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Purity: ≥98%
P7C3 (P-7C3; P7 C-3; P 7C3) is a novel and potent proneurogenic and neuroprotective agent that acts by targeting the NAMPT (Nicotinamide phosphoribosyltransferase) enzyme. P 7C3 protects newborn neurons from apoptotic cell death, and promotes neurogenesis in mice and rats in the subgranular zone of the hippocampal dentate gyrus, the site of normal neurogenesis in adult mammals. P7C3 is orally available, nontoxic, stable in mice, rats, and cell culture, and capable of penetrating the blood-brain barrier.
| ln Vitro |
P7C3 prevents BV2 cells from producing pro-inflammatory factors when exposed to LPS [3]. In BV2 cells treated with 100 ng/mL of LPS, P7C3 dramatically and dose-dependently decreased the protein levels of iNOS and COX-2 without compromising cell viability [3]. In BV2 cells, P7C3 prevents LPS-induced nuclear translocation of the NF-κB p65 subunit [3]. By preventing IκB kinase (IKK) activation, P7C3 prevents LPS-induced inhibitory κB α (IκBα) degradation [3].
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| ln Vivo |
In vivo P7C3 (20 mg/kg/d; i.p.; twice daily; for 21 days) prevents the loss of dopaminergic (DA) neurons mediated by microglia and microglial activation [3].
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| Cell Assay |
Western Blot Analysis[3]
Cell Types: BV2 cells Tested Concentrations: 0.1 μM, 1 μM, 10 μM Incubation Duration: 2 hrs (hours) Experimental Results: decreased the protein levels of iNOS, COX-2. |
| Animal Protocol |
Animal/Disease Models: 6-8 weeks male C57BL/6 mice (25-30 g)[3]
Doses: 20 mg/kg/d Route of Administration: intraperitoneal (ip)injection, twice (two times) daily, for 21 days Experimental Results: Strikingly diminished the expressions of (a microglia marker) and GFAP (an astrocyte marker) LPS-induced in the substantia nigra pars compacta (SNpc). |
| References |
[1]. Pieper AA et al. Discovery of a proneurogenic, neuroprotective chemical. Cell. 2010 Jul 9;142(1):39-51.
[2]. Pieper AA et al. P7C3 and an unbiased approach to drug discovery for neurodegenerative diseases. Chem Soc Rev. 2014 Oct 7;43(19):6716-26. [3]. Chao Gu , et al. P7C3 Inhibits LPS-Induced Microglial Activation to Protect Dopaminergic Neurons Against Inflammatory Factor-Induced Cell Death in vitro and in vivo. Front Cell Neurosci. 2018; 12: 400. [4]. Blaya MO, Wasserman JM, Pieper AA, Sick TJ, Bramlett HM, Dietrich WD. Neurotherapeutic capacity of P7C3 agents for the treatment of Traumatic Brain Injury. Neuropharmacology. 2019;145(Pt B):268-282. |
| Molecular Formula |
C21H18BR2N2O
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| Molecular Weight |
474.19
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| CAS # |
301353-96-8
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| Related CAS # |
P7C3-A20;1235481-90-9
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| SMILES |
OC(CNC1=CC=CC=C1)CN2C3=C(C4=C2C=CC(Br)=C4)C=C(Br)C=C3
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1089 mL | 10.5443 mL | 21.0886 mL | |
| 5 mM | 0.4218 mL | 2.1089 mL | 4.2177 mL | |
| 10 mM | 0.2109 mL | 1.0544 mL | 2.1089 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.
Cell. 2014 Sep 11;158(6):1324-34. |
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P7C3-A20 enhances the flux of nicotinamide through the salvage pathway. Cell. 2014 Sep 11;158(6):1324-34. |
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