| Size | Price | Stock | Qty |
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| 1mg |
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| Targets |
Omtriptolide targets the same pathways as triptolide, which include inhibition of NF-κB activation, suppression of cytokine production, and induction of apoptosis. As a diterpene triepoxide, it has immunosuppressive and anti-inflammatory activities. Its mechanism involves inhibition of T-cell proliferation and modulation of multiple signaling pathways involved in inflammation and cell proliferation.
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| ln Vitro |
Triptolide is a traditional Chinese medicine that has pro-apoptotic, anti-inflammatory, and anti-proliferative effects [1].
In vitro, Omtriptolide exhibits the same activities as triptolide, including anti-inflammatory, antiproliferative, and proapoptotic properties. As a prodrug, it is converted to triptolide in vivo, which exerts the pharmacological effects. