Baricitinib
Based on 78 publication(s) in Google Scholar
Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.93%
- CAS. Nr.: 1187594-09-7
- Formel: C16H17N7O2S
- Molecular Weight:371.42
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Publications Citing Use of MedChemExpress (MCE) Baricitinib
More- Signal Transduct Target Ther. 2025 Dec 15;10(1):406. [Abstract]
- Signal Transduct Target Ther. 2021 Apr 24;6(1):165. [Abstract]
- Science. 2017 Dec 1;358(6367):eaan4368. [Abstract]
- Cell. 2021 Apr 15;184(8):2167-2182.e22. [Abstract]
- Drug Resist Updat. 2025 Jul:81:101224. [Abstract]
- Ann Rheum Dis. 2025 Sep 25:S0003-4967(25)04383-3. [Abstract]
- Cancer Res. 2021 Dec 15;81(24):6131-6141. [Abstract]
- Sci Immunol. 2024 Jul 12;9(97):eadn0178. [Abstract]
- ACS Nano. 2024 Mar 19;18(11):8337-8349. [Abstract]
- Nat Commun. 2023 Apr 24;14(1):2342. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Adv Sci (Weinh). 2024 Dec 5:e2410360. [Abstract]
- Adv Sci (Weinh). 2020 Sep 24;7(21):2002518. [Abstract]
- J Clin Invest. 2024 Oct 1;134(19):e176828. [Abstract]
- J Clin Invest. 2021 Dec 15;131(24):e145501. [Abstract]
- Sci Adv. 2024 Mar 22;10(12):eadl0368. [Abstract]
- J Allergy Clin Immunol. 2024 Apr;153(4):1125-1139. [Abstract]
- J Immunother Cancer. 2026 Jan 8;14(1):e012121. [Abstract]
- J Immunother Cancer. 2025 May 11;13(5):e010831. [Abstract]
- J Exp Med. 2024 Mar 4;221(3):e20230683. [Abstract]
- Diabetologia. 2024 Jan;67(1):124-136. [Abstract]
- Cell Death Dis. 2025 Jul 11;16(1):512. [Abstract]
- Proc Natl Acad Sci U S A. 2025 Aug 19;122(33):e2514837122. [Abstract]
- Acta Pharmacol Sin. 2021 May;42(5):814-823. [Abstract]
- Phytomedicine. 2025 Nov 25:150:157605. [Abstract]
- Br J Pharmacol. 2024 Dec;181(23):4804-4821. [Abstract]
- Mol Syst Biol. 2024 Jan;20(1):28-55. [Abstract]
- JHEP Rep. 2025 Nov 6.
- Aging Cell. 2025 Oct 20:e70273. [Abstract]
- J Autoimmun. 2022 Feb;127:102793. [Abstract]
- JCI Insight. 2025 Dec 11:e185380. [Abstract]
- Mol Ther Nucleic Acids. 2025 Mar 5;36(2):102502. [Abstract]
- J Ethnopharmacol. 2026 Apr 24:361:121268. [Abstract]
- Commun Biol. 2021 Jun 2;4(1):654. [Abstract]
- Inflammation. 2021 Feb;44(1):206-216. [Abstract]
- Int J Mol Sci. 2026 Jun 3;27(11):5047. [Abstract]
- Int J Mol Sci. 2025 May 19;26(10):4849. [Abstract]
- Int Immunopharmacol. 2026 Feb 15:171:116137. [Abstract]
- Int Immunopharmacol. 2024 Aug 9:140:112894. [Abstract]
- Eur J Pharm Sci. 2024 Jul 4:106845. [Abstract]
- Int Immunopharmacol. 2022 Sep:110:109044. [Abstract]
- RSC Adv. 2018 Jun 13;8(38):21534-21540. [Abstract]
- Rheumatology (Oxford). 2023 Aug 1;62(8):2908-2917. [Abstract]
- Toxicol Sci. 2020 Aug 1;176(2):410-422. [Abstract]
- J Dermatol Sci. 2025 Mar;117(3):52-60. [Abstract]
- J Biol Chem. 2026 Jan 23;302(3):111200. [Abstract]
- Sci Rep. 2022 May 12;12(1):7843. [Abstract]
- Pharmacol Rep. 2024 Oct;76(5):1079-1088. [Abstract]
- Int J Obes (Lond). 2015 Nov;39(11):1607-18. [Abstract]
- Heliyon. 2018 Nov 26;4(11):e00979. [Abstract]
- J Immunol. 2013 Oct 1;191(7):3568-77. [Abstract]
- Immunol Res. 2025 Jun 26;73(1):99. [Abstract]
- Platelets. 2022 Apr 3;33(3):404-415. [Abstract]
- PLoS One. 2017 Jul 14;12(7):e0181126. [Abstract]
- Biomed Chromatogr. 2026 Mar;40(3):e70376. [Abstract]
- Res Sq. 2026 May 18.
