| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Other Sizes |
| Targets |
PKCα 19 μM (IC50)
Leucosceptoside A targets multiple proteins involved in metabolic and inflammatory pathways. It inhibits α-glucosidase, an enzyme that breaks down carbohydrates, contributing to its anti-hyperglycemic activity. It also inhibits PKCα (protein kinase C alpha) with an IC50 of 19.0 μM. Additionally, Leucosceptoside A modulates psoriasis-like inflammation by inhibiting the PI3K/AKT signaling pathway in keratinocytes. |
|---|---|
| ln Vitro |
Leucosceptoside A exhibits a minimal inhibitory impact on the angiotensin converting enzyme (ACE)[1]. The death of mesencephalic neurons mediated by 1-methyl-4-phenylpyridinium ion (MPP+) is considerably reduced by leucosceptoside A (4-16 μM)[2].
In vitro, Leucosceptoside A shows inhibitory activity against α-glucosidase and PKCα with IC50 values of 19.0 μM. It has anti-hyperglycemic and anti-hypertensive activities. Leucosceptoside A regulates psoriasis-like inflammation in keratinocytes by inhibiting the PI3K/AKT signaling pathway. These in vitro activities support its potential for studying metabolic disorders, hypertension, and inflammatory skin diseases. |
| ln Vivo |
In vivo data for Leucosceptoside A is not extensively reported in publicly available sources. As a phenylethanoid glycoside with anti-hyperglycemic, anti-hypertensive, and anti-inflammatory activities in vitro, the compound has potential applications in animal models of diabetes, hypertension, and psoriasis. However, specific published in vivo efficacy studies are not detailed in the current literature. Leucosceptoside A is primarily used as a research tool for studying metabolic and inflammatory pathways.
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| Enzyme Assay |
The in vitro enzyme inhibition assay for Leucosceptoside A uses α-glucosidase and PKCα enzymes. α-Glucosidase activity is measured using a chromogenic substrate such as p-nitrophenyl-α-D-glucopyranoside, and IC50 values are calculated from dose-response curves. PKCα activity is measured using a kinase assay with a peptide substrate. PI3K/AKT signaling inhibition is assessed in keratinocytes by Western blotting for phosphorylated AKT.
|
| Cell Assay |
Cellular assays for Leucosceptoside A are conducted in keratinocytes to study its effects on psoriasis-like inflammation. Cells are treated with varying concentrations of Leucosceptoside A, and inflammatory markers are measured by qPCR or ELISA. PI3K/AKT signaling is assessed by Western blotting for phosphorylated AKT and downstream targets. Cell viability is measured using standard assays such as MTT. α-Glucosidase inhibition is confirmed in cell-based models of glucose metabolism.
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| Animal Protocol |
In vivo studies for Leucosceptoside A would typically involve animal models of diabetes, hypertension, or psoriasis. The compound would be administered via oral or intraperitoneal routes at doses determined by pharmacokinetic studies. Efficacy would be assessed by measuring blood glucose levels, blood pressure, or skin inflammation. However, specific published in vivo protocols for Leucosceptoside A are not available in the current literature. The compound is currently used as a research tool.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Leucosceptoside A is not extensively reported in publicly available sources. The compound has a molecular weight of 638.61 g/mol and a molecular formula of C30H38O15. It has a CAS number of 83529-62-8. As a glycoside, it is expected to have moderate oral bioavailability. Detailed PK parameters such as half-life and bioavailability are not available in the current literature for this research compound.
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| Toxicity/Toxicokinetics |
Toxicity data for Leucosceptoside A is limited in publicly available sources. As a natural compound isolated from Oroxylum indicum, it is expected to have a favorable safety profile. However, as with all research compounds, Leucosceptoside A is intended for research use only and not for human therapeutic applications. Standard in vitro cytotoxicity assays and in vivo tolerability studies would be required for a complete toxicity assessment.
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| References |
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| Additional Infomation |
According to reports, leucopicrin A has been found in thornless amaranth, rehmannia, and other organisms with available data.
Leucosceptoside A (CAS 83529-62-8) is a phenylethanoid glycoside from Oroxylum indicum with anti-hyperglycemic and anti-hypertensive activities. It inhibits α-glucosidase and PKCα with an IC50 of 19.0 μM. It regulates psoriasis-like inflammation in keratinocytes by inhibiting PI3K/AKT signaling. It has a molecular formula of C30H38O15 and a molecular weight of 638.61 g/mol. Leucosceptoside A is a valuable research tool for studying metabolic and inflammatory diseases. |
| Molecular Formula |
C30H38O15
|
|---|---|
| Molecular Weight |
638.61
|
| Exact Mass |
638.221
|
| CAS # |
83529-62-8
|
| PubChem CID |
10394343
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.545g/cm3
|
| Boiling Point |
884.547ºC at 760 mmHg
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| Flash Point |
283.993ºC
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| Index of Refraction |
1.664
|
| Hydrogen Bond Donor Count |
8
|
| Hydrogen Bond Acceptor Count |
15
|
| Rotatable Bond Count |
12
|
| Heavy Atom Count |
45
|
| Complexity |
952
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| Defined Atom Stereocenter Count |
10
|
| SMILES |
O([C@@H]1O[C@@H](C)[C@H](O)[C@@H](O)[C@H]1O)[C@@H]1[C@@H](O)[C@H](OCCC2C=CC(O)=C(O)C=2)O[C@H](CO)[C@H]1OC(=O)/C=C/C1C=CC(O)=C(OC)C=1
|
| InChi Key |
ZMYQRHSOVRDQDL-CPPDSBOHSA-N
|
| InChi Code |
InChI=1S/C30H38O15/c1-14-23(36)24(37)25(38)30(42-14)45-28-26(39)29(41-10-9-16-3-6-17(32)19(34)11-16)43-21(13-31)27(28)44-22(35)8-5-15-4-7-18(33)20(12-15)40-2/h3-8,11-12,14,21,23-34,36-39H,9-10,13H2,1-2H3/b8-5+/t14-,21+,23-,24+,25+,26+,27+,28+,29+,30-/m0/s1
|
| Chemical Name |
[(2R,3R,4R,5R,6R)-6-[2-(3,4-dihydroxyphenyl)ethoxy]-5-hydroxy-2-(hydroxymethyl)-4-[(2S,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxyoxan-3-yl] (E)-3-(4-hydroxy-3-methoxyphenyl)prop-2-enoate
|
| 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 | 1.5659 mL | 7.8295 mL | 15.6590 mL | |
| 5 mM | 0.3132 mL | 1.5659 mL | 3.1318 mL | |
| 10 mM | 0.1566 mL | 0.7830 mL | 1.5659 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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