| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 250mg | |||
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| Targets |
4-PPBP maleate targets the σ1 receptor, a chaperone protein that modulates various signaling pathways, and the NR1a/2B NMDA receptor. It is a potent σ1 receptor ligand and agonist. Additionally, it acts as a selective non-competitive antagonist at recombinant NR1a/2B NMDA receptors expressed in Xenopus oocytes. This dual activity makes 4-PPBP maleate a valuable tool for studying both σ1 receptor and NMDA receptor function.
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| ln Vitro |
4-PPBP maleate causes phosphorylation of ERK1/2 in primary neurons [3].
In vitro, 4-PPBP maleate is a potent σ1 receptor ligand and agonist. It also acts as a selective non-competitive antagonist at recombinant NR1a/2B NMDA receptors expressed in Xenopus oocytes. These in vitro properties make 4-PPBP maleate a valuable tool for studying σ1 receptor and NMDA receptor function in neuropharmacology. |
| ln Vivo |
4-PPBP maleate (1 μmol/kg; intravenous injection) reduces brain damage after transient focal ischemia in rats [2].
In vivo, 4-PPBP maleate has been used in research on σ receptor and NMDA receptor function. It has been investigated for potential applications in treating wrinkled skin as a cosmetic agent. However, detailed in vivo efficacy data for therapeutic applications are limited in publicly available sources. |
| Enzyme Assay |
The in vitro receptor binding assay for 4-PPBP maleate involves measuring its binding affinity to the σ1 receptor. The compound is incubated with membranes expressing the σ1 receptor in the presence of a radiolabeled σ1 ligand (e.g., [3H](+)-pentazocine). Binding affinity (Ki) is determined using competition binding assays. For NMDA receptor activity, functional antagonism can be assessed using electrophysiological recordings in Xenopus oocytes expressing NR1a/2B receptors in the presence of the compound.
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| Cell Assay |
The in vitro cell-based assay for 4-PPBP maleate involves culturing cells expressing the σ1 receptor or NMDA receptors and treating them with the compound to assess effects on receptor function. For σ1 receptor activity, cells are treated with 4-PPBP maleate and σ1 receptor-mediated signaling (e.g., calcium mobilization or modulation of other receptors) is assessed. For NMDA receptor activity, cells expressing NR1a/2B are treated with the compound in the presence of NMDA and glycine, and calcium influx or electrophysiological responses are measured. Cell viability is assessed using MTT or CellTiter-Glo assays.
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| Animal Protocol |
Animal/Disease Models: Male rats weighing 300 to 385 grams (transient focal ischemia model) [2]
Doses: 1 μmol/kg Route of Administration: Continuous intravenous (iv) (iv)infusion every hour starting 1 hour after the onset of ischemia , continued until 22 hrs (hrs (hours)) of reperfusion. Experimental Results: Brain damage was diminished after transient focal ischemia in rats. In vivo animal studies for 4-PPBP maleate have not been extensively reported. If conducted, such studies might involve mouse or rat models of neurological or psychiatric disorders, where 4-PPBP maleate is administered and behavioral or biochemical endpoints are assessed. Standard protocols for these models would be employed. No specific data are available. |
| ADME/Pharmacokinetics |
4-PPBP maleate has a molecular weight of 409.52 and a molecular formula of C25H31NO4. It is soluble in ethanol and DMSO (up to 25 mM). The compound's pharmacokinetic properties, including oral bioavailability and half-life, have been characterized in preclinical studies. It can be formulated for in vivo administration.
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| Toxicity/Toxicokinetics |
The toxicity profile of 4-PPBP maleate has not been systematically evaluated. As a σ1 receptor ligand and NMDA receptor antagonist, its primary safety concerns would relate to effects on the central nervous system. Standard toxicology assessments would include acute and sub-chronic toxicity studies in rodents, with endpoints including clinical signs, body weight, clinical pathology, and histopathology. No specific toxicity data are available.
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| References |
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| Additional Infomation |
4-PPBP maleate is a research compound and has not been approved for clinical use. It is a potent σ1 receptor ligand and agonist and a selective non-competitive antagonist at NR1a/2B NMDA receptors. 4-PPBP maleate is a piperidine derivative used as a research tool for studying σ receptors and NMDA receptor function in neuropharmacology.
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| Molecular Formula |
C25H31NO4
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| Molecular Weight |
409.526
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| Exact Mass |
409.225
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| Elemental Analysis |
C, 73.32; H, 7.63; N, 3.42; O, 15.63
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| CAS # |
201216-39-9
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| PubChem CID |
11682970
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
30
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| Complexity |
399
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CN(CCC1C2=CC=CC=C2)CCCCC3=CC=CC=C3.C(=C\C(=O)O)\C(=O)O
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| InChi Key |
OASPNIMFGJVLES-BTJKTKAUSA-N
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| InChi Code |
InChI=1S/C21H27N.C4H4O4/c1-3-9-19(10-4-1)11-7-8-16-22-17-14-21(15-18-22)20-12-5-2-6-13-20;5-3(6)1-2-4(7)8/h1-6,9-10,12-13,21H,7-8,11,14-18H2;1-2H,(H,5,6)(H,7,8)/b;2-1-
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| Chemical Name |
4-Phenyl-1-(4-phenylbutyl)piperidine maleate
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| Synonyms |
4-PPBP maleate
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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 : ~250 mg/mL (~610.47 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 | 2.4418 mL | 12.2091 mL | 24.4182 mL | |
| 5 mM | 0.4884 mL | 2.4418 mL | 4.8836 mL | |
| 10 mM | 0.2442 mL | 1.2209 mL | 2.4418 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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