Name: Resiquimod (R-848)
Brand: Selleck Chemicals
SKU: S8133
Rating: 5 (19 reviews)

Spring naar

Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.98%

99.98

Gerelateerde doelwitten	PD-1/PD-L1 CXCR STING AhR Immunology & Inflammation related CD markers Interleukins Anti-infection Antioxidant COX
Overig TLR Inhibitoren	FSL-1 Resatorvid (TAK-242) TLR2-IN-C29 Lipopolysaccharides (LPS) Motolimod CU-CPT22 TLR4-IN-C34 Vesatolimod (GS-9620) E6446 Dihydrochloride E6446

Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving	PMID
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	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	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	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	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
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			Agonist activity at human TLR7 expressed in HEK293 cells coexpressing pNiFty2-SEAP reporter by reporter gene assay, EC50=0.2601μM.	20232824
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
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
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
Klik om meer experimentele gegevens over cellijnen te bekijken

Chemische informatie, opslag en stabiliteit (Chemical Information, Storage & Stability)

Molecuulgewicht	314.38	Formule	C₁₇H₂₂N₄O₂	Opslag (vanaf de datum van ontvangst)	3 jaar-20°Cpoeder
CAS-nr.	144875-48-9	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	S28463			Smiles	CCOCC1=NC2=C(N1CC(C)(C)O)C3=CC=CC=C3N=C2N

Oplosbaarheid (Solubility)

In vitro
Batch:

DMSO : 62 mg/mL (197.21 mM)
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 51 mg/mL

Water : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Molecuulgewicht
=	×	×

Verdunningscalculator Molecuulgewichtcalculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	3.150mg/ml (10.02mM)	Taking the 1 mL working solution as an example, add 50 μL 63 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo formulatiecalculator (heldere oplossing)

Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in de sectie oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH₂O, mengen en verhelderen.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme (Mechanism of Action)

Targets/IC₅₀/Ki	TLR7 TLR8
In vitro	Resiquimod (R-848) activates immune cells and induces proliferation of wild-type splenocytes via the Toll-like receptor 7 (TLR7)-MyD88-dependent signaling pathway. This compound also modulates dendritic cells to augment cytomegalovirus- and HIV-1-specific T cell responses. It induces the differentiation of myeloid-derived suppressor cells into macrophages and dendritic cells, and may improve cancer immunotherapy by reducing immunosuppressive MDSCs.
In vivo	In wild-type mice, Resiquimod (R-848) (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. In a murine model of allergic asthma, this compound (i.n., 20 μg/mouse) reduces allergen induced airway reactivity and inflammation via reduction in Nrf2 signaling.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/11812998/ [2] https://pubmed.ncbi.nlm.nih.gov/14530357/ [3] https://pubmed.ncbi.nlm.nih.gov/24748512/ [4] https://pubmed.ncbi.nlm.nih.gov/26851512/ [5] https://pubmed.ncbi.nlm.nih.gov/25475963/

Informatie over klinische proeven (Clinical Trial Information)

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-07-10)

NCT-nummer	Werving	Aandoeningen	Sponsor/medewerkers	Startdatum	Fasen
NCT06488118	UNKNOWN	Innate Immunity; Mucosal Immunity; Asthma; Viral Infection	Akhilesh Jha	2024-05-24
NCT06021002	UNKNOWN	Innate Inflammatory Response; Asthma; Nasal Allergy	Cambridge University Hospitals NHS Foundation Trust	2022-08-09
NCT01204684	COMPLETED	Glioma; Anaplastic Astrocytoma; Anaplastic Astro-oligodendroglioma; Glioblastoma	Jonsson Comprehensive Cancer Center	2010-10-08	PHASE2
NCT06021002	Recruiting	Innate Inflammatory Response\|Asthma\|Nasal Allergy	Cambridge University Hospitals NHS Foundation Trust	2022-08-09	Not Applicable
NCT00960752	COMPLETED	Melanoma	M.D. Anderson Cancer Center	2010-05-20	PHASE2
NCT02126579	COMPLETED	Melanoma; Metastatic Melanoma; Mucosal Melanoma	Craig L Slingluff, Jr	2014-05-01	PHASE1; PHASE2

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):

Resiquimod (R-848) TLR7/8-agonist

Molecuulgewicht: 314.38

Kwaliteitscontrole (Quality Control)

Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)

Chemische informatie, opslag en stabiliteit (Chemical Information, Storage & Stability)

Oplosbaarheid (Solubility)

Molariteitscalculator

In vivo formulatiecalculator (heldere oplossing)

Werkingsmechanisme (Mechanism of Action)

Informatie over klinische proeven (Clinical Trial Information)

Resiquimod (R-848) TLR7/8-agonist

Molecuulgewicht: 314.38

Kwaliteitscontrole (Quality Control)

Celkweek, behandeling & werkzame concentratie (Cell Culture, Treatment & Working Concentration)

Chemische informatie, opslag en stabiliteit (Chemical Information, Storage & Stability)

Oplosbaarheid (Solubility)

Molariteitscalculator

In vivo formulatiecalculator (heldere oplossing)

Werkingsmechanisme (Mechanism of Action)

Informatie over klinische proeven (Clinical Trial Information)

Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)