| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Sotirimod functions as a Toll-like receptor 7 (TLR7) agonist. By activating TLR7, which is expressed on immune cells such as dendritic cells and macrophages, it stimulates the innate immune system. This leads to the production of pro-inflammatory cytokines and type I interferons (e.g., IFN-α), which enhance the immune response against pathogens and tumors.
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| ln Vitro |
In vitro, Sotirimod acts as a TLR7 agonist, activating immune cells and stimulating cytokine production. Its immunostimulatory activity can be assessed in cell-based assays using peripheral blood mononuclear cells (PBMCs) or purified dendritic cells, measuring the production of cytokines such as interferon-α, IL-12, and TNF-α by ELISA or multiplex assays.
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| ln Vivo |
In vivo, Sotirimod has been studied for the treatment of actinic keratosis and other dermatologic conditions. As an immunostimulant, it enhances the local immune response to clear abnormal cells or infections. Its topical application has been investigated for its efficacy in treating skin lesions, with clinical trials evaluating lesion clearance rates.
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| Enzyme Assay |
In vitro receptor binding assays for Sotirimod typically measure its affinity for Toll-like receptor 7 (TLR7). The compound's ability to activate TLR7 can also be assessed using reporter cell lines that express TLR7 and a reporter gene (e.g., NF-κB-driven luciferase) under the control of a TLR-responsive promoter, measuring luminescence upon treatment.
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| Cell Assay |
In vitro cellular assays for Sotirimod involve treating immune cells (e.g., PBMCs, dendritic cells) with the compound and measuring the production of cytokines (e.g., IFN-α, TNF-α) and the upregulation of activation markers (e.g., CD80, CD86) by flow cytometry or ELISA. These assays confirm its immunostimulatory activity as a TLR7 agonist.
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| Animal Protocol |
In vivo animal models for Sotirimod include models of actinic keratosis, skin infections (e.g., viral or fungal), or cancer to evaluate its immunostimulatory and therapeutic efficacy. The compound is typically applied topically, and its effects on lesion regression, tumor growth, or infection clearance are assessed, along with local immune cell infiltration.
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| ADME/Pharmacokinetics |
Sotirimod has a molecular formula of C14H17N5 and a molecular weight of 255.32 g/mol. Its IUPAC name is 2-methyl-1-(2-methylpropyl)-1H-imidazo[4,5-c][1,5]naphthyridin-4-amine. It is also known as R-850 and S-30594. The compound is an immunomodulator and TLR7 agonist, typically stored as a powder at -20°C.
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| Toxicity/Toxicokinetics |
Sotirimod is an immunostimulant with a well-characterized mechanism of action as a TLR7 agonist. As with any immunomodulator, potential toxicity may include excessive immune activation and inflammation, leading to local or systemic adverse effects. In topical formulations, it may cause application site reactions. It is for research use only.
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| Additional Infomation |
Drug Indication
This drug has been studied for the treatment of actinic keratosis and skin infections/diseases. Sotirimod, also known as R-850, is a synthetic small-molecule immunomodulator and a Toll-like receptor 7 (TLR7) agonist. It is an immunostimulant studied for dermatologic conditions. The compound is for research use only and is not approved for human therapeutic use. |
| Molecular Formula |
C14H17N5
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|---|---|
| Molecular Weight |
255.325
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| Exact Mass |
255.148
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| CAS # |
227318-75-4
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| PubChem CID |
6450818
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| Appearance |
White to off-white solid powder
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| Density |
1.33g/cm3
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| Boiling Point |
493.9ºC at 760mmHg
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| Flash Point |
252.5ºC
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| Vapour Pressure |
6.73E-10mmHg at 25°C
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| Index of Refraction |
1.698
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| LogP |
2.456
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
19
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| Complexity |
321
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| Defined Atom Stereocenter Count |
0
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| SMILES |
NC1=NC2=CC=CN=C2C3=C1N=C(C)N3CC(C)C
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| InChi Key |
ZXBCLVSLRUWISJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H17N5/c1-8(2)7-19-9(3)17-12-13(19)11-10(18-14(12)15)5-4-6-16-11/h4-6,8H,7H2,1-3H3,(H2,15,18)
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| Chemical Name |
2-methyl-1-(2-methylpropyl)imidazo[4,5-c][1,5]naphthyridin-4-amine
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| Synonyms |
IRM6 IRM 6 IRM-6R-850 S-30594R850 S30594
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~25 mg/mL (~97.9 mM; with ultrasonication and warming by heating to 80°C)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.79 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9165 mL | 19.5825 mL | 39.1650 mL | |
| 5 mM | 0.7833 mL | 3.9165 mL | 7.8330 mL | |
| 10 mM | 0.3917 mL | 1.9583 mL | 3.9165 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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