Resiquimod | 雷西莫德 | R848 | TLR7/TLR8 Agonist (GMP)

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雷西莫特 /Resiquimod 98%

货号：A119633 同义名： 雷西莫德 / R848;S28463

Resiquimod（R848）（GMP）是根据GMP指南生产的，用作细胞治疗制造中的辅助试剂。它是Toll样受体7和8（TLR7/TLR8）的激动剂，能诱导人类mMDSC成熟为炎性巨噬细胞。

Resiquimod 化学结构
CAS号：144875-48-9

Resiquimod 3D分子结构
CAS号：144875-48-9

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Resiquimod 纯度/质量文件产品仅供科研

货号：A119633 标准纯度： 98% 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nat. Commun., 2024, 15, 7687. Ambeed. [ A119633 ]; • ACS Nano, 2024. Ambeed. [ A1194179 ]; • J. Mol. Cell. Cardiol., 2024, 196, 94-104. Ambeed. [ A133052 ]; • iScience, 2024, 110928. Ambeed. [ A1375212 ]; • Mol. Pharmaceutics, 2024. Ambeed. [ A305202 , A409401 ]; 更多 >

Resiquimod 生物活性

描述

Toll-like receptors (TLRs) are a family of pattern recognition receptors involving in the innate and adaptive immunity. The activation of TLR7, which is intracellular receptor expressed on endosomal membranes, can induce Type 1 interferon and inflammatory response^[1]. Resiquimod is an immune system modifier as a TLR7 agonist with high potency induce cytokine expression for the treatment of viral and tumor lesions^[2]. The EC₅₀ of the resiquimod is 1.4 μM to TLR7^[3].
Acute myeloid leukemia (AML) cells were treated with 5 μg/mL of resiquimod during 24 h. The expression of MHC class I and II molecules on the membrane of primary AML cells measured by flow cytometry and the production of IL-6, IL-1β and TNF-α measured by multiplex fluorescent bead immunoassay, were increased after the treatment with resiquimod^[4].
The resiquimod were injected to BALB/c mice with breast cancer intraperitoneally for three continuous days in a week for three weeks. The resiquimod could significantly retard tumor growth compared with the vehicle group by reducing the density of tumor vasculature and inducing tumor cell apoptosis^[5].

作用机制

The effect of resiquimod in the TLR signaling pathway is through binding to the TLR7. Therefore, it can activate the TLR7 mainly on dendritic cells, macrophages, and B-lymphocytes.

Resiquimod 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
HEK293 cells		Function assay		Agonist activity at human TLR7 expressed in HEK293 cells coexpressing pNiFty2-SEAP reporter by reporter gene assay, EC50=0.2601 μM	20232824
HEK293 cells		Function assay	24 h	Agonist activity at human TLR-7 expressed in HEK293 cells after 24 hrs by SEAP reporter gene assay, EC50=1.5 μM	24383475
Huh7 replicon cells		Function 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
human PBMC		Function assay	24 h	Increase in IFNalpha level in human PBMC after 24 hrs relative to control	17548497

Resiquimod 动物研究

Dose	C57BL/6 Mice: 1 mg/kg^[6] (intratracheally); 2 mg/kg^[7] (i.v.) C3H/HeN Mice: 1 mg/kg - 5 mg/kg^[8] (i.v.) BALB/c Mice: 3 mg/kg^[5] (i.p.) Mice: 10 mg/kg^[9] (i.p.), 2 mg/kg^[10] (s.c.)
Administration	i.v., i.p., s.c.

Resiquimod 临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02688478	Allergies	Not Applicable	Recruiting	May 7, 2020	Canada, British Columbia ... 展开 >> University of British columbia Recruiting Vancouver, British Columbia, Canada, V5Z 1M9 Contact: Christopher Carlsten, MD, PHD 604-875-4122 carlsten@mail.ubc.ca Principal Investigator: Christopher Carlsten, MD, MPH 收起 <<
NCT02637219	-		Completed	-	United States, Washington ... 展开 >> VA Puget Sound Health Care System Seattle, Washington, United States, 98108 收起 <<
NCT02687503	Respiratory Tract Infections	Not Applicable	Active, not recruiting	January 2019	United States, Wisconsin ... 展开 >> UW Health 20 S. Park Clinic Madison, Wisconsin, United States, 53715 UW Health West Towne Clinic Madison, Wisconsin, United States, 53717 收起 <<

Resiquimod 参考文献

[1]Chi H, Li C, Zhao FS, et al. Anti-tumor Activity of Toll-Like Receptor 7 Agonists. Front Pharmacol. 2017.

