMC4486197.

2: Khan IM, Perrard XY, Brunner G, Lui H, Sparks LM, Smith SR, Wang X, Shi ZZ, Lewis DE, Wu H, Ballantyne CM. Intermuscular and perimuscular fat expansion in obesity correlates with skeletal muscle T cell and macrophage infiltration and insulin resistance. Int J Obes (Lond). 2015 Jun 4. doi: 10.1038/ijo.2015.104. [Epub ahead of print] PubMed PMID: 26041698.

3: Keystone EC, Taylor PC, Drescher E, Schlichting DE, Beattie SD, Berclaz PY, Lee CH, Fidelus-Gort RK, Luchi ME, Rooney TP, Macias WL, Genovese MC. Safety and efficacy of baricitinib at 24 weeks in patients with rheumatoid arthritis who have had an inadequate response to methotrexate. Ann Rheum Dis. 2015 Feb;74(2):333-40. doi: 10.1136/annrheumdis-2014-206478. Epub 2014 Nov 27. PubMed PMID: 25431052; PubMed Central PMCID: PMC4316868.

4: Shi JG, Chen X, Lee F, Emm T, Scherle PA, Lo Y, Punwani N, Williams WV, Yeleswaram S. The pharmacokinetics, pharmacodynamics, and safety of baricitinib, an oral JAK 1/2 inhibitor, in healthy volunteers. J Clin Pharmacol. 2014 Dec;54(12):1354-61. doi: 10.1002/jcph.354. PubMed PMID: 24965573.

5: Norman P. Selective JAK inhibitors in development for rheumatoid arthritis. Expert Opin Investig Drugs. 2014 Aug;23(8):1067-77. doi: 10.1517/13543784.2014.918604. Epub 2014 May 12. Review. PubMed PMID: 24818516.

6: Smolen JS, van der Heijde D, Machold KP, Aletaha D, Landewé R. Proposal for a new nomenclature of disease-modifying antirheumatic drugs. Ann Rheum Dis. 2014 Jan;73(1):3-5. doi: 10.1136/annrheumdis-2013-204317. Epub 2013 Sep 26. PubMed PMID: 24072562.

7: van Vollenhoven RF. Small molecular compounds in development for rheumatoid arthritis. Curr Opin Rheumatol. 2013 May;25(3):391-7. doi: 10.1097/BOR.0b013e32835fd828. Review. PubMed PMID: 23492738.