- SSRN. 2026 Apr 1.
- bioRxiv. 2025 Sep 10:2025.09.05.673576. [Abstract]
- bioRxiv. 2025 Sep 24.
- University of Greifswald. 2025.
- bioRxiv. 2025 Jul 31.
- SSRN. 2025 Jul 30.
- bioRxiv. 2025 Jul 29.
- bioRxiv. 2025 April 12.
- bioRxiv. 2025 February 21.
- bioRxiv. 2024 Jul 7:2024.07.04.601620. [Abstract]
- Res Sq. 2024 Jul 16.
- bioRxiv. 2024 Jul 12:2024.07.11.603146. [Abstract]
- Karolinska Institutet. 2024 May 31.
- Research Square Preprint. 2024 Mar 21.
- Chemrxiv. 2023 Aug 3.
- Chemrxiv. Aug 11, 2021.
- Research Square Preprint. 2020 Dec 11:rs.3.rs-119695. [Abstract]
- bioRxiv. 2020 Nov 6:2020.10.04.325415. [Abstract]
- bioRxiv. 2020 Jun.
- bioRxiv. 2020 Mar.
- University of Toyama. 2018, Nov.
- bioRxiv. 2018 Feb.
Customer Validation & Images
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Biologische Aktivität
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JAK2 5.7 nM (IC50) |
JAK1 5.9 nM (IC50) |
Tyk2 53 nM (IC50) |
JAK3 560 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Calvarial osteoblast | CC50 |
>50 μM
Compound: 29
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Cytotoxicity against osteoblast cells (unknown origin)
Cytotoxicity against osteoblast cells (unknown origin)
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[PMID: 33539089] |
| PBMC | IC50 |
40 nM
Compound: 3
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Inhibition of IL-6 induced MCP-1 production in human PBMC cells preincubated with compound for 10 mins followed by IL-6 stimulation and measured after 48 hrs by ELISA analysis
Inhibition of IL-6 induced MCP-1 production in human PBMC cells preincubated with compound for 10 mins followed by IL-6 stimulation and measured after 48 hrs by ELISA analysis
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[PMID: 32120325] |
| T-cell | IC50 |
234 nM
Compound: INCB028050
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Inhibition of JAK1 in human whole blood assessed as reduction in IL6-induced STAT1 phosphorylation in CD4+ T cells preincubated with compound for 30 mins followed by IL-6 addition and measured after 20 mins by flow cytometry analysis
Inhibition of JAK1 in human whole blood assessed as reduction in IL6-induced STAT1 phosphorylation in CD4+ T cells preincubated with compound for 30 mins followed by IL-6 addition and measured after 20 mins by flow cytometry analysis
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[PMID: 24006460] |
| T-cell | IC50 |
63.8 nM
Compound: INCB028050
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Inhibition of JAK2 in human whole blood assessed as reduction in GM-CSF-induced STAT5 phosphorylation in CD3-positive T cell preincubated with compound for 30 mins followed by GM-CSF addition and measured after 20 mins by flow cytometry analysis
Inhibition of JAK2 in human whole blood assessed as reduction in GM-CSF-induced STAT5 phosphorylation in CD3-positive T cell preincubated with compound for 30 mins followed by GM-CSF addition and measured after 20 mins by flow cytometry analysis
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[PMID: 24006460] |
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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1187594-09-7
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Appearance Solid
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Molecular Weight 371.42
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Formel C16H17N7O2S
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Color White to off-white
