| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
PF-03654746 Tosylate targets the histamine H3 receptor, a presynaptic receptor that modulates the release of histamine and other neurotransmitters in the brain. As an antagonist, it blocks this receptor, which can enhance cognitive function. It reduces allergen-induced nasal symptoms and has been studied for cognitive disorders and Alzheimer's disease.
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| ln Vitro |
In vitro, PF-03654746 Tosylate is a potent and selective antagonist of the histamine H3 receptor. Its activity is assessed in receptor binding assays using cell membranes expressing the human H3 receptor. It has shown high brain penetration, making it useful for studying central nervous system disorders.
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| ln Vivo |
In vivo, PF-03654746 Tosylate has been shown to reduce allergen-induced nasal symptoms. It has also been studied for its potential to improve cognitive efficacy and disease-modifying effects in Alzheimer's disease. Its high brain penetration makes it a valuable tool for CNS research.
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| Enzyme Assay |
In vitro receptor binding assays for PF-03654746 Tosylate are performed to measure its affinity for the histamine H3 receptor. These assays typically involve competitive displacement of a radiolabeled ligand from the receptor using membranes from cells expressing the human H3 receptor. Its potency is determined from the resulting IC50 values.
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| Cell Assay |
Cellular assays for PF-03654746 Tosylate are not well-defined. As a histamine H3 receptor antagonist, its effects can be studied in neuronal cell lines or primary neurons by measuring the release of neurotransmitters, such as histamine, acetylcholine, or dopamine, upon receptor modulation.
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| Animal Protocol |
In vivo animal studies for PF-03654746 Tosylate are conducted in models of allergic rhinitis, cognitive dysfunction, and Alzheimer's disease. Animals are treated with the compound, and endpoints such as nasal symptom scores, cognitive performance in behavioral tests, and disease pathology are assessed.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of PF-03654746 Tosylate are characteristic of a small molecule with high brain penetration. It has a molecular weight of 494.6 and a molecular formula of C25H32F2N2O4S. It is a tosylate salt and is typically stored in a cool, dry place.
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| Toxicity/Toxicokinetics |
The toxicological profile of PF-03654746 Tosylate is not fully detailed. As a research compound, its safety is evaluated in preclinical studies. It is for research use only and is not for human therapeutic use. Standard safety precautions should be followed.
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| References |
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| Additional Infomation |
PF-03654746 Tosylate is a potent and selective histamine H3 receptor antagonist with high brain penetration. It is developed by Pfizer for neurological and psychiatric research. It has been studied for its potential in treating Alzheimer's disease and cognitive dysfunction. It is available for research use only.
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| Molecular Formula |
C18H24N2OF2.C7H8O3S
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|---|---|
| Molecular Weight |
494.59438
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| Exact Mass |
494.205
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| CAS # |
1039399-17-1
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| Related CAS # |
PF-03654746;935840-31-6
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| PubChem CID |
24862242
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| Appearance |
White to off-white solid powder
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| LogP |
6.233
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
34
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| Complexity |
626
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
IKAYTZLLIWAEDV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H24F2N2O.C7H8O3S/c1-2-21-17(23)14-10-18(20,11-14)15-6-5-13(16(19)9-15)12-22-7-3-4-8-22;1-6-2-4-7(5-3-6)11(8,9)10/h5-6,9,14H,2-4,7-8,10-12H2,1H3,(H,21,23);2-5H,1H3,(H,8,9,10)
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| Chemical Name |
N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]cyclobutane-1-carboxamide;4-methylbenzenesulfonic acid
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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) |
H2O : ≥ 8.4 mg/mL (~16.98 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 | 2.0219 mL | 10.1094 mL | 20.2188 mL | |
| 5 mM | 0.4044 mL | 2.0219 mL | 4.0438 mL | |
| 10 mM | 0.2022 mL | 1.0109 mL | 2.0219 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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