Size | Price | Stock | Qty |
---|---|---|---|
100mg |
|
||
250mg |
|
||
500mg |
|
||
1g |
|
||
2g |
|
||
Other Sizes |
|
Purity: ≥98%
Imiquimod (S-26308; R-837; TMX-101; Aldara; Zyclara) is an immune response modifier that acts as an agonist of the TLR7 (toll-like receptor 7). Imiquimod is an approved prescription medication that is used to treat genital warts, superficial basal cell carcinoma, and actinic keratosis. Scientists at 3M's pharmaceuticals division discovered the drug and 3M obtained the first FDA approval in 1997 under the brand name of Aldara. As of 2015, imiquimod is generic and is available worldwide under many brands. Imiquimod signals to the innate arm of the immune system through the TLR7, commonly involved in pathogen recognition. Cells activated by imiquimod via TLR-7 secrete cytokines such as interferon-α (INF-α), interleukin-6 (IL-6), and tumor necrosis factor-α (TNF-α). Imiquimod has been studied in combination with pembrolizumab for treating stage IIIB-IV melanoma.
ln Vitro |
|
||
---|---|---|---|
ln Vivo |
Imiquimod can be used to create animal models of psoriasis. Imiquimod incites the innate immune response in animal models through NK cell activation, nitric oxide and cytokine secretion from activated macrophages, and B lymphocyte differentiation and proliferation. By triggering, producing, and releasing cytokines such as interleukin (IL)-6, tumor necrosis factor (TNF)-alpha, and interferon-alpha (IFN-alpha), imiquimod activates the innate immune response [1].
|
||
Animal Protocol |
|
||
References |
[1]. Athina Angelopoulou, et al. Imiquimod - A toll like receptor 7 agonist - Is an ideal option for management of COVID 19. Environ Res. 2020 Sep; 188: 109858.
[2]. Aditya K Gupta, et al. Imiquimod: a review. J Cutan Med Surg. Nov-Dec 2002;6(6):554-60. [3]. Yuji Kan, et al. Imiquimod suppresses propagation of herpes simplex virus 1 by upregulation of cystatin A via the adenosine receptor A1 pathway. J Virol. 2012 Oct;86(19):10338-46. [4]. Michael P Schön, et al. The small antitumoral immune response modifier imiquimod interacts with adenosine receptor signaling in a TLR7- and TLR8-independent fashion. J Invest Dermatol. 2006 Jun;126(6):1338-47. |
Molecular Formula |
C14H16N4
|
---|---|
Molecular Weight |
240.3
|
CAS # |
99011-02-6
|
Related CAS # |
Imiquimod hydrochloride;99011-78-6;Imiquimod maleate;896106-16-4;Imiquimod-d6;Imiquimod-d9;2712126-48-0
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
SMILES |
NC1=NC2=CC=CC=C2C3=C1N=CN3CC(C)C
|
Chemical Name |
1-isobutyl-1H-imidazo[4,5-c]quinolin-4-amine
|
Synonyms |
S26308; R 837; TMX-101; S 26308; R837; TMX 101; S-26308; R837; TMX101; Brand names: Aldara; Zyclara; Vyloma; Beselna.
|
HS Tariff Code |
2934.99.9001
|
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)
|
Solubility (In Vitro) |
|
|||
---|---|---|---|---|
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 | 4.1615 mL | 20.8073 mL | 41.6146 mL | |
5 mM | 0.8323 mL | 4.1615 mL | 8.3229 mL | |
10 mM | 0.4161 mL | 2.0807 mL | 4.1615 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.