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SMILES
N#CCC1(N2N=CC(C3=C4C(NC=C4)=NC=N3)=C2)CN(S(=O)(CC)=O)C1
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Synonyms
LY3009104; INCB028050
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (78)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]2025 Dec 15;10(1):406. PMID: 41392286 -
Signal Transduct Target Ther
An integrative drug repositioning framework discovered a potential therapeutic agent targeting COVID-19. [Abstract]2021 Apr 24;6(1):165. PMID: 33895786 -
Science
2017 Dec 1;358(6367):eaan4368. PMID: 29191878 -
Cell
2021 Apr 15;184(8):2167-2182.e22. PMID: 33811809 -
Drug Resist Updat
DTX2 attenuates Lenvatinib-induced ferroptosis by suppressing docosahexaenoic acid biosynthesis through HSD17B4-dependent peroxisomal β-oxidation in hepatocellular carcinoma. [Abstract]2025 Jul:81:101224. PMID: 40058099 -
Ann Rheum Dis
Augmentation of immunothrombosis as a key mechanism underlying JAK inhibition associated hypercoagulability in rheumatoid arthritis. [Abstract]2025 Sep 25:S0003-4967(25)04383-3. PMID: 41006174 -
Cancer Res
2021 Dec 15;81(24):6131-6141. PMID: 34728538 -
Sci Immunol
2024 Jul 12;9(97):eadn0178. PMID: 38996010 -
ACS Nano
Coassembly Nanomedicine Mediated by Intermolecular Interactions Between Methotrexate and Baricitinib for Improved Rheumatoid Arthritis Treatment. [Abstract]2024 Mar 19;18(11):8337-8349. PMID: 38437640 -
Nat Commun
TMEM25 inhibits monomeric EGFR-mediated STAT3 activation in basal state to suppress triple-negative breast cancer progression. [Abstract]2023 Apr 24;14(1):2342. PMID: 37095176 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Adv Sci (Weinh)
Targeted SPP1 Inhibition of Tumor-Associated Myeloid Cells Effectively Decreases Tumor Sizes. [Abstract]2024 Dec 5:e2410360. PMID: 39639496 -
Adv Sci (Weinh)
CD63+ Cancer-Associated Fibroblasts Confer Tamoxifen Resistance to Breast Cancer Cells through Exosomal miR-22. [Abstract]2020 Sep 24;7(21):2002518. PMID: 33173749 -
J Clin Invest
Viral infection induces inflammatory signals that coordinate YAP regulation of dysplastic cells in lung alveoli. [Abstract]2024 Oct 1;134(19):e176828. PMID: 39352385 -
J Clin Invest
Antibody-drug conjugates plus Janus kinase inhibitors enable MHC-mismatched allogeneic hematopoietic stem cell transplantation. [Abstract]2021 Dec 15;131(24):e145501. PMID: 34730109 -
Sci Adv
2024 Mar 22;10(12):eadl0368. PMID: 38507500 -
J Allergy Clin Immunol
Recapitulating primary immunodeficiencies with expanded potential stem cells: proof-of-concept with STAT1 gain-of-function. [Abstract]2024 Apr;153(4):1125-1139. PMID: 38072195 -
J Immunother Cancer
Memory B cell subset shapes antitumor immunity and response to PD-1 blockade in mismatch repair-deficient colorectal cancers. [Abstract]2026 Jan 8;14(1):e012121. PMID: 41506788 -
J Immunother Cancer
Combinatorial treatment with upadacitinib abrogates systemic toxicity of a tumor-targeted IL-2 fusion protein. [Abstract]2025 May 11;13(5):e010831. PMID: 40350206 -
J Exp Med
2024 Mar 4;221(3):e20230683. PMID: 38324068 -
Diabetologia
2024 Jan;67(1):124-136. PMID: 37924378 -
Cell Death Dis
IFNγ augments TKI efficacy by alleviating protein unfolding stress to promote GSDME-mediated pyroptosis in hepatocellular carcinoma. [Abstract]2025 Jul 11;16(1):512. PMID: 40645933 -
Proc Natl Acad Sci U S A
Stress granule-mediated ZBP1 activation drives necroptotic cell death in non-obstructive azoospermia and testicular aging. [Abstract]2025 Aug 19;122(33):e2514837122. PMID: 40811463 -
Acta Pharmacol Sin
