Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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ln Vitro |
TLR7/8 agonist 1 (compound 5d) exhibited strong immunostimulatory action. With minimal activity loss, TLR7/8 agonist 1 acts as an easy precursor for fluorophore covalent attachment. With an EC50 of 20 nM, TLR7/8 Agonist 1 maintains TLR7 agonistic activity [1]. A preliminary screen of human TLR7 (50 nM) and TLR8 (55 nM) revealed considerably differing agonistic potencies for TLR7/8 agonist 1 (Compound 1) [2].
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References |
[1]. Shukla NM, et al. Syntheses of fluorescent imidazoquinoline conjugates as probes of Toll-like receptor 7. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6384-6.
[2]. Beesu M, et al. Structure-Based Design of Human TLR8-Specific Agonists with Augmented Potency and Adjuvanticity. J Med Chem. 2015 Oct 8;58(19):7833-49 |
Molecular Formula |
C22H27CL2N5
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Molecular Weight |
432.39
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Exact Mass |
431.1644
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CAS # |
1620278-72-9
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Related CAS # |
TLR7/8 agonist 1;1258457-59-8
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SMILES |
Cl.Cl.N1(C(CC2C=CC(CN)=CC=2)=NC2C(N)=NC3C=CC=CC=3C1=2)CCCC
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Synonyms |
TLR7/8 agonist 5d TLR7/8 agonist5d TLR7/8 agonist-5d
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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) |
DMSO : ~83.33 mg/mL (~192.72 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.81 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.81 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.81 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.3127 mL | 11.5636 mL | 23.1273 mL | |
5 mM | 0.4625 mL | 2.3127 mL | 4.6255 mL | |
10 mM | 0.2313 mL | 1.1564 mL | 2.3127 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.