| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
Pirepemat fumarate targets monoaminergic systems in the brain, displaying its highest in vitro affinities for 5-HT and NA-related targets. It is a cortical-preferring catecholamine transmission- and cognition-promoting agent. It may act by modulating cortical catecholamine levels, improving cognitive function in conditions associated with monoaminergic hypofunction.
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| ln Vitro |
The compound with the highest in vitro affinity for targets associated to 5-HT and NA is IRL752 fumarate [2].
In vitro, Pirepemat fumarate displays its highest affinities for 5-HT and NA-related targets. It is a cortical-preferring catecholamine- and cognition-promoting agent. Detailed in vitro activity data, including specific receptor binding affinities and functional assays, are limited in the available literature. |
| ln Vivo |
IRL752 (3.7-100 µmol/kg, subcutaneous injection) fumarate can reverse deficits caused by monoaminergic hypofunction, but it has no discernible effect on acute hyperdopaminergic or hypoglutamatergic motor responses [2].
In vivo, Pirepemat fumarate can be used in Parkinson's disease (PD) research. Subcutaneous administration can reverse deficits caused by monoaminergic hypofunction, but it has no discernible effect on acute hyperdopaminergic or hypoglutamatergic motor responses. It is a cortical-preferring catecholamine and cognition-promoting agent. |
| Enzyme Assay |
Pirepemat fumarate's receptor binding affinities can be characterized using radioligand binding assays. The compound's highest affinities are for 5-HT and NA-related targets. Functional assays may measure the compound's effects on neurotransmitter release or receptor signaling.
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| Cell Assay |
In vitro cell experiments with Pirepemat fumarate involve treating neuronal cells with the compound and assessing its effects on neurotransmitter signaling and cellular function. The compound's effects on 5-HT and NA-related pathways are studied.
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| Animal Protocol |
Animal/Disease Models: normal rats [2]
Doses: 3.7-100 µmol/kg Route of Administration: subcutaneous injection, 30 minutes before test Experimental Results: Caused dose-dependent and regional-selective changes in brain monoamine transport index and gene expression. In vivo animal studies with Pirepemat fumarate have been conducted using Parkinson's disease models. The compound is typically administered via subcutaneous injection. It can reverse deficits caused by monoaminergic hypofunction. |
| ADME/Pharmacokinetics |
Pharmacokinetic data specific to Pirepemat fumarate are limited in the available literature. As a small molecule, the compound is expected to have reasonable oral bioavailability and blood-brain barrier penetration. Further pharmacokinetic studies are needed.
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| Toxicity/Toxicokinetics |
Pirepemat fumarate is considered safe for research use at typical concentrations. As a research compound, it is intended for laboratory use only and not for human consumption. The compound should be handled under standard laboratory safety practices.
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| References |
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| Additional Infomation |
Pirepemat fumarate (IRL752 fumarate) is a cortical-preferring catecholamine- and cognition-promoting agent. It can be used in Parkinson's disease study. It displays its highest in vitro affinities for 5-HT and NA-related targets. It can reverse deficits caused by monoaminergic hypofunction.
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| Molecular Formula |
C15H17F2NO5
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|---|---|
| Molecular Weight |
329.30
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| Exact Mass |
329.107
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| CAS # |
2251806-70-7
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| Related CAS # |
Pirepemat;1227638-29-0
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| PubChem CID |
163408775
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
23
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| Complexity |
346
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CO[C@@]1(CCNC1)C2=C(C(=CC=C2)F)F.C(=C/C(=O)O)\C(=O)O
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| InChi Key |
FHXIIHXNSWGBPV-KGLGULAYSA-N
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| InChi Code |
InChI=1S/C11H13F2NO.C4H4O4/c1-15-11(5-6-14-7-11)8-3-2-4-9(12)10(8)13;5-3(6)1-2-4(7)8/h2-4,14H,5-7H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1+/t11-;/m1./s1
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| Chemical Name |
(E)-but-2-enedioic acid;(3S)-3-(2,3-difluorophenyl)-3-methoxypyrrolidine
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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 : ~100 mg/mL (~303.67 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.59 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 25.0 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: ≥ 2.5 mg/mL (7.59 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 25.0 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: ≥ 2.5 mg/mL (7.59 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 | 3.0367 mL | 15.1837 mL | 30.3674 mL | |
| 5 mM | 0.6073 mL | 3.0367 mL | 6.0735 mL | |
| 10 mM | 0.3037 mL | 1.5184 mL | 3.0367 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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