Baricitinib phosphate NEW
| Price | $40 | $57 | $94 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: Baricitinib phosphate | CAS No.: 1187595-84-1 |
| Purity: 99.68% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | Baricitinib phosphate |
| Description | Baricitinib phosphate (INCB028050) is a selective orally bioavailable JAK1/JAK2 inhibitor. |
| Cell Research | Baricitinib(INCB 028050) is dissolved in stock solutions, and then diluted with appropriate media before use[1]. Human PBMCs are isolated by leukapheresis followed by Ficoll-Hypaque centrifugation. 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]. |
| Kinase Assay | Enzyme assays are performed using a homogeneous time-resolved fluorescence assay with recombinant epitope tagged kinase domains (JAK1, 837-1142; JAK2, 828-1132; JAK3, 718-1124; Tyk2, 873-1187) or full-length enzyme (cMET and Chk2) and peptide substrate. Each enzyme reaction is performed with or without test compound (11-point dilution), JAK, cMET, or Chk2 enzyme, 500 nM (100 nM for Chk2) peptide, ATP (at the Km specific for each kinase or 1 mM), and 2.0% DMSO in assay buffer. The calculated IC50 value is the compound concentration required for inhibition of 50% of the fluorescent signal. Additional kinase assays are performed at Cerep using standard conditions at 200 nM. Enzymes tested included: Abl, Akt1, AurA, AurB, CDC2, CDK2, CDK4, CHK2, c-kit, EGFR, EphB4, ERK1, ERK2, FLT-1, HER2, IGF1R, IKKα, IKKβ, JNK1, Lck, MEK1, p38α, p70S6K, PKA, PKCα, Src, and ZAP70[1]. |
| In vitro | Baricitinib (INCB028050) effectively inhibits JAK signaling and function in various cell-based assays, showcasing its potent anti-inflammatory properties. In Peripheral Blood Mononuclear Cells (PBMCs), it impedes IL-6-induced phosphorylation of STAT3 (pSTAT3) and reduces MCP-1 chemokine production, with half-maximal inhibitory concentrations (IC50) of 44 nM and 40 nM, respectively. Further, in naive T-cells, Baricitinib blocks pSTAT3 activation by IL-23 with an IC50 of 20 nM, crucially preventing the release of inflammatory cytokines IL-17 and IL-22 from Th17 cells, at an IC50 of 50 nM. Unlike Baricitinib, the structurally similar JAK1/2 inhibitors INCB027753 and INCB029843 show no significant activity in these assays even at concentrations up to 10 μM[1]. |
| In vivo | Baricitinib (INCB028050) treatment significantly reduces hind paw swelling in comparison to the vehicle control, achieving a 50% reduction at a dosage of 1 mg/kg and over 95% reduction at dosages of 3 or 10 mg/kg over a two-week period. This is noteworthy because paw volume measurements commence on day 0 of treatment in animals already exhibiting considerable disease symptoms, enabling observations of over 100% inhibition in cases where animals demonstrate significant swelling reductions. Furthermore, at a daily dose of 0.7 mg, Baricitinib-treated mice show markedly decreased inflammation, as evidenced by H&E staining, alongside reduced CD8 infiltration, and lowered MHC class I and II expression relative to vehicle-control treated mice. Additionally, the presence of CD8+NKG2D+ cells, pivotal in the progression of both murine and human alopecia areata (AA), is substantially reduced in Baricitinib-treated mice when compared to those treated with the vehicle control. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 50 mg/mL (106.52 mM) |
| Keywords | LY-3009104 | inhibit | INCB-028050 Phosphate | Janus kinase | JAK | Baricitinib phosphate | Baricitinib | LY 3009104 Phosphate | INCB-028050 | LY-3009104 Phosphate | Inhibitor | LY 3009104 | Baricitinib Phosphate | INCB 028050 Phosphate | INCB028050 Phosphate | LY3009104 Phosphate | INCB 028050 |
| Inhibitors Related | Delgocitinib | Deucravacitinib | Ruxolitinib | Ibrutinib | Ruxolitinib phosphate | JAK-IN-10 | Gefitinib |
| Related Compound Libraries | Bioactive Compound Library | Kinase Inhibitor Library | EMA Approved Drug Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Viral Compound Library | Drug Repurposing Compound Library | Inhibitor Library | FDA-Approved Kinase Inhibitor Library | Bioactive Compounds Library Max |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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