1. Metabolic Enzyme/Protease Neuronal Signaling Apoptosis Immunology/Inflammation
  2. Lactate Dehydrogenase α-synuclein Apoptosis Caspase Interleukin Related Phosphatase NOD-like Receptor (NLR)
  3. Senkyunolide A

Senkyunolide A is a phthalein compound. Senkyunolide A inhibits the proliferation of tumor cells and has anticancer activity. Senkyunolide A inhibits the progression of osteoarthritis through the NLRP3 signaling pathway. Senkyunolide A protects nerve cells from Corticosterone (HY-B1618) -induced apoptosis by regulating protein phosphatase 2A and α-synuclein signaling pathways. Senkyunolide A inhibits the expression of CD137, a diagnostic biomarker for atherosclerosis.

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Senkyunolide A Chemical Structure

Senkyunolide A Chemical Structure

CAS No. : 63038-10-8

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Based on 2 publication(s) in Google Scholar

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Description

Senkyunolide A is a phthalein compound. Senkyunolide A inhibits the proliferation of tumor cells and has anticancer activity. Senkyunolide A inhibits the progression of osteoarthritis through the NLRP3 signaling pathway. Senkyunolide A protects nerve cells from Corticosterone (HY-B1618) -induced apoptosis by regulating protein phosphatase 2A and α-synuclein signaling pathways. Senkyunolide A inhibits the expression of CD137, a diagnostic biomarker for atherosclerosis[1][2][3][4][5].

IC50 & Target[4]

Caspase-1

 

NLRP3

 

In Vitro

Senkyunolide A (0-2.5 μg/mL; 24 h) inhibits the proliferation of HT-29 and CCD-18Co cells with IC50 of 10.4 μM and 20.95 μM, respectively [1].
Senkyunolide A (100 μM; 6 h) inhibits the high expression of CD137 in TNF-α treated MAECs cells[2].
Senkyunolide A (0.125-0.5 μg/mL; 24-72 h) improves cell viability, decreases apoptosis, LDH release, α-syn expression and PP2P phosphorylation in PC12 cells treated with corticosterone (HY-B1618)[3].
Senkyunolide A (20-80 μg/mL; 48 h) promotes cell proliferation and inhibits cell apoptosis in IL-1β-treated chondrocytes, and inhibits cell inflammation by blocking the NLRP3 signaling pathway[4].

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

Western Blot Analysis[4]

Cell Line: Chondrocytes
Concentration: 20, 40 and 80 μg/mL
Incubation Time: 48 h
Result: Decreased the levels of NLRP3, ASC and caspase-1.
Reduced the levels of TNF-a, IL-6 and IL-18.
Parmacokinetics
Catalog_No Species Routes PKIndicators IndicatorName DoseUnit1 ValueUnit2
HY-N0743 rat Intravenous injection 20 mg/kg
HY-N0743 rat Intravenous injection Tmax Tmax 20 mg/kg /
HY-N0743 rat Intravenous injection Cmax Cmax 20 mg/kg /
HY-N0743 rat Intravenous injection T1/2 T1/2 20 mg/kg 0.65 hr
HY-N0743 rat Intravenous injection AUC AUC(0-∞) 20 mg/kg 2.81 mg·h/L
HY-N0743 rat Intravenous injection Vd Vd/F 20 mg/kg 6.74
HY-N0743 rat Intravenous injection Clearance (CL) CL/F 20 mg/kg 7.20 L/h
HY-N0743 rat Intravenous injection Bioavailability F 20 mg/kg / %
In Vivo

Senkyunolide A (20-40 mg/kg; Intraperitoneal injection; 1 week) shows improvement in the mouse model of osteoarthritis[4].
Pharmacokinetic Analysis in Rats[5]

Route Dose (mg/kg) Tmax (h) Cmax (mg/L) t1/2 (h) AUC0→∞ (mg/h per liter) Vd/F (L/kg) CL/F (L/h per kilogram) F (%)
i.v. 20 (pure) / 19.67 0.65 2.81 6.74 7.20 /
i.v. 7.65 (ext)* / 4.86 0.69 0.95 7.12 9.17 /
i.p. 50 0.04 17.60 0.67 5.29 9.98 10.92 75.3
i.p. 100 0.04 31.01 0.99 10.65 13.78 9.72 75.8
p.o. 100 0.21 1.66 0.52 1.11 68.97 94.81 7.9
*The herbal extract containing 7.65% of senkyunolide A was given at a dose of 100 mg/kg.

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

Animal Model: Male C57BL/6 mice (200-220 g) with osteoarthritis[4]
Dosage: 20 and 40 mg/kg
Administration: Intraperitoneal injection (i.p.); 1 week
Result: Alleviated articular cartilage destruction by inhibiting NLRP3 signalling pathway.
Significantly reduced the levels of NLRP3, ASC and caspase-1.
Molecular Weight

192.26

Formula

C12H16O2

CAS No.
Appearance

Liquid (Density: 1.1±0.1 g/cm3)

Color

Colorless to light yellow

SMILES

O=C1O[C@@H](CCCC)C2=C1C=CCC2

Structure Classification
Initial Source
Shipping

Shipping with dry ice.

Storage

-80°C, protect from light, stored under nitrogen

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (520.13 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 5.2013 mL 26.0067 mL 52.0134 mL
5 mM 1.0403 mL 5.2013 mL 10.4027 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, 6 months (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months.

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  • Dilution Calculator

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

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

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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 (13.00 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 (13.00 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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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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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

Purity: 99.92%

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, 6 months (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 5.2013 mL 26.0067 mL 52.0134 mL 130.0336 mL
5 mM 1.0403 mL 5.2013 mL 10.4027 mL 26.0067 mL
10 mM 0.5201 mL 2.6007 mL 5.2013 mL 13.0034 mL
15 mM 0.3468 mL 1.7338 mL 3.4676 mL 8.6689 mL
20 mM 0.2601 mL 1.3003 mL 2.6007 mL 6.5017 mL
25 mM 0.2081 mL 1.0403 mL 2.0805 mL 5.2013 mL
30 mM 0.1734 mL 0.8669 mL 1.7338 mL 4.3345 mL
40 mM 0.1300 mL 0.6502 mL 1.3003 mL 3.2508 mL
50 mM 0.1040 mL 0.5201 mL 1.0403 mL 2.6007 mL
60 mM 0.0867 mL 0.4334 mL 0.8669 mL 2.1672 mL
80 mM 0.0650 mL 0.3251 mL 0.6502 mL 1.6254 mL
100 mM 0.0520 mL 0.2601 mL 0.5201 mL 1.3003 mL
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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.

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Senkyunolide A
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