Resiquimod (R-848)

別名：S28463

製品コード：S8133 純度：99.98%

Resiquimod (R-848, S28463) is an immune response modifier that acts as a potent TLR 7/TLR 8 agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α. Resiquimod reduces hepatitis C virus (HCV) infection. Phase 2.

CAS No. 144875-48-9

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫なし(納期7~10日)
20mg	JPY 22000	国内在庫なし(納期7~10日)
50mg	JPY 40500	国内在庫あり
200mg	JPY 97000	国内在庫あり
1g	JPY 145500	国内在庫あり

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（16）

製品安全説明書

現在のバッチを見る：純度： 99.98%

99.98

Resiquimod (R-848)関連製品

関連ターゲット	TLR7 TLR8 TLR9 TLR4 TLR2 TLR3 TLR1 TLR6	もっと見る
関連製品	Resatorvid (TAK-242) Motolimod Cu-CPT22 Vesatolimod (GS-9620) TLR2-IN-C29 MD2-IN-1 Lipopolysaccharides IRAK4-IN-2 CU-T12-9 E6446 TLR4-IN-C34	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 Bioactive Compound Library-I Highly Selective Inhibitor Library	もっと見る

TLR阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
PBMC	Function assay	300 nM	18 hrs	Induction of type 1 IFN secretion in human PBMC at 300 nM after 18 hrs by ELISA, Activity=0.00726μM.	20232824
PBMC	Function assay	100 nM	18 hrs	Induction of type 1 IFN secretion in human PBMC at 100 nM after 18 hrs by ELISA, Activity=0.00561μM.	20232824
PBMC	Function assay	10 nM	18 hrs	Induction of type 1 IFN secretion in human PBMC at 10 nM after 18 hrs by ELISA, Activity<0.00125μM.	20232824
PBMC	Function assay	30 nM	18 hrs	Induction of type 1 IFN secretion in human PBMC at 30 nM after 18 hrs by ELISA, Activity=0.00125μM.	20232824
PBMC	Function assay	1000 nM	18 hrs	Induction of type 1 IFN secretion in human PBMC at 1000 nM after 18 hrs by ELISA, Activity=0.00775μM.	20232824
PBMC	Function assay	22.5 uM	24 hrs	Agonist activity at TLR7/TLR8 in human PBMC assessed as induction of TNF-alpha production at 22.5 uM after 24 hrs by flow cytometric analysis	24383475
PBMC	Immunomodulatory assay	16 uM	24 hrs	Immunomodulatory activity in human PBMC assessed as induction of IL-6 secretion at 16 uM after 24 hrs by ELISA	28254484
BMD	Function assay	1 uM	48 hrs	Induction of TLR7 receptor-mediated C57BL/6 mouse BMD cells activation assessed as upregulation of CD86 at 1 uM after 48 hrs by flow cytometry	19299126
BMD	Function assay	1 uM	48 hrs	Induction of TLR7 receptor-mediated C57BL/6 mouse BMD cells activation assessed as upregulation of MHC class-2 at 1 uM after 48 hrs by flow cytometry	19299126
BMD	Function assay	1 uM	48 hrs	Induction of TLR7 receptor-mediated C57BL/6 mouse BMD cells activation assessed as upregulation of CD40 at 1 uM after 48 hrs by flow cytometry	19299126
BMD	Function assay	5 uM	24 hrs	Induction of TLR7 receptor-mediated C57BL/6 mouse BMD cells activation assessed as IL12 production at 5 uM after 24 hrs by ELISA	19299126
Huh7	Antiviral assay		48 hrs	Antiviral activity against HCV infected human Huh7 replicon cells treated for 48 hrs with drug-induced mixed donor human PBMC supernatants assessed as viral levels by luciferase assay, EC50=0.024μM.	17548497
Huh7	Antiviral assay		48 hrs	Antiviral activity against HCV infected human Huh7 replicon cells treated for 48 hrs with drug-induced single donor human PBMC supernatants assessed as viral levels by luciferase assay, EC50=0.0265μM.	17548497
PBMC	Function assay		24 hrs	Induction of IFNalpha2a level in human PBMC assessed as drug level causing maximal cytokine induction after 24 hrs relative to control, Activity=0.1μM.	17548497
PBMC	Function assay		24 hrs	Toxic induction of IL1-beta level in human PBMC assessed as drug level causing maximal cytokine induction after 24 hrs relative to control, Activity=1μM.	17548497
PBMC	Function assay		24 hrs	Toxic induction of IL6 level in human PBMC assessed as drug level causing maximal cytokine induction after 24 hrs relative to control, Activity=1μM.	17548497
PBMC	Function assay		24 hrs	Toxic induction of TNFalpha level in human PBMC assessed as drug level causing maximal cytokine induction after 24 hrs relative to control, Activity=1μM.	17548497
HEK293	Function assay		6 hrs	Agonist activity at human TLR7 expressed in HEK293 cells after 6 hrs by NFkappaB-luciferase reporter gene assay, MEC=0.1μM.	30143425
HEK293	Function assay		6 hrs	Agonist activity at human TLR8 expressed in HEK293 cells after 6 hrs by NFkappaB-luciferase reporter gene assay, MEC=0.3μM.	30143425
HEK	Function assay		8 to 12 hrs	Agonist activity at human TLR7 expressed in HEK cells after 8 to 12 hrs by NFkappaB/SEAP reporter gene assay, EC50=1.34μM.	29152046
HEK	Function assay		24 hrs	Agonist activity at human TLR7 transfected in HEK cells assessed as NFkappaB induction after 24 hrs by specific secreted alkaline phosphatase gene assay, EC50=1.4μM.	22837811
HEK293	Function assay		24 hrs	Agonist activity at human TLR-7 expressed in HEK293 cells after 24 hrs by SEAP reporter gene assay, EC50=1.5μM.	24383475
HEK293	Function assay		6 hrs	Agonist activity at human TLR8 expressed in HEK293 cells incubated for 6 hrs by luciferase reporter gene assay, EC50=4μM.	27270029
HEK293	Function assay		24 hrs	Agonist activity at human TLR-8 expressed in HEK293 cells after 24 hrs by SEAP reporter gene assay, EC50=4.5μM.	24383475
HEK	Function assay		8 to 12 hrs	Agonist activity at human TLR8 expressed in HEK cells after 8 to 12 hrs by NFkappaB/SEAP reporter gene assay, EC50=6.13μM.	29152046
HEK	Function assay		24 hrs	Agonist activity at human TLR8 transfected in HEK cells assessed as NFkappaB induction after 24 hrs by specific secreted alkaline phosphatase gene assay, EC50=6.4μM.	22837811
PBMC	Function assay		24 hrs	Increase in IFNalpha level in human PBMC after 24 hrs relative to control	17548497
PBMC	Function assay		24 hrs	Increase in 2',5'-oligoadenylate synthase level in human PBMC after 24 hrs relative to control	17548497
PBMC	Toxicity assay		24 hrs	Toxicity assessed as increase in IL6 level in human PBMC after 24 hrs relative to control	17548497
Huh7	Antiviral assay		24 hrs	Antiviral activity against HCV infected human Huh7 replicon cells treated for 24 hrs with drug-induced human PBMC supernatants assessed as viral levels by luciferase assay	17548497
HEK293	Function assay			Agonist activity at human TLR7 expressed in HEK293 cells coexpressing pNiFty2-SEAP reporter by reporter gene assay, EC50=0.2601μM.	20232824
Huh7	Antiviral assay			Antiviral activity against HCV infected human Huh7 replicon cells treated with drug-induced human PBMC supernatants assessed as viral levels by luciferase assay	17548497
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生物活性