[2]Meyer T, Surber C, et al. Resiquimod, a topical drug for viral skin lesions and skin cancer. Expert Opin Investig Drugs. 2013;22(1):149-59.

[3]Kubli-Garfias C, Vázquez-Ramírez R, et al. Insights on the mechanism of action of immunostimulants in relation to their pharmacological potency. The effects of imidazoquinolines on TLR8. PLoS One. 2017;12(6):e0178846.

[4]Smits EL, Cools N, et al. The Toll-like receptor 7/8 agonist resiquimod greatly increases the immunostimulatory capacity of human acute myeloid leukemia cells. Cancer Immunol Immunother. 2010;59(1):35-46.

[5]Yin T, He S, Wang Y. Toll-like receptor 7/8 agonist, R848, exhibits antitumoral effects in a breast cancer model. Mol Med Rep. 2015;12(3):3515-3520.

Resiquimod 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.18mL

0.64mL

0.32mL

15.90mL

3.18mL

1.59mL

31.81mL

6.36mL

3.18mL

Resiquimod 技术信息

CAS号	144875-48-9
分子式	C₁₇H₂₂N₄O₂
分子量	314.382

别名	雷西莫德 ;R848;S28463;VML-600
运输	蓝冰

存储条件

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 30 mg/mL(95.43 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

