Baricitinib (INCB028050)

For research use only. Not for use in humans.

製品コードS2851 別名:LY3009104

Baricitinib (INCB028050)化学構造

分子量(MW):371.42

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.

サイズ 価格(税別) 在庫  
JPY 46800 あり
JPY 63400 あり
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バルク問合せ

カスタマーフィードバック(4)

  • bDNA analysis showing that the JAK1/2 inhibitors CYT387, AZD1480 and Baricitinib positively regulate UCP1 expression in PSC-WA. Values are mean ± s.d. of n = three biological replicates and differences from DMSO are significant for * P < 0.005. P values were calculated using the two-tailed paired Student's t-test.

    Nat Cell Biol,2014, 17(1):57-67. Baricitinib (INCB028050) purchased from Selleck.

  • (A-C) Anti-proliferative activity of NDI-031301 (A), tofacitinib (B) or baricitinib (C) on transformed Ba/F3 cells. Ba/F3 cells transformed by TEL-ABL, TEL-JAK1, TEL-JAK2, TEL-JAK3, or TEL-TYK2 were cultured with graded concentrations of the indicated inhibitor for 72 h. Cell viability values are mean SD percentages of the untreated control value in triplicate experiments.

    Br J Haematol, 2017, 177(2):271-282. Baricitinib (INCB028050) purchased from Selleck.

  • HT‐29/B6‐GR/MR cells were stimulated with or without DBA and with or without IL‐13 in the presence or absence of baricitinib or AS1517499 for 96 h, then rested FCS and IL‐13 free for 3 h and treated again with IL‐13 for 30 min. Then, total cellular protein was extracted, fractionated by SDS‐Page, and immuno‐probed for phospho‐specific ERK1/2, JNK, p38, or STAT6 expression. Human β‐actin served as loading control.

    J Physiol, 2015, 593(24):5269-82. Baricitinib (INCB028050) purchased from Selleck.

  • JAK inhibitors work on “type 17” cytokine production in-vitro in Spondyloarthritis on established peripheral Th17 cells and on synovial fluid CD4+ T cells. (a) Reduction of IL-17A secretion by JAK inhibitors (Tofa, JAK3 > JAK1/2; Ruxo, JAK2 > JAK1; Bari, JAK1/2 > TYK2; CEP, JAK2) in AS CD4+ T cells (n = 6), primed under Th17-promoting conditions for 6 days, upon restimulation with anti-CD2/3/28 beads for 24 hours measured by ELISA. (b) Effects of JAK inhibitors on IL-17A secretion (ELISA) from synovial CD4+ T cells of SPA patients cultured for 3 days (n = 4, Bari n = 3). Statistical analysis: mean ± SEM, repeated measures 1-way ANOVA followed by Dunnett’s method for multiple comparisons. Bari:Baricitinib.

    Sci Rep, 2018, 8(1):15645. Baricitinib (INCB028050) purchased from Selleck.

製品安全説明書

JAK阻害剤の選択性比較

生物活性

製品説明 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.
ターゲット
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
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human CD34+ cells NGHwZYlHfW6ldHnvckBie3OjeR?= M1fHZ|Q2KG2rboO= NUGxZZp5UW6qaXLpeIlwdiCxZjDKRWszKGixbX;kbY1meiCrbjDoeY1idiCFREO0L{Bk\WyuczDzdIls\WRiaX70c{BpfW2jbjD3bI9t\SCkbH;v[EBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGVRVy2rbnT1Z4VlKFOWQWStOUBxcG:|cHjvdplt[XSrb36gdJJmcW6ldXLheIVlKG[xcjC0OUBucW6|IH\vcIxwf2WmIHL5JGVRVyCjZHTpeIlwdiCvZXHzeZJm\CCjZoTldkAyPSCvaX7zJIJ6KE[DQ2OgZY5idHm|aYOsJGlEPTB;MD6wPFc5|ryP MVmyOFQyPzV|Mx?=
human UT7 cells NHfuO|NHfW6ldHnvckBie3OjeR?= NU\pRY9oUW6qaXLpeIlwdiCxZjDKRWszKGmwIHj1cYFvKFWWNzDj[YxteyCjc4Pld5Nm\CCjczDzeZBxemW|c3nvckBw\iCHUF:td5RqdXWuYYTl[EBUXEGWNTDwbI9{eGixconsZZRqd25iYomgRYxxcGGVY4Ll[Y4h[XO|YYm= M2LRb|I3Ozd{NkWz
human TF1 cells MYnGeY5kfGmxbjDhd5NigQ>? NUjoepo{UW6qaXLpeIlwdiCxZjDKRWsyKGmwIHj1cYFvKFSIMTDj[YxteyCjc4Pld5Nm\CCjczDzeZBxemW|c3nvckBw\iCLTE[td5RqdXWuYYTl[EBUXEGWMzDwbI9{eGixconsZZRqd25iYomgRYxxcGGVY4Ll[Y4h[XO|YYm= MkLaNlY{PzJ4NUO=

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

アッセイ
Methods Test Index PMID
Western blot
phSTAT1 / phSTAT3 ; 

PubMed: 28369741     


Effect of Janus kinase (JAK) inhibition on phosphorylated signal transducer and activator of transcription (STAT) phosphorylation in RA neutrophils. Freshly isolated (0 h) RA neutrophils exhibited elevated levels of STAT-1 and STAT-3, which decreased during 60 min incubation in untreated conditions. Addition of baricitinib and tofacitinib (200 ng/ml) at 0 h induced a loss of phosphorylated STAT-1 and STAT-3 compared to untreated cells at 30 and 60 min.

28369741
体内試験 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]

お薦めの試験操作(参考用のみ)

動物試験:[1]
- 合併
  • 動物モデル: Collagen-induced arthritis (CIA) mice
  • 投薬量: 10 mg/mL
  • 投与方法: orally
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 74 mg/mL (199.23 mM)
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
混合させたのち直ちに使用することを推奨します。
5mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 371.42
化学式

C16H17N7O2S

CAS No. 1187594-09-7
Storage powder
in solvent
別名 LY3009104
Smiles CC[S](=O)(=O)N1CC(CC#N)(C1)[N]2C=C(C=N2)C3=NC=NC4=C3C=C[NH]4

投与溶媒組成計算器(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)
投与量 mg/kg 動物平均体重 g 投与体積(動物毎) ul 動物数
ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)
% DMSO % % Tween 80 % ddH2O
計算リセット

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04208464 Not yet recruiting Drug: Baricitinib Idiopathic Inflammatory Myopathies University of Manchester|Eli Lilly and Company|Manchester Clinical Trials Unit|Karolinska Institutet July 1 2020 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
NCT03952559 Recruiting Drug: Baricitinib|Drug: Placebo|Drug: Topical corticosteroid Atopic Dermatitis Eli Lilly and Company|Incyte Corporation May 24 2019 Phase 3
NCT03773978 Recruiting Drug: Baricitinib|Drug: Placebo Juvenile Idiopathic Arthritis Eli Lilly and Company December 17 2018 Phase 3

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問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?

  • 回答:

    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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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID