Baricitinib

別名：INCB028050, LY3009104

製品コード：S2851 純度：99.96%

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.

CAS No. 1187594-09-7

サイズ	価格(税別)	在庫状況
5mg	JPY 40500	国内在庫あり
50mg	JPY 118500	国内在庫なし(納期7~10日)
200mg	JPY 190500	国内在庫あり
1g	JPY 295500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（57）

製品安全説明書

現在のバッチを見る：純度： 99.96%

99.96

Baricitinib関連製品

関連ターゲット	JAK1 JAK2 JAK3 Tyk2	もっと見る
関連製品	AZD1480 WP1066 Momelotinib (CYT387) Filgotinib (GLPG0634) AT9283 Gandotinib (LY2784544) TG101209 Cerdulatinib (PRT062070) hydrochloride Pacritinib NVP-BSK805 2HCl WHI-P154 FLLL32 Decernotinib (VX-509) CEP-33779 AZ 960 Cerdulatinib (PRT062070) ZM 39923 HCl XL019 BMS-911543 Curcumol Solcitinib Oclacitinib maleate Pyridone 6 Creatine Ritlecitinib (PF-06651600) Deucravacitinib (BMS-986165) Itacitinib (INCB39110) Peficitinib BD750 WHI-P97 JANEX-1 Brevilin A 1,2,3,4,5,6-Hexabromocyclohexane Brepocitinib (PF-06700841) FM-381 SAR-20347 Selective JAK3 inhibitor 1	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library FDA-approved Drug Library Natural Product Library Tyrosine Kinase Inhibitor Library JAK/STAT compound library	もっと見る

シグナル伝達経路

JAKシグナル伝達経路

JAK阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
HeLa	Function assay	5 uM	2 hrs	Inhibition of IFNgamma-induced JAK2 phosphorylation in human HeLa cells at 5 uM incubated for 2 hrs by Western blot method	27137359
human CD34+ cells	Function assay		45 mins	Inhibition of JAK2 homodimer in human CD34+ cells spiked into human whole blood assessed as inhibition of EPO-induced STAT-5 phosphorylation preincubated for 45 mins followed by EPO addition measured after 15 mins by FACS analysis, IC50=0.0878μM	24417533
CD34+	Function assay		45 mins	Inhibition of JAK2 homodimer in human CD34+ cells spiked into human whole blood assessed as inhibition of EPO-induced STAT-5 phosphorylation preincubated for 45 mins followed by EPO addition measured after 15 mins by FACS analysis, IC50 = 0.0878 μM.	24417533
human UT7 cells	Function assay			Inhibition of JAK2 in human UT7 cells assessed as suppression of EPO-stimulated STAT5 phosphorylation by AlphaScreen assay	26372653
human TF1 cells	Function assay			Inhibition of JAK1 in human TF1 cells assessed as suppression of IL6-stimulated STAT3 phosphorylation by AlphaScreen assay	26372653
TF1	Function assay			Inhibition of JAK1 in human TF1 cells assessed as suppression of IL6-stimulated STAT3 phosphorylation by AlphaScreen assay, INH = 0.017 μM.	26372653
UT7	Function assay			Inhibition of JAK2 in human UT7 cells assessed as suppression of EPO-stimulated STAT5 phosphorylation by AlphaScreen assay, INH = 0.31 μM.	26372653
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
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生物活性

製品説明

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
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]
Kinase Assay	Biochemical assays
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.
実験結果図	Methods	Biomarkers	結果図	PMID
実験結果図	Western blot	phSTAT1 / phSTAT3		28369741

In Vivo
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]
動物実験	動物モデル	Collagen-induced arthritis (CIA) mice
	投与量	10 mg/mL
	投与経路	orally

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05914584	Not yet recruiting	Hospital-acquired Pneumonia	Nantes University Hospital	July 1 2023	Phase 2\|Phase 3
NCT05189106	Recruiting	Amyotrophic Lateral Sclerosis\|Alzheimer Disease\|Mild Cognitive Impairment	Massachusetts General Hospital	December 5 2022	Phase 1\|Phase 2
NCT05074420	Recruiting	Covid19\|Corona Virus Infection	Eli Lilly and Company	December 21 2021	Phase 3
NCT04208464	Completed	Idiopathic Inflammatory Myopathies	University of Manchester\|Eli Lilly and Company\|Clinical Trials Unit Manchester\|Karolinska Institutet	October 7 2021	Phase 2
NCT04358614	Completed	COVID\|Pneumonia	Fabrizio Cantini\|Hospital of Prato	March 16 2020	Phase 2\|Phase 3

参考
[1] Fridman JS, et al. J Immunol, 2010, 184(9), 5298-5307. [2] Kontzias A, et al. Curr Opin Pharmacol, 2012, 12(4), 464-470. [3] Norman P, et al. Expert Opin Ther Pat, 2012, 22(10), 1233-1249. [4] Norman P, et al. Expert Opin Ther Pat, 2012, 22(9), 1105-1109. + 展開

参考

[4] Norman P, et al. Expert Opin Ther Pat, 2012, 22(9), 1105-1109.

+ 展開

化学情報

分子量	371.42	化学式	C₁₆H₁₇N₇O₂S
CAS No.	1187594-09-7	SDF	Download Baricitinib SDFをダウンロードする
Smiles	CCS(=O)(=O)N1CC(C1)(CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 74 mg/mL ( (199.23 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(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）μL 動物数匹

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

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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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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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):