| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Perakine targets aldose reductase, a potent drug target for diabetes. Aldose reductase is an enzyme involved in the polyol pathway, which converts glucose to sorbitol. By inhibiting aldose reductase, Perakine may reduce the accumulation of sorbitol and prevent diabetic complications. The compound also serves as a substrate for Perakine reductase (PR), an aldo-keto reductase involved in ajmaline biosynthesis.
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| ln Vitro |
In vitro studies demonstrate that Perakine acts as an inhibitor of aldose reductase. The compound exhibits anti-inflammatory, analgesic, and antitumor properties. Its in vitro activity is assessed using aldose reductase enzyme assays, where the compound's ability to inhibit the enzyme is measured. Anti-inflammatory activity is evaluated in cell-based assays by measuring the inhibition of pro-inflammatory cytokine production. Antitumor activity is assessed in cancer cell lines using cell viability assays.
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| ln Vivo |
In vivo activity of Perakine has not been extensively characterized in the available literature. As an aldose reductase inhibitor with anti-inflammatory and antitumor properties, the compound has potential therapeutic applications in diabetes, inflammation, and cancer. However, detailed in vivo efficacy data are not extensively reported. The compound is primarily used as a research tool.
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| Enzyme Assay |
In vitro enzyme assays for Perakine involve measuring its inhibition of aldose reductase activity. The assay typically uses purified aldose reductase enzyme, a substrate (e.g., DL-glyceraldehyde), and NADPH. The compound is incubated with the enzyme and substrates, and the oxidation of NADPH is monitored spectrophotometrically at 340 nm. IC₅0 values are calculated from dose-response curves. The compound's activity as a substrate for Perakine reductase is assessed by measuring the NADPH-dependent reduction of Perakine to raucaffrinoline.
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| Cell Assay |
Cellular assays for Perakine are conducted to evaluate its anti-inflammatory and antitumor effects. Immune cells (e.g., macrophages) are treated with the compound and stimulated with LPS or other inflammatory stimuli. Cytokine production (e.g., TNF-alpha, IL-6) is measured by ELISA. Antitumor activity is assessed in cancer cell lines by treating cells with varying concentrations of the compound and measuring cell viability using MTT or similar assays. Apoptosis is evaluated by Annexin V/PI staining or caspase-3/7 activity.
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| Animal Protocol |
In vivo animal studies for Perakine are limited. For anti-inflammatory studies, animal models of inflammation could be used. For antitumor studies, xenograft models could be employed. For diabetes studies, animal models of diabetes could be used to assess the compound's effects on aldose reductase activity and diabetic complications. However, specific in vivo study protocols are not extensively reported.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Perakine have not been extensively characterized. The compound has a molecular weight of 350.41 and a molecular formula of C21H22N2O3. The compound is an indole alkaloid with moderate lipophilicity. Detailed PK parameters such as half-life, bioavailability, and volume of distribution are not reported in the available literature. The compound is typically stored at -20degC.
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| Toxicity/Toxicokinetics |
Toxicological data for Perakine are limited. The compound is not intended for human therapeutic use and is supplied for research purposes only. In cell-based assays, the compound is generally well-tolerated at concentrations used for activity studies. The compound is derived from Rauwolfia species, which contain various alkaloids with pharmacological activities. Standard safety precautions should be followed when handling this compound.
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| References | |
| Additional Infomation |
Perragin is an indole alkaloid with an ajemaran-type skeleton, characterized by the loss of 17α-acetoxy, 21β-methyl, and 1-methyl groups, as well as the corresponding unsaturated bond at N(1)=C(2), and the substitution of a 20α-formyl group for a 20β-ethyl side chain. It is derived from the hydride of ajemaran.
Perakine is an indole alkaloid from Rauwolfia species that inhibits aldose reductase and exhibits anti-inflammatory, analgesic, and antitumor properties. It is a substrate for Perakine reductase in ajmaline biosynthesis. The compound is not an FDA-approved drug and has no clinical indications. It is available in high purity (≥98%) and is typically stored at -20degC. |
| Molecular Formula |
C21H22N2O3
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|---|---|
| Molecular Weight |
350.4110
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| Exact Mass |
350.163
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| CAS # |
4382-56-3
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| PubChem CID |
56927765
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| Appearance |
White to off-white solid
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
492.8±45.0 °C at 760 mmHg
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| Flash Point |
251.9±28.7 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.805
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| LogP |
1.17
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
26
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| Complexity |
720
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| Defined Atom Stereocenter Count |
7
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| SMILES |
O(C(C([H])([H])[H])=O)C1([H])C23C4=C([H])C([H])=C([H])C([H])=C4N=C2C2([H])C([H])([H])C4([H])C([H])(C([H])=O)C([H])(C([H])([H])[H])N2C([H])(C3([H])[H])C41[H]
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| InChi Key |
GDXJMOGWONJRHL-HWUILILVSA-N
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| InChi Code |
InChI=1S/C21H22N2O3/c1-10-13(9-24)12-7-16-19-21(14-5-3-4-6-15(14)22-19)8-17(23(10)16)18(12)20(21)26-11(2)25/h3-6,9-10,12-13,16-18,20H,7-8H2,1-2H3/t10-,12?,13-,16-,17-,18?,20+,21+/m0/s1
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| Chemical Name |
[(1R,10S,13R,14S,16S,18R)-13-formyl-14-methyl-8,15-diazahexacyclo[14.2.1.01,9.02,7.010,15.012,17]nonadeca-2,4,6,8-tetraen-18-yl] acetate
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~50 mg/mL (~142.69 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.67 mg/mL (1.91 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 6.7 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: ≥ 0.67 mg/mL (1.91 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 6.7 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: ≥ 0.67 mg/mL (1.91 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 | 2.8538 mL | 14.2690 mL | 28.5380 mL | |
| 5 mM | 0.5708 mL | 2.8538 mL | 5.7076 mL | |
| 10 mM | 0.2854 mL | 1.4269 mL | 2.8538 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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