DMF: 50 mg/mL(159.04 mM)，配合低频超声助溶

动物实验配方

IP 2% DMSO+water 5 mg/mL clear

PO 0.5% CMC-Na 75 mg/mL suspension

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT02688478	Allergies	Not Applicable	Recruiting	May 7, 2020	Canada, British Columbia ... 展开 >> University of British columbia Recruiting Vancouver, British Columbia, Canada, V5Z 1M9 Contact: Christopher Carlsten, MD, PHD 604-875-4122 carlsten@mail.ubc.ca Principal Investigator: Christopher Carlsten, MD, MPH 收起 <<
NCT02637219	-		Completed	-	United States, Washington ... 展开 >> VA Puget Sound Health Care System Seattle, Washington, United States, 98108 收起 <<
NCT02687503	Respiratory Tract Infections	Not Applicable	Active, not recruiting	January 2019	United States, Wisconsin ... 展开 >> UW Health 20 S. Park Clinic Madison, Wisconsin, United States, 53715 UW Health West Towne Clinic Madison, Wisconsin, United States, 53717 收起 <<
NCT02660723	Healthy	Not Applicable	Completed	-	France ... 展开 >> CHU de Nice, CRC, Hôpital de l'Archet 151 route de saint-antoine de ginestière Nice, Alpes-Maritimes, France, 06200 收起 <<
NCT01094496	Bladder Cancer	Phase 2	Terminated(Portfolio prioritiz... 展开 >>ation due to slow enrollment) 收起 <<	October 2017	United States, Arizona ... 展开 >> BCG Oncology, PC Phoenix, Arizona, United States, 85032 United States, California University of California - San Diego La Jolla, California, United States, 92093 University of Southern California Norris Comprehensive Cancer Center LA-USC Medical Center Los Angeles, California, United States, 90033 United States, Colorado University of Colorado Cancer Center Aurora, Colorado, United States, 80045 United States, Florida University of Florida Gainesville, Florida, United States, 32610 Moffitt Cancer Center Tampa, Florida, United States, 33612 United States, Iowa University of Iowa Hospitals and Clinics Iowa City, Iowa, United States, 52242 United States, Kentucky University of Kentucky Markey Cancer Center Clinical Research Organization Lexington, Kentucky, United States, 40536-0093 United States, Maryland University of Maryland Greenebaum Cancer Center Baltimore, Maryland, United States, 21201 United States, Michigan Henry Ford Health System Detroit, Michigan, United States, 48202 United States, Missouri Washington University School of Medicine St. Louis, Missouri, United States, 63110 United States, New York Roswell Park Cancer Center Buffalo, New York, United States, 14263 Weill Cornell Medical College New York, New York, United States, 10021 University of Rochester Rochester, New York, United States, 14642 SUNY Upstate Medical University Syracuse, New York, United States, 13210 Syracuse VA Medical Center Syracuse, New York, United States, 13210 United States, Pennsylvania Thomas Jefferson University Philadelphia, Pennsylvania, United States, 19107 收起 <<
NCT01204684	Glioma Anapla... 展开 >>stic Astrocytoma Anaplastic Astro-oligodendroglioma Glioblastoma 收起 <<	Phase 2	Active, not recruiting	October 2019	United States, California ... 展开 >> University of Los Angeles, California Los Angeles, California, United States, 90095 收起 <<
NCT00175435	Hepatitis B	Phase 1 Phase 2	Completed	-	Canada, British Columbia ... 展开 >> Vancouver General Hospital Vaccine Education Centre Vancouver, British Columbia, Canada 收起 <<
NCT00948961	Advanced Malignancies	Phase 1 Phase 2	Completed	-	United States, Connecticut ... 展开 >> Yale Comprehensive Cancer Center New Haven, Connecticut, United States, 06519-1717 United States, Florida Mount Sinai Comprehensive Cancer Center Miami Beach, Florida, United States, 33140 United States, Michigan Henry Ford Health System Detroit, Michigan, United States, 48202 United States, New York Memorial Sloan Kettering Cancer Center New York, New York, United States, 10017 Weill Cornell Cancer Center New York, New York, United States, 10065 United States, North Carolina Carolina BioOncology Institute, PLLC Huntersville, North Carolina, United States, 28078 United States, Oregon Providence Portland Cancer Center Portland, Oregon, United States, 97213 收起 <<
NCT02090374	Allergic Rhinitis ... 展开 >> Asthma Latent Tuberculosis 收起 <<	Not Applicable	Completed	-	United Kingdom ... 展开 >> Imperial Clinical Respiratory Research Unit (ICRRU), St Mary's Hospital Paddington, London, United Kingdom, W2 1NY 收起 <<
NCT00115141	Warts	Phase 2	Completed	-	-
NCT02126579	Melanoma Meta... 展开 >>static Melanoma Mucosal Melanoma 收起 <<	Phase 1 Phase 2	Recruiting	December 2018	United States, Texas ... 展开 >> MDAnderson Cancer Center Active, not recruiting Houston, Texas, United States, 77030 United States, Virginia University of Virginia Recruiting Charlottesville, Virginia, United States, 22908 Contact: Emily Allred, PhD 434-982-1902 eh4m@virginia.edu Contact: Alexandra Carney, MPH 434-982-6714 alc6a@virginia.edu Principal Investigator: Craig L. Slingluff, MD, M.D. 收起 <<
NCT01806961	-		Terminated(sponsor decision)	-	-
NCT00114920	Warts	Phase 2	Completed	-	United States, Indiana ... 展开 >> Welborn Clinic Evansville, Indiana, United States, 47713 收起 <<
NCT00960752	Melanoma	Phase 2	Active, not recruiting	May 2019	United States, Texas ... 展开 >> University of Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 收起 <<
