| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
(−)-P7C3-S243 (compound 15) exhibited weak inhibitory activity against CYP1A2 (IC50 = 20 μM) and CYP2C19 (IC50 = 1.9 μM) in vitro, but no inhibitory activity against many other tested CYP subtypes [1]. (−)-P7C3-S243 bound to μ-opioid receptors (IC50 = 8.2 μM) and TSPO (IC50 = 0.35 μM) in vitro, but did not bind to most other tested neuronal receptors and channels [1].
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| ln Vivo |
(−)-P7C3-S243 (10 μM (12 μL/day)/0.1-10 mg/kg/day; intraventricular/peritoneal injection; twice daily for 7 days) doubled the number of surviving newborn hippocampal neurons and improved the survival rate of hippocampal neurons in environmentally deprived mice[1]. (−)-P7C3-S243 (1-10 mg/kg; intraperitoneal injection; twice daily for 21 days) dose-dependently protected mature dopaminergic neurons in the substantia nigra of MPTP-treated mice[1]. (−)-P7C3-S243 (10 mg/kg; intraperitoneal injection; 10 days) doubled the level of postnatal hippocampal neurogenesis in TgF344-AD rats, protected rats from early depressive-like behavior and late cognitive impairment, reduced neurodegeneration and neuronal loss, and improved age-related depressive-like behavior in wild-type rats[2].
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| Animal Protocol |
Animal/Disease Models:C57BL/J6 (12 weeks old) [1]
Doses: 10 μM; 0.1-10 mg/kg/day Route of Administration: Intraventricular injection; 0.5 μL/h; 7 days; Intraperitoneal injection; twice daily; 7 days Experimental Results: Compared with the control group mice, the number of surviving BrdU+ neonatal hippocampal neurons was approximately doubled. The dose-response curve was smooth, with activity detectable at 1 mg/kg/day and maximum efficacy achieved at 10 mg/kg/day; the efficacy reflected an increase in the survival rate of neonatal hippocampal neurons through neuroprotective effects (rather than increased proliferation). Animal/Disease Models:C57Bl/6 (adult male; MPTP-induced Parkinson's disease) [1] Doses: 1, 3, 5, 10 mg/kg/day Route of Administration: Intraperitoneal injection; twice daily for 21 days Experimental Results: Significant neuroprotective activity was observed at a dose of 1 mg/kg/day, and at the highest tested dose of 10 mg/kg/day, more than 85% of TH+ dopaminergic neurons in the substantia nigra were rescued (compared to the MPTP-treated vector control group); it showed higher efficacy than P7C3-A20 and had strict enantiomer specificity (only the (−)-S enantiomer was active). Animal/Disease Models:Fischer 344 rats (male and female, 6 months old at the start of treatment; TgF344-AD transgenic rats overexpressing human mutant APP_SW and PS1ΔE9 genes; wild type) [2] Doses: 10 mg/kg/d Route of Administration: Once daily for 9 months (assessed at 15 months); for 18 months (assessed at 24 months) Experimental Results: At 15 months, TgF344-AD transgenic rats showed a reduction in immobility time in the Porsolt forced swimming test to levels comparable to wild-type rats. No motor activity or cognitive deficits were observed in any group at 15 months. TgF344-AD rats showed improved performance in the Morris water maze reverse memory test, with the time required to locate the target location reduced to levels similar to 24-month-old wild-type (WT) rats. In 24-month-old WT rats, the drug improved depressive-like behavior, reducing the mean resting time in the Porsolt forced swimming test from 45 seconds to 20 seconds (p=0.0176), but did not improve depressive-like behavior in 24-month-old TgF344-AD rats. In 24-month-old TgF344-AD rats, the drug significantly reduced vacuolar formation in the hippocampus and cerebral cortex. In 24-month-old TgF344-AD rats, the drug prevented neuronal loss in the hippocampus and cerebral cortex and increased the number of neurons in the granular cell layer of the dentate gyrus. At 24 months, amyloid plaque deposition, soluble or insoluble Aβ1-40/Aβ1-42 peptide levels, tau hyperphosphorylation (Tau PS199/202), or glial cell activation (GFAP+ astrocytes or Iba1+ microglia) were not altered in TgF344-AD rats. |
| References |
|
| Molecular Formula |
C21H18BR2FN3O
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|---|---|
| Molecular Weight |
507.19
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| CAS # |
1597443-57-6
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
F[C@@H](CNC1=NC(OC)=CC=C1)CN2C3=CC=C(Br)C=C3C4=C2C=CC(Br)=C4
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 1.9716 mL | 9.8582 mL | 19.7165 mL | |
| 5 mM | 0.3943 mL | 1.9716 mL | 3.9433 mL | |
| 10 mM | 0.1972 mL | 0.9858 mL | 1.9716 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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