| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
TLR7 agonist 4 selectively targets Toll-like receptor 7 (TLR7), an endosomal receptor that recognizes single-stranded RNA. Activation of TLR7 leads to the induction of innate immune responses, including the production of pro-inflammatory cytokines.
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|---|---|
| ln Vitro |
TLR7 agonist 4 is a potent TLR7 agonist with an EC50 of 4.3 nM. It stimulates mouse bone marrow-derived macrophages to produce the pro-inflammatory cytokine TNFalpha. The compound activates TLR7, facilitating research in immunology and inflammatory diseases.
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| ln Vivo |
Dedicated in vivo efficacy studies for TLR7 agonist 4 are not extensively documented in standard profiles. As an immune activator, it is expected to induce cytokine production and modulate immune responses in animal models, with potential applications in vaccine adjuvants or cancer immunotherapy.
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| Enzyme Assay |
TLR7 activation is measured in HEK293 cells overexpressing human TLR7 and an NF-kappaB-driven reporter gene. Cells are treated with TLR7 agonist 4, and luciferase activity is measured after incubation. The EC50 is calculated from the concentration-response curve.
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| Cell Assay |
Mouse bone marrow-derived macrophages are isolated and cultured. They are treated with varying concentrations of TLR7 agonist 4. After stimulation, culture supernatants are collected, and TNFalpha levels are quantified by ELISA. Activation of downstream signaling pathways (NF-kappaB, MAPK) is confirmed by Western blot.
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| Animal Protocol |
In vivo protocols would typically involve subcutaneous or intravenous administration of TLR7 agonist 4 to mice (e.g., C57BL/6). Blood is collected at various time points post-administration, and serum cytokine levels (TNFalpha, IL-6, IFNalpha) are measured by ELISA to assess immune activation.
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| ADME/Pharmacokinetics |
PK properties for TLR7 agonist 4 are not extensively documented. As a small molecule with an EC50 in the low nanomolar range, it is likely to have favorable bioavailability for research purposes. Detailed ADME parameters are not publicly reported.
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| Toxicity/Toxicokinetics |
Toxicological data for TLR7 agonist 4 is not available in standard profiles. Given its mechanism as an immune agonist, potential toxicities associated with excessive cytokine production (cytokine storm) would be a primary concern. Extensive toxicology studies are not reported.
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| References | |
| Additional Infomation |
TLR7 agonist 4 is a research tool for studying innate immune activation. TLR7 agonists have clinical applications as vaccine adjuvants (e.g., imiquimod for topical use) and are being investigated for cancer immunotherapy. This compound is not an approved drug.
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| Molecular Formula |
C23H34N6O3
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|---|---|
| Molecular Weight |
442.55
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| Exact Mass |
442.269
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| CAS # |
2413016-42-7
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| PubChem CID |
138719993
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| Appearance |
White to off-white solid powder
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| LogP |
0.8
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
32
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| Complexity |
631
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| Defined Atom Stereocenter Count |
0
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| SMILES |
NC1N=C2C=CC=CC2=C2N(C(COCC)=NC=12)CC(OCCNC(C(C)(N)C)=O)(C)C
|
| InChi Key |
HKPICDFVVGLXQD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H34N6O3/c1-6-31-13-17-28-18-19(15-9-7-8-10-16(15)27-20(18)24)29(17)14-22(2,3)32-12-11-26-21(30)23(4,5)25/h7-10H,6,11-14,25H2,1-5H3,(H2,24,27)(H,26,30)
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| Chemical Name |
2-amino-N-[2-[1-[4-amino-2-(ethoxymethyl)imidazo[4,5-c]quinolin-1-yl]-2-methylpropan-2-yl]oxyethyl]-2-methylpropanamide
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2596 mL | 11.2982 mL | 22.5963 mL | |
| 5 mM | 0.4519 mL | 2.2596 mL | 4.5193 mL | |
| 10 mM | 0.2260 mL | 1.1298 mL | 2.2596 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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