Baricitinib (INCB028050)

Catalog No.S2851 Synonyms: LY3009104

For research use only.

Baricitinib (LY3009104, INCB028050) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM in cell-free assays, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Baricitinib is found to reduce or interrupt the passage of the virus into target cells and is used in the treatment research for COVID-19. Phase 3.

Baricitinib (INCB028050) Chemical Structure

CAS No. 1187594-09-7

Selleck's Baricitinib (INCB028050) has been cited by 31 publications

Purity & Quality Control

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Biological Activity

Description Baricitinib (LY3009104, INCB028050) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM in cell-free assays, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Baricitinib is found to reduce or interrupt the passage of the virus into target cells and is used in the treatment research for COVID-19. Phase 3.
Targets
JAK2 [1]
(Cell-free assay)
JAK1 [1]
(Cell-free assay)
TYK2 [1]
(Cell-free assay)
JAK3 [1]
(Cell-free assay)
5.7 nM 5.9 nM 53 nM >400 nM
In vitro

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 PBMCs. Baricitinib also inhibits pSTAT3 stimulated by IL-23 with IC50 od 20 nM in isolated naive T-cells. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human CD34+ cells MXrGeY5kfGmxbjDhd5NigQ>? NVO5S3djPDVibXnudy=> MmW0TY5pcWKrdHnvckBw\iCMQVuyJIhwdW:maX3ldkBqdiCqdX3hckBETDN2KzDj[YxteyC|cHnr[YQhcW62bzDoeY1idiC5aH;s[UBjdG:xZDDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFXQU{1qdmS3Y3XkJHNVSVRvNTDwbI9{eGixconsZZRqd25icILlbY5kfWKjdHXkJIZweiB2NTDtbY5{KG[xbHzve4VlKGK7IFXQU{Bi\GSrdHnvckBu\WG|dYLl[EBi\nSncjCxOUBucW6|IHL5JGZCS1NiYX7hcJl{cXNuIFnDOVA:OC5yOEe4{txO M1zQblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEG3OVM{Lz5{NESxO|U{OzxxYU6=
human UT7 cells NYPy[3hWTnWwY4Tpc44h[XO|YYm= NEftb|dKdmirYnn0bY9vKG:oIFrBT|IhcW5iaIXtZY4hXVR5IHPlcIx{KGG|c3Xzd4VlKGG|IIP1dJBz\XO|aX;uJI9nKEWSTz3zeIlufWyjdHXkJHNVSVR3IIDoc5NxcG:{eXzheIlwdiCkeTDBcJBp[VOlcnXlckBie3OjeR?= M3;MU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{eyOlU{Lz5{NkO3NlY2OzxxYU6=
human TF1 cells MUfGeY5kfGmxbjDhd5NigQ>? MX\Jcohq[mm2aX;uJI9nKEqDS{GgbY4hcHWvYX6gWGYyKGOnbHzzJIF{e2W|c3XkJIF{KHO3cIDy[ZN{cW:wIH;mJGlNPi2|dHnteYxifGWmIGPURXQ{KHCqb4PwbI9zgWyjdHnvckBjgSCDbIDoZXNkemWnbjDhd5NigQ>? M3PTN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{eyOlU{Lz5{NkO3NlY2OzxxYU6=
CD34+ M1nFSmZ2dmO2aX;uJIF{e2G7 NIGy[3c1PSCvaX7z NFPweI9KdmirYnn0bY9vKG:oIFrBT|IhcG:vb3TpcYVzKGmwIHj1cYFvKEOGM{SrJINmdGy|IIPwbYtm\CCrboTvJIh2dWGwIIfoc4xmKGKub3;kJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gSXBQNWmwZIXj[YQhW1SDVD21JJBpd3OyaH;yfYxifGmxbjDwdoVqdmO3YnH0[YQh\m:{IES1JI1qdnNiZn;scI94\WRiYomgSXBQKGGmZHn0bY9vKG2nYYP1doVlKGGodHXyJFE2KG2rboOgZpkhTkGFUzDhcoFtgXOrczygTWM2OCB;IECuNFg4QCEQvF2u Mle3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2MUe1N|MoRjJ2NEG3OVM{RC:jPh?=
TF1 NGH6T2VHfW6ldHnvckBie3OjeR?= M{eybWlvcGmkaYTpc44hd2ZiSlHLNUBqdiCqdX3hckBVTjFiY3XscJMh[XO|ZYPz[YQh[XNic4XwdJJme3Orb36gc4YhUUx4LYP0bY12dGG2ZXSgV3RCXDNicHjvd5Bpd3K7bHH0bY9vKGK7IFHsdIhiW2O{ZXXuJIF{e2G7LDDJUmghRSByLkCxO{DPxE1w NELIbGU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO3NlY2Oyd-Mk[zO|I3PTN:L3G+
UT7 Mn34SpVv[3Srb36gZZN{[Xl? NEjTUJpKdmirYnn0bY9vKG:oIFrBT|IhcW5iaIXtZY4hXVR5IHPlcIx{KGG|c3Xzd4VlKGG|IIP1dJBz\XO|aX;uJI9nKEWSTz3zeIlufWyjdHXkJHNVSVR3IIDoc5NxcG:{eXzheIlwdiCkeTDBcJBp[VOlcnXlckBie3OjeTygTW5JKD1iMD6zNUDPxE1w MmnKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ|N{K2OVMoRjJ4M{eyOlU{RC:jPh?=
HeLa NXrCNm91TnWwY4Tpc44h[XO|YYm= M{XpSVUhfU1? MnTONkBpenN? M{CzO2lvcGmkaYTpc44hd2ZiSV\O[4FudWFvaX7keYNm\CCMQVuyJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDI[WxiKGOnbHzzJIF1KDVidV2gbY5kfWKjdHXkJIZweiB{IHjyd{BjgSCZZYP0[ZJvKGKub4SgcYV1cG:m MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF|N{O1PUc,OjdzM{ezOVk9N2F-
A673 M4XJfJFJXFNiYYPzZZk> NUnZ[Jl5eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFG2O|Mh[2WubIO= NWK2eo1QRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-SH MkHhdWhVWyCjc4PhfS=> Mn;tdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tV2gh[2WubIO= MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
NB1643 NFTrSWlyUFSVIHHzd4F6 M2XEWJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQkG2OFMh[2WubIO= NXn1PIpJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh41 NVjvcGdWeUiWUzDhd5NigQ>? NUHDbXVFeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoOFEh[2WubIO= Mm\ZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
LAN-5 M3rUdJFJXFNiYYPzZZk> NGPQTpJyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTFHOMVUh[2WubIO= MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Assay
Methods Test Index PMID
Western blot phSTAT1 / phSTAT3 28369741
In vivo Baricitinib inhibits IL-6–stimulated phosphorylation of STAT3 in whole blood with an IC50 of 128 nM. Baricitinib (10 mg/kg p.o.) is expected to inhibit JAK1/2 signaling (by ≥50%) in rats for about 8 hours. Baricitinib (10 mg/mL, p.o.) inhibits disease scores in dose-dependent manner in rats with established disease in the adjuvant arthritis model. Baricitinib treatment, compared with vehicle, inhibits the increase in hind paw volumes during the 2 weeks of treatment by 50% at a dose of 1 mg/kg and >95% at doses of 3 mg/kg or 10 mg/kg. Baricitinib treatment, compared with vehicle, also inhibits composite score of immune infiltrate, edema, and periarticular tissue appearance by 27% at a dose of 1 mg/kg, 64% at doses of 3 mg/kg and 82% at doses of 10 mg/kg in rats with established disease in the adjuvant arthritis model. Baricitinib reduces bone resorption by 15%, 61%, and 67% with increasing dose level (1, 3, and 10 mg/kg) in rats with established disease in the adjuvant arthritis model. Baricitinib (10 mg/kg, daily for 2 wk, p.o.) results in radiographic improvements with restoration of the normal architecture and appearance to the ankle and tarsals in rats with established disease in the adjuvant arthritis model. Baricitinib reduces levels of pSTAT3 in a dose- and time-dependent manner in the peripheral blood of rAIA animals. Baricitinib (10 mg/mL, p.o.) improves a composite score of joint damage by 47% in the murine CIA model. Baricitinib (10 mg/kg) reduces pannus (74%) and bone damage (78%) and improves cartilage damage (43%) and signs of inflammation (33%), resulting in a 53% improvement in an aggregate score of disease in the collagen Ab-induced arthritis (CAIA) murine model. Baricitinib (10 mg/kg) inhibits the delayed-type hypersensitivity response by 48% in both the CIA and CAIA models. [1] Baricitinib is efficacious in active rheumatoid arthritis patients refractory to disease modifying drugs and biologics. [2] Baricitinib preferentially inhibits JAK1 and JAK2, with 10-fold selectivity over Tyk2 and 100-fold over JAK3. The observed effects of GLPG-0634 on the ACR20, albeit in a smaller study, appear to be at least as good as that seen with tofacitinib and superior to that of baricitinib, since baricitinib only moderately affect the ACR20 values in Phase IIa clinical studies. [3] Baricitinib has the dose-limiting side-effect of inducing anaemia which has been attributed to its effects on JAK2 but has clearly shown efficacy. [4]

