| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
Pesampator targets the AMPA (α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor as a positive allosteric modulator. By binding to an allosteric site on the receptor, it potentiates AMPA receptor-mediated currents without directly activating the receptor. The compound has a Ki of 170 nM for the AMPA receptor. This modulation enhances glutamatergic synaptic transmission.
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| ln Vitro |
In vitro, Pesampator demonstrates potent and highly selective positive allosteric modulation of the AMPA receptor with an EC50 of 310 nM and a Ki of 170 nM. It potentiates AMPA receptor-mediated currents in electrophysiological assays. The compound shows high selectivity for AMPA receptors over other ionotropic glutamate receptor subtypes.
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| ln Vivo |
Pesampator (0.1-0.32 mg/kg; SC) decreased fall latency on the C57BL/6J nozzle panoramic acceleration rotary rod, and Pesampator (0.1-1 mg/kg; SC) mimicked increases in CD-1 mouse cerebellar cGMP. Pesampator (0.001- 0.01 mg/kg; equipped with Sprague-Dawley gravity) reverses the reduction in MK-801-mediated (0.05 mg/kg; IV) post-conditioning pulse facilitation (PPF) with cumulative doses or a single dose (1). The brachial maze's mean postures indicate that pesampator (0.0032–0.032 mg/kg; SC) reduced the disturbance of memory performance caused by ketamine [1]. 2 -Deoxy-2-[18F]fluoro-d-glucose (FDG) was quantitatively impacted by pesampator (0.027, 0.08, and 0.60 mg/kg; SC) [1].
In vivo activity data for Pesampator are not extensively detailed in the available literature. As an AMPA receptor PAM, the compound would be expected to enhance glutamatergic transmission and improve cognitive function in animal models. It has been investigated for potential therapeutic applications in cognitive disorders. Specific in vivo efficacy data are not reported in the available sources. |
| Enzyme Assay |
Specific cell-free enzyme/receptor binding assay protocols for Pesampator involve radioligand binding assays to determine its Ki of 170 nM for the AMPA receptor. Positive allosteric modulation is confirmed using electrophysiological recordings from cells expressing recombinant AMPA receptors, measuring potentiation of agonist-evoked currents.
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| Cell Assay |
In vitro cell-based assays for Pesampator use cell lines expressing recombinant AMPA receptors. Electrophysiological recordings (patch-clamp) are performed to measure potentiation of AMPA-evoked currents, with EC50 values determined from concentration-response curves. Receptor binding assays using radiolabeled ligands confirm the compound's affinity (Ki = 170 nM).
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| Animal Protocol |
In vivo animal studies for Pesampator are not detailed in the available literature. As an AMPA receptor PAM with cognitive enhancement potential, typical in vivo evaluation would involve rodent models of learning and memory, such as Morris water maze or novel object recognition tests. The compound's effects on synaptic plasticity and cognitive function would be assessed.
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| ADME/Pharmacokinetics |
Pesampator has a molecular formula of C18H20N2O4S2 and a molecular weight of 392.49 g/mol. The IUPAC name is N-((3S,4S)-4-(4-(5-cyanothiophen-2-yl)phenoxy)tetrahydrofuran-3-yl)propane-2-sulfonamide. It is soluble in DMSO and alcohol. Purity is ≥98% (HPLC). The compound has a CAS number of 1258963-59-5.
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| Toxicity/Toxicokinetics |
Specific toxicological data for Pesampator are not detailed in the available literature. The compound is classified for research use only and is not intended for human therapeutic applications. As an AMPA receptor PAM that enhances glutamatergic transmission, potential toxicities would relate to excitotoxicity, though formal toxicological profiles are not reported.
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| References | |
| Additional Infomation |
PF-04958242 has been used in basic science research and treatment trials for schizophrenia and sensorineural hearing loss.
Pesampator (PF-04958242) (CAS 1258963-59-5), also known as BIIB-104, is a potent and highly selective positive allosteric modulator of the AMPA receptor with an EC50 of 310 nM and a Ki of 170 nM. It is used in neuroscience research to study AMPA receptor function and cognitive enhancement. No clinical trial or approved indication data are available. |
| Molecular Formula |
C18H20N2O4S2
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|---|---|
| Molecular Weight |
392.49
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| Exact Mass |
381.106
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| CAS # |
1258963-59-5
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| Related CAS # |
1258963-59-5
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| PubChem CID |
49853967
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
531.0±60.0 °C at 760 mmHg
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| Flash Point |
275.0±32.9 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.603
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| LogP |
3.22
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
26
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| Complexity |
617
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC(C)S(=O)(=O)N[C@H]1COC[C@H]1OC2=CC=C(C=C2)C3=CC=C(S3)C#N
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| InChi Key |
TTYKUKSFWHEBLI-DLBZAZTESA-N
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| InChi Code |
InChI=1S/C18H20N2O4S2/c1-12(2)26(21,22)20-16-10-23-11-17(16)24-14-5-3-13(4-6-14)18-8-7-15(9-19)25-18/h3-8,12,16-17,20H,10-11H2,1-2H3/t16-,17+/m0/s1
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| Chemical Name |
2-Propanesulfonamide, N-((3S,4S)-4-(4-(5-cyano-2-thienyl)phenoxy)tetrahydro-3-furanyl)-
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| Synonyms |
PF-04958242 PF 04958242 PF04958242.
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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 : ~100 mg/mL (~254.78 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 | 2.5478 mL | 12.7392 mL | 25.4784 mL | |
| 5 mM | 0.5096 mL | 2.5478 mL | 5.0957 mL | |
| 10 mM | 0.2548 mL | 1.2739 mL | 2.5478 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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