| Size | Price | Stock | Qty |
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| 5mg |
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| Targets |
CL-075 targets Toll-like receptor 8 (TLR8), a pattern recognition receptor expressed primarily on monocytes, macrophages, and dendritic cells. TLR8 recognizes single-stranded RNA and initiates innate immune responses. CL-075 activates TLR8, triggering the MyD88-dependent signaling pathway. This leads to the activation of NF-κB and IRF7 transcription factors, resulting in the production of pro-inflammatory cytokines (TNF-α, IL-12, IL-6) and type I interferons.
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| ln Vitro |
In rabbit tumor cells, CL075 (2 μM; 4 h) stimulates the production of IL-6, IL-8, and IFN-γ [1]. In rabbit tumor cells, CL075 (2 μM; 48 h) causes total IgM synthesis and cell growth [1]. In 293 cells, CL075 (2 μM; 7 hours) activates rabTLR8[1].
In vitro, CL-075 induces production of TNF-α and IL-12 from peripheral blood mononuclear cells (PBMCs). It promotes maturation of monocyte-derived dendritic cells in combination with Poly(I:C). At a concentration of 0.4 μM, CL-075 induces NF-κB activation. The compound demonstrates potent TLR8 agonistic activity with specificity for TLR8 over TLR7. Detailed in vitro activity data including EC50 values are available from published studies. |
| ln Vivo |
In rabbits, CL075 (5 μM (0.5 mL); sc) elicits the tiny arrowhead reaction [1].
In vivo, CL-075 has been studied for its immunostimulatory effects in animal models. As a TLR8 agonist, it activates innate immune responses, inducing the production of inflammatory cytokines and type I interferons. The compound has been investigated for its potential as a vaccine adjuvant and in cancer immunotherapy. Specific in vivo data including dose-response relationships and efficacy in disease models are available from published studies. |
| Enzyme Assay |
In vitro receptor binding assays for TLR8 agonists typically use HEK293 or other cell lines expressing human TLR8 along with an NF-κB-driven reporter gene (e.g., luciferase). Cells are treated with CL-075 at various concentrations, and reporter gene activity is measured after 16-24 hours. EC50 values for TLR8 activation are calculated from dose-response curves. Specificity for TLR8 over TLR7 is assessed using cells expressing TLR7. Positive controls include R848 (resiquimod) or other TLR7/8 agonists.
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| Cell Assay |
Cellular assays for TLR8 agonists typically use human PBMCs, monocytes, or monocyte-derived dendritic cells. Cells are treated with CL-075 at various concentrations, and cytokine production (TNF-α, IL-12, IL-6, IFN-α) is measured in the culture supernatant by ELISA or multiplex immunoassay. Cell surface marker expression (e.g., CD80, CD86, HLA-DR) is assessed by flow cytometry to measure dendritic cell maturation. The degree of cytokine induction and cell activation is calculated from dose-response curves.
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| Animal Protocol |
In vivo animal studies for TLR8 agonists typically use mouse models. Since mice do not express TLR8 (TLR8 is functional in humans and other species but not in mice), humanized TLR8 mouse models or non-human primates are used. Animals are administered CL-075 intravenously, subcutaneously, or topically, and immune responses are assessed by measuring cytokine levels in serum, immune cell activation in lymphoid organs, and antigen-specific antibody responses (for vaccine adjuvant studies). Efficacy in tumor models may also be assessed.
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| ADME/Pharmacokinetics |
CL-075 is administered via various routes including intravenous, subcutaneous, or topical application for research purposes. As a small-molecule TLR8 agonist, it has favorable physicochemical properties for formulation. The compound is metabolized in the liver, and its metabolites are excreted via the kidneys. Detailed PK parameters such as half-life, Cmax, and AUC are available from preclinical studies.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of CL-075 would typically include acute and repeated-dose toxicity in rodents and non-human primates, as well as genotoxicity and safety pharmacology assessments. As a TLR8 agonist, the compound is expected to induce immune activation, which may result in systemic inflammatory responses such as cytokine release syndrome at high doses. Careful dose optimization is required to balance efficacy and safety. The compound is generally well-tolerated at therapeutic doses.
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| References |
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| Additional Infomation |
CL-075 (3M002) is a selective TLR8 agonist with immunomodulatory activity. It activates the MyD88-dependent signaling pathway, inducing NF-κB and IRF7 activation and production of inflammatory cytokines and type I interferons. The compound is used in immunology research for studying innate immune signaling, antiviral defense, vaccine adjuvant design, and cancer immunotherapy. It is a synthetic imidazoquinoline derivative available for research use only.
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| Molecular Formula |
C13H13N3S
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|---|---|
| Molecular Weight |
243.328
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| Exact Mass |
243.083
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| CAS # |
256922-53-9
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| PubChem CID |
10198719
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| Appearance |
White to off-white solid powder
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| LogP |
3.309
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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 |
17
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| Complexity |
273
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NFYMGJSUKCDVJR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H13N3S/c1-2-5-10-16-11-12(17-10)8-6-3-4-7-9(8)15-13(11)14/h3-4,6-7H,2,5H2,1H3,(H2,14,15)
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| Chemical Name |
2-propyl-[1,3]thiazolo[4,5-c]quinolin-4-amine
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| Synonyms |
CL075 3M-002 CL-075 3M002 CL-075
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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 : ~22 mg/mL (~90.41 mM)
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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 | 4.1096 mL | 20.5482 mL | 41.0965 mL | |
| 5 mM | 0.8219 mL | 4.1096 mL | 8.2193 mL | |
| 10 mM | 0.4110 mL | 2.0548 mL | 4.1096 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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