| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Collagen synthesis[1]
Isosaponarin targets the TGF-β type II receptor (TβR-II) and prolyl 4-hydroxylase (P4H), functioning as an agonist that promotes collagen synthesis. By up-regulating TβR-II and P4H protein production, isosaponarin increases type I collagen production at the mRNA level in human fibroblasts. It also inhibits the increase in Ca²⁺ levels induced by 4-aminopyridine in rat synaptosomes, reducing phosphorylation of PKC, PKCα, SNAP-25, and MARCKS, thereby inhibiting vesicular glutamate release. This neuroactive profile makes it a specialized tool for dermatological and neurological research. |
|---|---|
| ln Vitro |
In vitro, isosaponarin (0.001-0.1 µg/mL; 24 h) increases collagen synthesis in human fibroblasts, caused by up-regulated TβR-II and P4H production. It significantly increased TβR-II protein level at concentrations of 0.001-0.01 µg/mL and P4Hα(I) production at 0.01 µg/mL. Isosaponarin significantly up-regulated procollagen α1(I) mRNA at 0.001 µg/mL, TβR-II mRNA at 0.001 µg/mL, and P4Hα(I) mRNA at 0.001-0.1 µg/mL. It inhibits 4-AP-evoked glutamate release with a half-maximum inhibition value of 22 μM. It suppresses the Ca²⁺-dependent PKC/SNAP-25 and MARCKS pathways in synaptosomes.
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| ln Vivo |
In vivo, isosaponarin (50 mg/kg; oral administration; single dose) is metabolized to isovitexin in the intestine, and most of it is not absorbed and is excreted in feces. This indicates that isosaponarin has limited oral bioavailability and undergoes extensive intestinal metabolism. Despite this, isosaponarin-rich plants exhibit strong antimicrobial, antioxidant, anti-hyaluronidase, antiplatelet, anti-atopic dermatitis, and anti-tumor effects. Its topical application may be more effective for dermatological applications. Further studies are needed to fully characterize its in vivo efficacy.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for isosaponarin typically involve assessing its interaction with TGF-β type II receptor (TβR-II) and prolyl 4-hydroxylase (P4H). The compound's ability to up-regulate TβR-II and P4H protein production is assessed in human fibroblasts by Western blot. Its effects on collagen synthesis are measured by assessing procollagen α1(I) mRNA expression by RT-PCR. Binding affinity to TβR-II or P4H can be assessed using surface plasmon resonance (SPR) or other biophysical methods. Assays are conducted under appropriate conditions with proper controls.
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| Cell Assay |
In vitro cell-based assays for isosaponarin utilize human skin fibroblast cells to assess collagen synthesis and related protein expression. Cells are treated with isosaponarin at concentrations of 0.001-0.1 µg/mL for 24 hours. Collagen synthesis is measured by assessing procollagen α1(I) mRNA expression by RT-PCR. TβR-II and P4Hα(I) protein and mRNA levels are measured by Western blot and RT-PCR. For neuroactive studies, rat synaptosomes are treated with isosaponarin (10-100 µM) added 10 minutes before 4-aminopyridine addition, and glutamate release is measured. Standard cell culture conditions (37°C, 5% CO₂) with appropriate media are employed.
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| Animal Protocol |
In vivo animal studies with isosaponarin typically involve oral administration to rodent models to study its metabolism, absorption, and excretion. In one study, 6-week-old female ICR mice were given a single oral dose of 50 mg/kg isosaponarin. The compound's metabolism in the intestine, absorption, and excretion were studied. Results showed that isosaponarin is metabolized to isovitexin in the intestine, and most of it is not absorbed and is excreted in feces. For topical applications, isosaponarin may be evaluated in models of skin conditions such as atopic dermatitis. All procedures must comply with institutional animal care and use guidelines.
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| ADME/Pharmacokinetics |
Isosaponarin has a molecular weight of 594.52 g/mol and a molecular formula of C₂₇H₃₀O₁₅. It is soluble in DMSO at 100-125 mg/mL. The compound is typically stored as a powder at -20°C for up to 3 years or in solvent at -80°C for up to 1 year, protected from light. Following oral administration, isosaponarin is metabolized to isovitexin in the intestine, and most of it is not absorbed and is excreted in feces. This suggests limited oral bioavailability for systemic applications.
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| Toxicity/Toxicokinetics |
Isosaponarin is intended for research use only and is not approved for human therapeutic applications. As a natural product research chemical, comprehensive toxicological data are not extensively documented in the publicly accessible literature. Standard safety precautions should be observed when handling this compound, including the use of appropriate personal protective equipment. As with all research chemicals, comprehensive toxicological profiling would be required before any consideration for clinical development. The compound should be handled in well-ventilated areas with proper waste disposal procedures.
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| References | |
| Additional Infomation |
Isosaponins have been reported to be found in Gypsophila vaccaria, Cerastium arvense, and other organisms with available data.
Isosaponarin (CAS#: 19416-87-6) has a molecular formula of C₂₇H₃₀O₁₅ and a molecular weight of 594.52 g/mol. It is a flavone glycoside isolated from wasabi leaves. Isosaponarin is a P4HA2 enzymatic agonist that increases collagen synthesis via up-regulated TβR-II and P4H production. It inhibits glutamate release in synaptosomes through the PKC/SNAP-25 pathway. Isosaponarin-rich plants exhibit antimicrobial, antioxidant, anti-hyaluronidase, antiplatelet, anti-atopic dermatitis, and anti-tumor effects. This compound is not a drug and has not undergone clinical trials. |
| Molecular Formula |
C27H30O15
|
|---|---|
| Molecular Weight |
594.52
|
| Exact Mass |
594.158
|
| CAS # |
19416-87-6
|
| PubChem CID |
154105
|
| Appearance |
White to yellow solid powder
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| Density |
1.7±0.1 g/cm3
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| Boiling Point |
970.8±65.0 °C at 760 mmHg
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| Flash Point |
322.4±27.8 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
|
| Index of Refraction |
1.729
|
| LogP |
-0.83
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| Hydrogen Bond Donor Count |
10
|
| Hydrogen Bond Acceptor Count |
15
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| Rotatable Bond Count |
6
|
| Heavy Atom Count |
42
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| Complexity |
971
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| Defined Atom Stereocenter Count |
10
|
| SMILES |
C1=CC(=CC=C1C2=CC(=O)C3=C(O2)C=C(C(=C3O)[C@H]4[C@@H]([C@H]([C@@H]([C@H](O4)CO)O)O)O)O)O[C@H]5[C@@H]([C@H]([C@@H]([C@H](O5)CO)O)O)O
|
| InChi Key |
SFNFQCXADNWOCI-KETMJRJWSA-N
|
| InChi Code |
InChI=1S/C27H30O15/c28-7-15-19(32)22(35)24(37)26(41-15)18-12(31)6-14-17(21(18)34)11(30)5-13(40-14)9-1-3-10(4-2-9)39-27-25(38)23(36)20(33)16(8-29)42-27/h1-6,15-16,19-20,22-29,31-38H,7-8H2/t15-,16-,19-,20-,22+,23+,24-,25-,26+,27-/m1/s1
|
| Chemical Name |
5,7-dihydroxy-6-[(2S,3R,4R,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]-2-[4-[(2S,3R,4R,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyphenyl]chromen-4-one
|
| 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) |
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
|
|---|---|
| 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 | 1.6820 mL | 8.4101 mL | 16.8203 mL | |
| 5 mM | 0.3364 mL | 1.6820 mL | 3.3641 mL | |
| 10 mM | 0.1682 mL | 0.8410 mL | 1.6820 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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