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Triptolide-4-acetate

Cat No.:V16857 Purity: ≥98%
Triptolide is a diterpene triepoxide found in the roots of Tripterygium wilfordii and has immunosuppressive, anti~inflammatory, anti-proliferation and anti-tumor effects.
Triptolide-4-acetate
Triptolide-4-acetate Chemical Structure CAS No.: 38748-32-2
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
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InvivoChem's Triptolide-4-acetate has been cited by 1 publication
Product Description
Triptolide is a diterpene triepoxide found in the roots of Tripterygium wilfordii and has immunosuppressive, anti~inflammatory, anti-proliferation and anti-tumor effects. Triptolide is an inhibitor (blocker/antagonist) of NF-κB activation.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
Treatment with triptolide of primary chronic leukemia (CLL) B cells and CD19+ B cells induced in cell cultures. Triptolide in cultures at high risk. (n =5) and low-risk CLL (n =12) B cells (10–50 nM range) with a significant degree of normal B cell sparing (n = 5). Triptolide therapy has the ability to stop heat shock-induced HSP expression, which is consistent with the transcription of heat shock-induced HSP [1]. A natural substance called triptolide is obtained from the Chinese plant Tripterygium wilfordii, and it has been shown to have anticancer effects on a number of cancer types. In acute liver cancer (ALL) cells, triptolide decreases MDM2 expression in a dose-dependent manner, even at low doses of 20–100 nM. With IC50 values ranging from 47 to 73 nM, triptolide demonstrated potent cytotoxic action in all eight native MDM2-expressing cell lines. When MDM2 was stable transfected, triptolide efficiently killed EU-4 cells with very low triptolide levels (IC50 value: 725 nM vs. 88 nM), making MDM2 less cytotoxic in these cells [2]. For a whole day, secreted PC12 cells were kept sterile with varying triptolide doses (0.01, 0.1, and 1 nM) in the presence of 10 μM Aβ25-35. Tripterygium wilfordii can be detected by the MTT method, and the results indicated that Aβ25-35 can decrease cell viability. Following tetracycline treatment, the viability of secretory PC12 cells increased dramatically. The outcomes demonstrate that triptolide can lessen the harm that Aβ25–35 causes to cells, suggesting that triptolide protects against nerve injury [3].
ln Vivo
After mice were injected intravenously with triptolide (TP), the concentration of TP rapidly decreased. In all three groups, triptolide concentrations dropped below the lower limit of measurement two hours after injection. In order to determine if P-mdr1a-siRNA therapy significantly boosted triptolide sodium induction, parameter comparisons between the desert and treatment groups were conducted. The results showed an increase in Cmax from 413±74 to 510±94 ng/mL (P<0.05) and an increase in AUC from 103.5±9.6 to 154.3±30.2 ng h/mL (P<0.05). The concurrent group with Tariquidar likewise showed a noteworthy rise in AUC, going from 103.5±9.6 ng h/mL in the control group to 145.9±24.6 ng h/mL in the triptolide + Tariquidar group. Triptolide clearance in the mouse model was thus dramatically decreased, going from 9564±1024.2 mL/min/kg in cardiac disease to 6576.4±1438.5 in league (P<0.05) and 5755.4±1200.1 in mice overall. triptolide+Tariquidar and triptolide+mdr1a-siRNA groups showed mL/min / kg (P<0.05) [4].
References
[1]. Ganguly S, et al. Targeting HSF1 disrupts HSP90 chaperone function in chronic lymphocytic leukemia. Oncotarget. 2015 Oct 13;6(31):31767-79.
[2]. Huang M, et al. Triptolide inhibits MDM2 and induces apoptosis in acute lymphoblastic leukemia cells through a p53-independent pathway. Mol Cancer Ther. 2013 Feb;12(2):184-94.
[3]. Xu P, et al. Triptolide Inhibited Cytotoxicity of Differentiated PC12 Cells Induced by Amyloid-Beta25-35 via the Autophagy Pathway. PLoS One. 2015 Nov 10;10(11):e0142719.
[4]. Kong LL, et al. Inhibition of P-glycoprotein Gene Expression and Function Enhances Triptolide-induced Hepatotoxicity in Mice. Sci Rep. 2015 Jul 2;5:11747.
[5]. Zhang W, et al. Triptolide Combined with Radiotherapy for the Treatment of Nasopharyngeal Carcinoma via NF-κB-Related Mechanism. Int J Mol Sci. 2016 Dec 19;17(12). pii: E2139.
[6]. Cai J, et al. Natural product triptolide induces GSDME-mediated pyroptosis in head and neck cancer through suppressing mitochondrial hexokinase-ΙΙ. J Exp Clin Cancer Res. 2021;40(1):190. Published 2021 Jun 9
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C20H24O6
Molecular Weight
360.41
CAS #
38748-32-2
Related CAS #
Triptolide-d3
Appearance
Typically exists as solids (or liquids in special cases) at room temperature
SMILES
CC(C)[C@@]12[C@@H](O1)[C@H]3[C@@]4(O3)[C@]5(CCC6=C([C@@H]5C[C@H]7[C@]4([C@@H]2O)O7)COC6=O)C
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~25 mg/mL (~69.37 mM)
H2O : < 0.1 mg/mL
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 1.17 mg/mL (3.25 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 11.7 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.

Solubility in Formulation 2: ≥ 1.17 mg/mL (3.25 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 11.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.7746 mL 13.8731 mL 27.7462 mL
5 mM 0.5549 mL 2.7746 mL 5.5492 mL
10 mM 0.2775 mL 1.3873 mL 2.7746 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.

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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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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.
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