Resiquimod (R-848)

別名: S28463 中文名稱：雷西莫特，瑞喹莫德

目錄號：S8133 Purity: 99.98%

Resiquimod (R-848, S28463)是一種免疫反應調節(jié)劑，用作有效的TLR 7/TLR 8激動劑并可誘導如 TNF-α、IL-6 和 IFN-α 等細胞因子的上調。Resiquimod 可減少 hepatitis C virus (HCV)感染。Phase 2。

Resiquimod (R-848) Chemical Structure

CAS: 144875-48-9

規(guī)格	價格	庫存
10mM (1mL in DMSO)	810.81	現(xiàn)貨
20mg	794.43	現(xiàn)貨
50mg	1777.23	現(xiàn)貨
200mg	5298.93	現(xiàn)貨
1g	7944.3	現(xiàn)貨
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400-668-6834 info@selleck.cn

產(chǎn)品質控

批次：純度： 99.98%

99.98

Resiquimod (R-848)相關產(chǎn)品

相關靶點	TLR7 TLR8 TLR9 TLR4 TLR2 TLR3 TLR1 TLR6	點擊展開
相關產(chǎn)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	點擊展開
相關化合物庫	激酶抑制劑庫 FDA藥物庫天然產(chǎn)物庫已知活性藥物庫-I 高選擇性抑制劑庫	點擊展開

細胞實驗數(shù)據(jù)示例

細胞系	實驗類型	給藥濃度	孵育時間	活性描述	文獻信息
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
點擊查看更多細胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

靶點

TLR7 ^[1]

TLR8 ^[1]

體外研究(In Vitro)
體外研究活性	Resiquimod激活免疫細胞，并通過Toll-樣受體7(TLR7)-MyD88-依賴性信號通路誘導野生型脾細胞的增殖。^[1] Resiquimod也會調節(jié)樹突細胞以增加巨細胞病毒-和HIV-1-特異性T細胞應答。^[2] Resiquimod誘導髓源性抑制細胞分化為巨噬細胞和樹突細胞，并且可以通過減少免疫抑制的MDSCs提高癌癥免疫治療效果。^[3]

體外研究(In Vitro)

體外研究活性

Resiquimod激活免疫細胞，并通過Toll-樣受體7(TLR7)-MyD88-依賴性信號通路誘導野生型脾細胞的增殖。^[1]

Resiquimod也會調節(jié)樹突細胞以增加巨細胞病毒-和HIV-1-特異性T細胞應答。^[2]

Resiquimod誘導髓源性抑制細胞分化為巨噬細胞和樹突細胞，并且可以通過減少免疫抑制的MDSCs提高癌癥免疫治療效果。^[3]

體內研究(In Vivo)
體內研究活性	在野生型小鼠中，Resiquimod (50 nmol, i.p.)誘導IFN-α，TNF-α和IL-12的血清濃度增加，而TLR7-缺失或MyD88-缺失的小鼠不會增加其細胞因子。^[1] 在過敏性哮喘小鼠模型中，Resiquimod (i.n., 20 μg/小鼠)通過減少Nrf2信號從而減少過敏原誘導的氣道反應和炎癥。^[4]

體內研究(In Vivo)

體內研究活性

在野生型小鼠中，Resiquimod (50 nmol, i.p.)誘導IFN-α，TNF-α和IL-12的血清濃度增加，而TLR7-缺失或MyD88-缺失的小鼠不會增加其細胞因子。^[1]

在過敏性哮喘小鼠模型中，Resiquimod (i.n., 20 μg/小鼠)通過減少Nrf2信號從而減少過敏原誘導的氣道反應和炎癥。^[4]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗信息 (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

參考文獻
[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

參考文獻

[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

化學信息&溶解度

分子量	314.38	分子式	C₁₇H₂₂N₄O₂
CAS號	144875-48-9	SDF	Download Resiquimod (R-848) SDF
Smiles	CCOCC1=NC2=C(N1CC(C)(C)O)C3=CC=CC=C3N=C2N
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 62 mg/mL ( (197.21 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 51 mg/mL (162.22 mM)

Water : Insoluble

DMSO : 63 mg/mL ( (200.39 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 63 mg/mL (200.39 mM)

Water : Insoluble

DMSO : 62 mg/mL ( (197.21 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 27 mg/mL (85.88 mM)

Water : Insoluble

摩爾濃度計算器

體內溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

動物體內配方計算器

實驗計算

摩爾濃度計算器

質量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

動物體內配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數(shù)量只

第二步：請輸入動物體內配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計算結果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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C8=C7/X	C8:	LOG(C8):

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Resiquimod (R-848)

產(chǎn)品質控

Resiquimod (R-848)相關產(chǎn)品

細胞實驗數(shù)據(jù)示例

生物活性

化學信息&溶解度

實驗計算

技術支持