2. NF-κB
  3. Keap1-Nrf2
  4. Chikusetsusaponin Iva

Chikusetsusaponin Iva  (Synonyms: Calenduloside F)

Cat. No.: HY-N0818 Purity: 98.95%
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Chikusetsusaponin IVa is an orally active protein kinase activator. Chikusetsusaponin IVa binds to YAP with a KD value of 0.388 mM. Chikusetsusaponin IVa reduces inflammatory mediators (IL-6, IL-10, COX-2) expression, NO production, promotes ROS generation, induces Apoptosis, inhibits MAPK, TAZ, and regulates Nrf2, JAK/STAT. Chikusetsusaponin Iva has anti-H9N2 AIV and anti-endometrial cancer activities. Chikusetsusaponin Iva shows anti-inflammatory, hepatoprotective and osteoprotective effects.

For research use only. We do not sell to patients.

Chikusetsusaponin Iva Chemical Structure

Chikusetsusaponin Iva Chemical Structure

CAS No. : 51415-02-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 2 publication(s) in Google Scholar

Other Forms of Chikusetsusaponin Iva:

Chikusetsusaponin Iva Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Chikusetsusaponin IVa is an orally active protein kinase activator. Chikusetsusaponin IVa binds to YAP with a KD value of 0.388 mM. Chikusetsusaponin IVa reduces inflammatory mediators (IL-6, IL-10, COX-2) expression, NO production, promotes ROS generation, induces Apoptosis, inhibits MAPK, TAZ, and regulates Nrf2, JAK/STAT. Chikusetsusaponin Iva has anti-H9N2 AIV and anti-endometrial cancer activities. Chikusetsusaponin Iva shows anti-inflammatory, hepatoprotective and osteoprotective effects[1][2][3][4][5][6][7][8][9][10].

Cellular Effect
Cell Line Type Value Description References
HCT-116 IC50
78.11 μM
Compound: 11
Cytotoxicity against human HCT116 cells by MTT assay
Cytotoxicity against human HCT116 cells by MTT assay
[PMID: 20951582]
HL-60 IC50
76.23 μM
Compound: 11
Cytotoxicity against human HL60 cells by MTT assay
Cytotoxicity against human HL60 cells by MTT assay
[PMID: 20951582]
Neutrophil IC50
4.76 μM
Compound: 6
Inhibition of fMLP/CB-activated human neutrophil degranulation assessed as inhibition of elastase release using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as a substrate after 5 mins
Inhibition of fMLP/CB-activated human neutrophil degranulation assessed as inhibition of elastase release using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as a substrate after 5 mins
[PMID: 21417387]
In Vitro

Chikusetsusaponin Iva (12.5-50 μM; 24 h) induces apoptosis in endometrial cancer cells (HEC1B) via promoting ROS production[1].
Chikusetsusaponin IVa (3.75-60 μg/mL) shows inhibitory effects on H9N2 AIV in A549 cells, with TI values of 4.00 (co-treatment) and 6.29 (posttreatment)[2].
Chikusetsusaponin IVa (50-200 μg/mL; 24 h) shows inhibitory effects on lipopolysaccharide-induced proinflammatory responses in THP-1 cells[3].
Chikusetsusaponin IVa binds to YAP with a KD of 0.388 mM[4].
Chikusetsusaponin IVa (10-40 μM; 24 h) increases the viability of Palmitic acid (HY-N0830)-damaged HepG2 cells and primary mouse hepatocytes and reduces LDH levels in culture supernatants[6].
Chikusetsusaponin Iva (3.125-12.5 μg/mL; 1 h) inhibits inflammatory responses in LPS-stimulated RAW264.7 cell line by inhibiting MAPK pathway[7].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chikusetsusaponin Iva Related Antibodies

Western Blot Analysis[1]

Cell Line: HEC1B
Concentration: 0 μM, 12.5 μM, 25 μM, 50 μM
Incubation Time: 24 h
Result: Decreased the phosphorylation levels of p38, ERK and JNK in a dose-dependent way.
Decreased the expression of Bcl-2 and increases the expression of Bax and cleaved caspase-3.
In Vivo