製品説明

Targets

TLR7 ^[1]

TLR8 ^[1]

In Vitro
In vitro	Resiquimod activates immune cells and induces proliferation of wild-type splenocytes via the Toll-like receptor 7 (TLR7)-MyD88-dependent signaling pathway. ^[1] Resiquimod also modulates dendritic cells to augment cytomegalovirus- and HIV-1-specific T cell responses. ^[2] Resiquimod induces the differentiation of myeloid-derived suppressor cells into macrophages and dendritic cells, and may improve cancer immunotherapy by reducing immunosuppressive MDSCs. ^[3]
細胞実験	細胞株	Peripheral blood leukocytes
	濃度	0.5–2 μg/ml
	反応時間	24 h
	実験の流れ	Cells were treated with various concentrations of drug.

In Vivo
In Vivo	In wild-type mice, Resiquimod (50 nmol, i.p.) induces increased serum concentrations of IFN-alpha, TNF-alpha and IL-12, while neither TLR7-deficient mice nor MyD88-deficient mice show an increase in these cytokines. ^[1] In a murine model of allergic asthma, Resiquimod (i.n., 20 μg/mouse) reduces allergen induced airway reactivity and inflammation via reduction in Nrf2 signaling. ^[4]
動物実験	動物モデル	Wild-type mice, TLR7-deficient mice, and MyD88-deficient mice
	投与量	50 nmol
	投与経路	i.p.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT06021002	Recruiting	Innate Inflammatory Response\|Asthma\|Nasal Allergy	Cambridge University Hospitals NHS Foundation Trust	August 9 2022	Not Applicable
NCT04127864	Active not recruiting	Colorectal Cancer\|Surgery	University of Copenhagen\|Zealand University Hospital	October 14 2019	--
NCT02688478	Unknown status	Allergies	University of British Columbia	February 2 2017	Not Applicable
NCT00960752	Completed	Melanoma	M.D. Anderson Cancer Center	May 20 2010	Phase 2

参考
[1] Hemmi H, et al. Nat Immunol. 2002, 3(2), 196-200. [2] Loré K, et al. J Immunol. 2003, 171(8), 4320-4328. [3] Lee M, et al. Arch Pharm Res. 2014, 37(9), 1234-1240. [4] Nadeem A, et al. Int J Biochem Cell Biol. 2016, 73, 53-62. [5] Zhou ZX, et al. Dev Comp Immunol. 2015 Mar;49(1):113-20. + 展開

参考

+ 展開

化学情報

分子量	314.38	化学式	C₁₇H₂₂N₄O₂
CAS No.	144875-48-9	SDF	Download Resiquimod (R-848) SDFをダウンロードする
Smiles	CCOCC1=NC2=C(N1CC(C)(C)O)C3=CC=CC=C3N=C2N
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 : 62 mg/mL ( (197.21 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。)

Ethanol : 51 mg/mL

Water : 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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