Activation of unfolded protein response overcomes Ibrutinib resistance in diffuse large B-cell lymphoma. [Abstract]2021 May;42(5):814-823. PMID: 32855532 -
Phytomedicine
Diosgenin ameliorates colitis by inhibiting mitochondrial DNA synthesis in macrophages via STAT2-CMPK2 pathway. [Abstract]2025 Nov 25:150:157605. PMID: 41351988 -
Br J Pharmacol
A novel inhibitor of class IIa histone deacetylases attenuates collagen-induced arthritis. [Abstract]2024 Dec;181(23):4804-4821. PMID: 39223784 -
Mol Syst Biol
Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]2024 Jan;20(1):28-55. PMID: 38177929 -
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Aging Cell
Baricitinib Augments Lonafarnib Therapy to Preserve Colonic Homeostasis and Microbial Balance in a Mouse Model of Progeria. [Abstract]2025 Oct 20:e70273. PMID: 41114526 -
J Autoimmun
Enhanced type I interferon signature induces neutrophil extracellular traps enriched in mitochondrial DNA in adult-onset Still's disease. [Abstract]2022 Feb;127:102793. PMID: 35123211 -
JCI Insight
An oral lichen planus-like mouse model driven by IFN-γ signaling and cytotoxic CD8+ T cells. [Abstract]2025 Dec 11:e185380. PMID: 41379548 -
Mol Ther Nucleic Acids
Inhibition of IFNAR-JAK signaling enhances tolerability and transgene expression of systemic non-viral DNA delivery. [Abstract]2025 Mar 5;36(2):102502. PMID: 40206655 -
J Ethnopharmacol
Cedrol from Platycladus orientalis (L.) Franco regulates M1/M2 polarization of macrophages and promotes hair regeneration. [Abstract]2026 Apr 24:361:121268. PMID: 41611183 -
Commun Biol
JAK inhibitors dampen activation of interferon-stimulated transcription of ACE2 isoforms in human airway epithelial cells. [Abstract]2021 Jun 2;4(1):654. PMID: 34079039 -
Inflammation
Inhibition of JAK-STAT Signaling by Baricitinib Reduces Interferon-γ-Induced CXCL10 Production in Human Salivary Gland Ductal Cells. [Abstract]2021 Feb;44(1):206-216. PMID: 32772240 -
Int J Mol Sci
Effect of the JAK Inhibitor Baricitinib on Cytokine Production and Bone Properties in a Mouse Model of Accelerated Aging. [Abstract]2026 Jun 3;27(11):5047. PMID: 42278571 -
Int J Mol Sci
Baricitinib and Lonafarnib Synergistically Target Progerin and Inflammation, Improving Lifespan and Health in Progeria Mice. [Abstract]2025 May 19;26(10):4849. PMID: 40429989 -
Int Immunopharmacol
Baricitinib alleviates myositis-associated interstitial lung disease in mice by inhibiting the NETs-cGAS-STING-EMT axis. [Abstract]2026 Feb 15:171:116137. PMID: 41481958 -
Int Immunopharmacol
Baricitinib alleviates cardiac fibrosis and inflammation induced by chronic sympathetic activation. [Abstract]2024 Aug 9:140:112894. PMID: 39126736 -
Eur J Pharm Sci
Exploring the interactions of JAK inhibitor and S1P receptor modulator drugs with the human gut microbiome: Implications for colonic drug delivery and inflammatory bowel disease. [Abstract]2024 Jul 4:106845. PMID: 38971433 -
Int Immunopharmacol
Effect of Baricitinib on the epithelial-mesenchymal transition of alveolar epithelial cells induced by IL-6. [Abstract]2022 Sep:110:109044. PMID: 35850052 -
RSC Adv
Lac water extract inhibits IFN-γ signaling through JAK2-STAT1-IRF1 axis in human melanoma. [Abstract]2018 Jun 13;8(38):21534-21540. PMID: 35539920
Baricitinib purchased from MedChemExpress. Usage Cited in: RSC Adv. 2018 Jun 13;8(38):21534-21540. [Abstract]
M14 and A2058 cells are treated with IFN-γ (10 ng/mL) after Lac (100 μg/mL) or baricitinib (0.5 μM) for the indicated times. Whole cell lysates are subjected to western blotting.