Chikusetsusaponin IVa (15-60 mg/kg; p.o.; once daily; 5 consecutive days) mitigates pulmonary impairment, improves the organism’s antioxidant activity, and regulates the Nrf2 and MAPK signaling pathways in lung tissue of H9N2 AIV-infected mice[2].
Chikusetsusaponin IVa (10-40 mg/kg; p.o.; daily; 14 days after BDL) significantly alleviates liver fibrosis and injury in CCl4 (HY-Y0298)-challenged and bile duct ligation (BDL)-induced liver fibrosis mouse models by downregulating YAP and TAZ expression[4].
Chikusetsusaponin IVa (50-100 mg/kg; from day 28 to day 40) shows anti-inflammatory and osteoprotective effects on rheumatoid arthritis via the JAK/STAT signaling pathway in mice[5].
Chikusetsusaponin IVa (50 mg/kg; i.g.; 8 weeks) can improve the symptoms of mice with high-fat diet (HFD)-induced metabolic dysfunction-associated steatotic liver disease (MASLD)[6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: DBA 1/J male mice (18-22 g, 6-8 weeks old) + Collagen (HY-NP102)-induced arthritis (CIA) model[5]
Dosage: 50 mg/kg、100 mg/kg
Administration: days 28-40
Result: Significantly reduced the arthritis index, hind paw thickness, and the number of swollen joints.
Decreased the immune organ index in a dose-dependent manner.
Reduced the concentration of inflammatory factors in peripheral serum and suppressed the mRNA expression of these factors in the spleen.
Inhibited the protein expression level of the JAK/STAT pathway.
Animal Model: C57BL/6J male mice (weight 20 g, 8-12 weeks old) + high-fat diet-induced metabolic dysfunction-associated fatty liver disease (MASLD) model[6]
Dosage: 50 mg/kg
Administration: Intragastric administration, 8 weeks
Result: Significantly reduced body weight and liver weight gains.
Decreased serum aspartate transaminase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP), γ-glutamyl transpeptidase (γ-GT), triacylglycerol (TG), total cholesterol (CHO), high-density lipoprotein cholesterol (HDL), low-density lipoprotein cholesterol (LDL), and nonesterified fatty acids (NEFAs) levels. Alleviated HFD-induced hepatic steatosis, inflammation, and fibrosis.
Improved glucose tolerance and insulin resistance.
Molecular Weight

794.97

Formula

C42H66O14
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@]1(CCC(C)(C)C2)[C@]2([H])C3=CC[C@@]4([H])[C@@](C)(CC[C@]5([H])[C@@]4(CC[C@H](O[C@]([C@@H]([C@@H](O)[C@@H]6O)O)([H])O[C@@H]6C(O)=O)C5(C)C)C)[C@]3(C)CC1)O[C@@H]([C@@H]([C@@H](O)[C@@H]7O)O)O[C@@H]7CO
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (125.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2579 mL 6.2895 mL 12.5791 mL
5 mM 0.2516 mL 1.2579 mL 2.5158 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (3.14 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (3.14 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
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+
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.2579 mL 6.2895 mL 12.5791 mL 31.4477 mL
5 mM 0.2516 mL 1.2579 mL 2.5158 mL 6.2895 mL
10 mM 0.1258 mL 0.6290 mL 1.2579 mL 3.1448 mL
15 mM 0.0839 mL 0.4193 mL 0.8386 mL 2.0965 mL
20 mM 0.0629 mL 0.3145 mL 0.6290 mL 1.5724 mL
25 mM 0.0503 mL 0.2516 mL 0.5032 mL 1.2579 mL
30 mM 0.0419 mL 0.2097 mL 0.4193 mL 1.0483 mL
40 mM 0.0314 mL 0.1572 mL 0.3145 mL 0.7862 mL
50 mM 0.0252 mL 0.1258 mL 0.2516 mL 0.6290 mL
60 mM 0.0210 mL 0.1048 mL 0.2097 mL 0.5241 mL
80 mM 0.0157 mL 0.0786 mL 0.1572 mL 0.3931 mL
100 mM 0.0126 mL 0.0629 mL 0.1258 mL 0.3145 mL
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Chikusetsusaponin Iva Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Chikusetsusaponin Iva51415-02-2Calenduloside FKeap1-Nrf2MASLDanti-inflammatoryosteoprotectiveliver fibrosisA549HEC1BHepG2Inhibitorinhibitorinhibit

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