NCT00116662	Warts	Phase 2	Completed	-	United States, Arkansas ... 展开 >> Arkansas Fayetteville, Arkansas, United States, 72703 Arkansas Little Rock, Arkansas, United States, 72205 United States, Georgia Georgia Newnan, Georgia, United States, 30263 United States, Illinois Illinois Buffalo Grove, Illinois, United States, 60089 United States, Indiana Indiana Lafayette, Indiana, United States, 47904 United States, Kansas Kansas Wichita, Kansas, United States, 67207 United States, Massachusetts Massachusetts Boston, Massachusetts, United States, 02114 United States, Missouri Missouri St. Louis, Missouri, United States, 63110 United States, Utah Utah Layton, Utah, United States, 84041 United States, Vermont Vermont Burlington, Vermont, United States, 05401 收起 <<
NCT01806961	-		Terminated(sponsor decision)	-	Germany ... 展开 >> Hauttumorcentrum Charité (HTCC) Berlin, Germany Medizinisches Zentrum Bonn - Friedensplatz Bonn, Germany Hautzentrum Düsseldorf, Germany Johannes Wesling Klinikum Minden Minden, Germany KLINIKUM VEST GmbH Knappschaftskrankenhaus Recklinghausen, Germany Switzerland Universitätsspital Basel Basel, Switzerland Inselspital Bern, Switzerland Kantonsspital St.Gallen St. Gallen, Switzerland Universitaetsspital Zurich Zurich, Switzerland 收起 <<
NCT00117871	Warts	Phase 2	Completed	-	United States, Minnesota ... 展开 >> Minnesota Clinical Study Center Fridley, Minnesota, United States, 55432 收起 <<
NCT00117923	Warts	Phase 2	Completed	-	United States, Oregon ... 展开 >> Oregon Medical Research Center Portland, Oregon, United States, 97223 收起 <<
NCT01737580	Influenza Vaccination in Senio... 展开 >>rs 收起 <<	Phase 1	Completed	-	Canada, British Columbia ... 展开 >> University of British Columbia Vancouver General Hospital Vancouver, British Columbia, Canada, V5Z 1M9 收起 <<
NCT01808950	Nodular Basal Cell Carcinoma	Phase 1 Phase 2	Terminated(safety issues)	-	Germany ... 展开 >> Hauttumorcentrum Charité (HTCC) Berlin, Germany Switzerland Universitaetsspital Zurich, Switzerland 收起 <<
NCT01808950	-		Terminated(safety issues)	-	-
NCT00470379	Melanoma (Skin)	Early Phase 1	Completed	-	United States, Minnesota ... 展开 >> Mayo Clinic Rochester, Minnesota, United States, 55905 收起 <<
NCT01748747	Recurrent Melanoma ... 展开 >> Stage IIA Melanoma Stage IIB Melanoma Stage IIC Melanoma Stage IIIA Melanoma Stage IIIB Melanoma Stage IIIC Melanoma Stage IV Melanoma 收起 <<	Early Phase 1	Completed	-	United States, Minnesota ... 展开 >> Mayo Clinic Rochester, Minnesota, United States, 55905 收起 <<
NCT01676831	Cutaneous T Cell Lymphoma	Phase 1 Phase 2	Unknown	-	United States, Pennsylvania ... 展开 >> University of Pennsylvania Philadelphia, Pennsylvania, United States, 19104 收起 <<
NCT00821652	Tumors	Phase 1	Completed	-	United States, New York ... 展开 >> Icahn School of Medicine at Mount Sinai New York, New York, United States, 10029 收起 <<
NCT01583816	Actinic Keratosis	Phase 2	Completed	-	Germany ... 展开 >> Hauttumorcentrum Charité (HTCC) Berlin, Germany Medizinisches Zentrum Bonn - Friedensplatz Bonn, Germany Hautzentrum Düsseldorf, Germany Johannes Wesling Klinikum Minden Minden, Germany KLINIKUM VEST GmbH Knappschaftskrankenhaus Recklinghausen, Germany Switzerland Kantonsspital Aarau Aarau, Switzerland Universitätsspital Basel Basel, Switzerland Inselspital Bern, Switzerland Kantonsspital St.Gallen St. Gallen, Switzerland Universitaetsspital Zurich Zurich, Switzerland 收起 <<
NCT00116675	Warts	Phase 2	Completed	-	United States, Arkansas ... 展开 >> Children's Clinic of Jonesboro, PA Jonesboro, Arkansas, United States, 72401 United States, California University of California - San Francisco San Francisco, California, United States, 94143 United States, Colorado Longmont Clinic/Longmont Medical Research Network Longmont, Colorado, United States, 80501 United States, Missouri Mercy Health Research St. Louis, Missouri, United States, 63141 United States, New Hampshire Dartmouth-Hitchcock Medical Center Lebanon, New Hampshire, United States, 03756 United States, Rhode Island Rhode Island Hospital - Jane Brown Building Providence, Rhode Island, United States, 02903 United States, Texas DermResearch, Inc. Austin, Texas, United States, 78759 United States, Utah Alpine Pediatrics Pleasant Grove, Utah, United States, 84062 United States, Washington Walla Walla Clinic Walla Walla, Washington, United States, 99362 United States, Wisconsin Advanced Healthcare Milwaukee, Wisconsin, United States, 53209 收起 <<

雷西莫特 /Resiquimod 98%

Resiquimod 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Resiquimod 质控信息

Resiquimod 生物活性

Resiquimod 细胞研究

Resiquimod 动物研究

Resiquimod 临床研究

Resiquimod 参考文献

Resiquimod 实验方案

Resiquimod 技术信息

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雷西莫特 /Resiquimod 98%

Resiquimod 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Resiquimod 质控信息

Resiquimod 生物活性

Resiquimod 细胞研究

Resiquimod 动物研究

Resiquimod 临床研究

Resiquimod 参考文献

Resiquimod 实验方案

Resiquimod 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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