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Rheumatology (Oxford)
Inhibitory effect of baricitinib on microglia and STAT3 in a region with a weak blood-brain barrier in a mouse model of rheumatoid arthritis. [Abstract]2023 Aug 1;62(8):2908-2917. PMID: 36648313 -
Toxicol Sci
Lead Impairs the Development of Innate Lymphoid Cells by Impeding the Differentiation of Their Progenitors. [Abstract]2020 Aug 1;176(2):410-422. PMID: 32428222 -
J Dermatol Sci
Type 2 cytokine-JAK1 signaling is involved in the development of dry skin-induced mechanical alloknesis. [Abstract]2025 Mar;117(3):52-60. PMID: 39616021 -
J Biol Chem
The stress-activated kinase p38 mediates non-canonical activation of Src and tyrosine phosphorylation of the adapter protein TAB1. [Abstract]2026 Jan 23;302(3):111200. PMID: 41581886 -
Sci Rep
Identification of novel off targets of baricitinib and tofacitinib by machine learning with a focus on thrombosis and viral infection. [Abstract]2022 May 12;12(1):7843. PMID: 35551258 -
Pharmacol Rep
Effect of 28 days treatment of baricitinib on mechanical allodynia, osteopenia, and loss of nerve fibers in an experimental model of type-1 diabetes mellitus. [Abstract]2024 Oct;76(5):1079-1088. PMID: 39155357 -
Int J Obes (Lond)
Intermuscular and perimuscular fat expansion in obesity correlates with skeletal muscle T cell and macrophage infiltration and insulin resistance. [Abstract]2015 Nov;39(11):1607-18. PMID: 26041698 -
Heliyon
Fungal metabolite (+)-terrein suppresses IL-6/sIL-6R-induced CSF1 secretion by inhibiting JAK1 phosphorylation in human gingival fibroblasts. [Abstract]2018 Nov 26;4(11):e00979. PMID: 30519664 -
J Immunol
Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases. [Abstract]2013 Oct 1;191(7):3568-77. PMID: 24006460 -
Immunol Res
Immunomodulatory activity of 4-(Benzyloxy)phenol facilitates intracellular mycobacterial clearance through p53 mediated IL-35 signaling dependent JAK1/STAT3 pathway in human macrophages. [Abstract]2025 Jun 26;73(1):99. PMID: 40571857 -
Platelets
Janus kinase inhibitors ruxolitinib and baricitinib impair glycoprotein-VI mediated platelet function. [Abstract]2022 Apr 3;33(3):404-415. PMID: 34097573 -
PLoS One
A Jak1/2 inhibitor, baricitinib, inhibits osteoclastogenesis by suppressing RANKL expression in osteoblasts in vitro. [Abstract]2017 Jul 14;12(7):e0181126. PMID: 28708884
Baricitinib purchased from MedChemExpress. Usage Cited in: PLoS One. 2017 Jul 14;12(7):e0181126. [Abstract]
An activator of Stat3, colivelin (0.1 or 1 µM), rescued Baricitinib-induced RANKL down-regulation in osteoblast cultures.
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Biomed Chromatogr
Assessment of Apalutamide Metabolic Stability in HLMs Matrix Using a Sensitive and Fast UPLC-MS/MS Method: In Silico Screening for Toxicity Alerts and Metabolic Lability. [Abstract]2026 Mar;40(3):e70376. PMID: 41582395 -
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bioRxiv
Curing autoimmune diabetes with islet and hematopoietic cell transplantation after CD117 antibody-based conditioning. [Abstract]2025 Sep 10:2025.09.05.673576. PMID: 40964321 -
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bioRxiv
Rebalancing Viral and Immune Damage versus Tissue Repair Prevents Death from Lethal Influenza Infection. [Abstract]2024 Jul 7:2024.07.04.601620. PMID: 39372755 -
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bioRxiv
Seasonal influenza A virus lineages exhibit divergent abilities to antagonize interferon induction and signaling. [Abstract]2024 Jul 12:2024.07.11.603146. PMID: 39026731 -
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Research Square Preprint
Activation of Interferon-Stimulated Transcriptomes and ACE2 Isoforms in Human Airway Epithelium Is Curbed by Janus Kinase Inhibitors. [Abstract]2020 Dec 11:rs.3.rs-119695. PMID: 33330857 -
bioRxiv
2020 Nov 6:2020.10.04.325415. PMID: 33052350 -
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Baricitinib purchased from MedChemExpress. Usage Cited in: University of Toyama. 2018, Nov.
Western analysis of pJAK2, JAK2, pSTAT1, STAT1 and IRF1 protein in M14 and A2058 cells treated with IFN-g (10 ng/mL) after Lac (100 μg/mL) or baricitinib (0.5 μM) for the indicated times.
