Baricitinib (LY3009104)

製品コードS2851 バッチS285104

印刷

化学情報

Synonyms

INCB028050, LY3009104

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₆H₁₇N₇O₂S

分子量

371.42

CAS No.

1187594-09-7

Solubility (25°C)*

体外

DMSO

74 mg/mL (199.23 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG 300 2 5%Tween80 3 50% ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	2.500mg/ml (6.73mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/mL clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify; add 50 μL Tween-80 to the above system, mix evenly to clarify; Then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Baricitinib 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.
in vitro	Baricitinib (LY3009104) 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. It also inhibits pSTAT3 stimulated by IL-23 with IC50 of 20 nM in isolated naive T-cells. ^[1]
in vivo	Baricitinib (LY3009104) inhibits IL-6–stimulated phosphorylation of STAT3 in whole blood with an IC50 of 128 nM. This compound (10 mg/kg p.o.) is expected to inhibit JAK1/2 signaling (by ≥50%) in rats for about 8 hours. It (10 mg/mL, p.o.) inhibits disease scores in dose-dependent manner in rats with established disease in the adjuvant arthritis model. This 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. The compound, 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. It 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. This chemical (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. It reduces levels of pSTAT3 in a dose- and time-dependent manner in the peripheral blood of rAIA animals. This agent (10 mg/mL, p.o.) improves a composite score of joint damage by 47% in the murine CIA model. It (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. The compound (10 mg/kg) inhibits the delayed-type hypersensitivity response by 48% in both the CIA and CAIA models. ^[1] It is efficacious in active rheumatoid arthritis patients refractory to disease modifying drugs and biologics. ^[2] This compound 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 it only moderately affect the ACR20 values in Phase IIa clinical studies. ^[3] It has the dose-limiting side-effect of inducing anaemia which has been attributed to its effects on JAK2 but has clearly shown efficacy. ^[4]

製品説明

Baricitinib 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.

in vitro

Baricitinib (LY3009104) 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. It also inhibits pSTAT3 stimulated by IL-23 with IC50 of 20 nM in isolated naive T-cells. ^[1]

in vivo

Baricitinib (LY3009104) inhibits IL-6–stimulated phosphorylation of STAT3 in whole blood with an IC50 of 128 nM. This compound (10 mg/kg p.o.) is expected to inhibit JAK1/2 signaling (by ≥50%) in rats for about 8 hours. It (10 mg/mL, p.o.) inhibits disease scores in dose-dependent manner in rats with established disease in the adjuvant arthritis model. This 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. The compound, 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. It 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. This chemical (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. It reduces levels of pSTAT3 in a dose- and time-dependent manner in the peripheral blood of rAIA animals. This agent (10 mg/mL, p.o.) improves a composite score of joint damage by 47% in the murine CIA model. It (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. The compound (10 mg/kg) inhibits the delayed-type hypersensitivity response by 48% in both the CIA and CAIA models. ^[1]

It is efficacious in active rheumatoid arthritis patients refractory to disease modifying drugs and biologics. ^[2]

This compound 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 it only moderately affect the ACR20 values in Phase IIa clinical studies. ^[3]

It has the dose-limiting side-effect of inducing anaemia which has been attributed to its effects on JAK2 but has clearly shown efficacy. ^[4]

プロトコル(参考用のみ)

キナーゼアッセイ	Biochemical assays
キナーゼアッセイ	Baricitinib (LY3009104) is evaluated 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 this 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 concentration of it required for inhibition of 50% of the fluorescent signal.
細胞アッセイ	細胞株	PBMCs
	濃度	5.9 nM (JAK1) and 5.7 nM (JAK2)
	反応時間
	実験の流れ	Cells were treated with indicated concentrations of Baricitinib (LY3009104).
動物実験	動物モデル	Collagen-induced arthritis (CIA) mice
	投薬量	10 mg/mL
	投与方法	orally

参考

https://pubmed.ncbi.nlm.nih.gov/20363976/
https://pubmed.ncbi.nlm.nih.gov/22819198/
https://pubmed.ncbi.nlm.nih.gov/22971156/

https://pubmed.ncbi.nlm.nih.gov/22812580/

+ 展开

カスタマーフィードバック

: , , Nat Cell Biol,2014, 17(1):57-67

: Data from [Data independently produced by , , Br J Haematol, 2017, 177(2):271-282]

: Data from [Data independently produced by , , J Physiol, 2015, 593(24):5269-82]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

T-bet+ CXCR3+ B cells drive hyperreactive B-T cell interactions in multiple sclerosis [ Cell Rep Med, 2025, 6(3):102027]	PubMed: 40107244
The pro-inflammatory cytokine IL6 suppresses mitochondrial function via the gp130-JAK1/STAT1/3-HIF1α/ERRα axis [ Cell Rep, 2025, 44(3):115403]	PubMed: 40056415
A STAT3/integrin axis accelerates pancreatic cancer initiation and progression [ Cell Rep, 2025, S2211-1247(25)00781-8]	PubMed: 40701148
Identification of Dinaciclib and Ganetespib as anti-inflammatory drugs using a novel HTP screening assay that targets IFNγ-dependent PD-L1 [ Front Immunol, 2025, 16:1502094]	PubMed: 40264756
Polarization of Vδ2 T cells to a Th2-like phenotype promotes plasmablast differentiation and possesses pro-fibrotic properties in IgG4-related disease [ Front Immunol, 2025, 16:1550405]	PubMed: 40213561
Pharmacological evaluation of drug therapies in Aicardi-Goutières syndrome: insights from patient-derived neural stem cells [ Front Pharmacol, 2025, 16:1549183]	PubMed: 40183101
Targeting interferon responses in juvenile dermatomyositis: Siglec-1 as an in vitro biomarker for JAK inhibitor efficacy [ Rheumatology (Oxford), 2025, keaf227]	PubMed: 40372702
Increased IFN responses drive myeloid cell activation in people living with HIV-1 [ Sci Rep, 2025, 15(1):20627]	PubMed: 40594068
The type 1 diabetes candidate genes PTPN2 and BACH2 regulate novel IFN-α-induced crosstalk between the JAK/STAT and MAPKs pathways in human beta cells [ Res Sq, 2025, rs.3.rs-6079043]	PubMed: 40162226
Proinflammatory transcriptomic and kinomic alterations in astrocytes derived from patients with familial Alzheimer's disease [ Brain Behav Immun Health, 2025, 47:101044]	PubMed: 40656638

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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