PF-4878691
Based on 1 Customer Validation
PF-4878691 (3M-852A) is an orally active TLR7 agonist. PF-4878691 has the innate immune response activity, antiviral efficacy against HCV, and can be used for the research of cancer.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.19%
- CAS. Nr.: 532959-63-0
- Formel: C17H23N5O2S
- Molecular Weight:361.46
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
IC50 & Target
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TLR7 |
IL-6 |
IL-8 |
IL-1β |
IL-2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
2657 nM
Compound: 852A
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Agonist activity at human TLR7 expressed in HEK293 cells by NFkappaB SEAP reporter gene assay
Agonist activity at human TLR7 expressed in HEK293 cells by NFkappaB SEAP reporter gene assay
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[PMID: 23265901] |
In Vitro
PF-4878691 (10 μM, 4 h) induces a complex transcription network responsible for activating plasmacytoid dendritic cells for innate antiviral immune responses with optimized responses towards RNA viruses, increases co-stimulatory capacity, and increases survival in plasmacytoid dendritic cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice , C57bl/6 J mice[3]
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Dosage:30 mg/kg, 60 mg/kg, 90 mg/kg, 150 mg/kg
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Administration:Oral gavage (p.o.)
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Result:Induced dose and time dependant lymphopenia and 2,5,oligoadenylate synthetase (2,5,OAS). Caused cardiovascular changes. Significantly increased TLR7 receptor RNA.
Chemical Information
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CAS. Nr. 532959-63-0
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Appearance Solid
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Molecular Weight 361.46
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Formel C17H23N5O2S
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Color White to off-white
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SMILES
CS(=O)(NCCCCN1C(CC)=NC2=C1C3=CC=CC=C3N=C2N)=O
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Synonyms
3M-852A
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 19.23 mg/mL (53.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.92 mg/mL (5.31 mM); Clear solution
This protocol yields a clear solution of ≥ 1.92 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (19.2 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.92 mg/mL (5.31 mM); Clear solution
This protocol yields a clear solution of ≥ 1.92 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (19.2 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
Reinheit & Dokumentation
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Fidock MD, et al. The innate immune response, clinical outcomes, and ex vivo HCV antiviral efficacy of a TLR7 agonist (PF-4878691). Clin Pharmacol Ther. 2011 Jun;89(6):821-9. [Content Brief]
[3]. Horscroft NJ, et al. Antiviral applications of Toll-like receptor agonists. J Antimicrob Chemother. 2012 Apr;67(4):789-801. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7666 mL | 13.8328 mL | 27.6656 mL | 69.1639 mL |
| 5 mM | 0.5533 mL | 2.7666 mL | 5.5331 mL | 13.8328 mL | |
| 10 mM | 0.2767 mL | 1.3833 mL | 2.7666 mL | 6.9164 mL | |
| 15 mM | 0.1844 mL | 0.9222 mL | 1.8444 mL | 4.6109 mL | |
| 20 mM | 0.1383 mL | 0.6916 mL | 1.3833 mL | 3.4582 mL | |
| 25 mM | 0.1107 mL | 0.5533 mL | 1.1066 mL | 2.7666 mL | |
| 30 mM | 0.0922 mL | 0.4611 mL | 0.9222 mL | 2.3055 mL | |
| 40 mM | 0.0692 mL | 0.3458 mL | 0.6916 mL | 1.7291 mL | |
| 50 mM | 0.0553 mL | 0.2767 mL | 0.5533 mL | 1.3833 mL |
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