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Lösungsmittel & Löslichkeit
DMSO : 25 mg/mL (67.31 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.73 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.73 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 0.5% Methylcellulose/saline water
Solubility: 2.5 mg/mL (6.73 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
For the determination of IL-6-induced MCP-1 production, PBMCs are plated at 3.3×105 cells per well in RPMI 1640+10% FCS in the presence or absence of various concentrations of INCB028050 (1 nM, 10 nM, 100 nM, 1 μM, and 10 μM). Following preincubation with compound for 10 min at room temperature, cells are stimulated by adding 10 ng/mL human recombinant IL-6 to each well. Cells are incubated for 48 h at 37°C, 5% CO2. Supernatants are harvested and analyzed by ELISA for levels of human MCP-1. The ability of INCB028050 to inhibit IL-6-induced secretion of MCP-1 is reported as the concentration required for 50% inhibition (IC50). Proliferation of Ba/F3-TEL-JAK3 cells is performed over 3 d using Cell-Titer Glo[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats[1]
Female rats (n=6 per gender per group) are given a dose of 10 mg/kg Baricitinib and given by oral gavage at 10 mL/kg. The first three rats are bled at 0 (predose), 2, 8, and 24 h, and the second three rats are bled 1, 4, and 12 h after dosing. EDTA is used as the anticoagulant, and samples are centrifuged to obtain plasma. An analytical method for the quantification of INCB028050 has been developed and used to analyze samples from toxicology studies. The method combines a protein precipitation extraction with 10% methanol in acetonitrile and LC/MS/MS analysis. The method has demonstrated a linear assay range 1-5000 nM using 0.1 mL of study samples. Data are processed using Analyst 1.3.1. A standard curve is determined from peak area ratio versus concentration using a weighted linear regression (1/x2).
Mice[2]
The C3H/HeJ graft-recipient mouse model of AA is used for these experiments. Briefly, alopecic skin from a C3H/HeJ mouse that spontaneously developed hair loss is grafted onto 8-10 week old C3H/HeJ mice free of disease. At the time of grafting, an osmotic pump that administered approximately 0.7 mg/day of Baricitinib or placebo is implanted. Osmotic pumps are changed monthly. A time-to-event survival analysis for interval censored data is performed. The survival and interval packages in R are used to perform log-rank tests. The hypothesis that the survival distributions are equal in the (n=10) Baricitinib-treated mice and (n=10) placebo-treated mice is rejected at the 5% level using Sun's score to perform an exact log-rank two-sample test with the p-value of 0.0035.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (286 KB)
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SDS (557 KB)
- English - EN (557 KB)
- Français - FR (557 KB)
- Deutsch - DE (557 KB)
- Norwegian - NO (557 KB)
- Español - ES (557 KB)
- Swedish - SV (557 KB)
- Italian - IT (557 KB)
- Portuguese - PT (557 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. 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. [Content Brief]
[2]. Jabbari A, et al. Reversal of Alopecia Areata Following Treatment With the JAK1/2 Inhibitor Baricitinib. EBioMedicine. 2015 Feb 26;2(4):351-5. [Content Brief]
[3]. Khan IM, et al. Intermuscular and perimuscular fat expansion in obesity correlates with skeletal muscle T cell and macrophage infiltration resistance. Int J Obes (Lond). 2015 Nov;39(11):1607-18. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6924 mL | 13.4618 mL | 26.9237 mL | 67.3092 mL |
| 5 mM | 0.5385 mL | 2.6924 mL | 5.3847 mL | 13.4618 mL | |
| 10 mM | 0.2692 mL | 1.3462 mL | 2.6924 mL | 6.7309 mL | |
| 15 mM | 0.1795 mL | 0.8975 mL | 1.7949 mL | 4.4873 mL | |
| 20 mM | 0.1346 mL | 0.6731 mL | 1.3462 mL | 3.3655 mL | |
| 25 mM | 0.1077 mL | 0.5385 mL | 1.0769 mL | 2.6924 mL | |
| 30 mM | 0.0897 mL | 0.4487 mL | 0.8975 mL | 2.2436 mL | |
| 40 mM | 0.0673 mL | 0.3365 mL | 0.6731 mL | 1.6827 mL | |
| 50 mM | 0.0538 mL | 0.2692 mL | 0.5385 mL | 1.3462 mL | |
| 60 mM | 0.0449 mL | 0.2244 mL | 0.4487 mL | 1.1218 mL |
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