Protocol (from reference)

Animal Research:[1]
  • Animal Models: Collagen-induced arthritis (CIA) mice
  • Dosages: 10 mg/mL
  • Administration: orally

Solubility (25°C)

In vitro

DMSO 74 mg/mL
(199.23 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.

5mg/mL

Chemical Information

Molecular Weight 371.42
Formula

C16H17N7O2S

CAS No. 1187594-09-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCS(=O)(=O)N1CC(C1)(CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3

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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. )

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05189106 Not yet recruiting Drug: Baricitinib Amyotrophic Lateral Sclerosis|Alzheimer Disease|Mild Cognitive Impairment Massachusetts General Hospital|Holy Cross Hospital Florida February 1 2022 Phase 1|Phase 2
NCT05074420 Not yet recruiting Drug: Baricitinib Covid19|Corona Virus Infection Eli Lilly and Company December 17 2021 Phase 3
NCT04208464 Recruiting Drug: Baricitinib Idiopathic Inflammatory Myopathies University of Manchester|Eli Lilly and Company|Manchester Clinical Trials Unit|Karolinska Institutet October 7 2021 Phase 2
NCT04358614 Completed Drug: Baricitinib 4 MG Oral Tablet COVID|Pneumonia Fabrizio Cantini|Hospital of Prato March 16 2020 Phase 2|Phase 3
NCT04088396 Recruiting Drug: Baricitinib|Drug: Placebo Systemic Juvenile Idiopathic Arthritis Eli Lilly and Company February 12 2020 Phase 3

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
Do you know if S2851 will dissolve directly into 0.5% methylcellulose (vehicle for oral gavage treatments) or is acid required to dissolve it?

Answer:
S2851 dissolve directly into 0.5% methylcellulose, and this is cited from the reference. We also test that dissolve S2851 into 30% PEG400/0.5% Tween80/5% propylene glycol. The solubility is about 30 mg/mL.

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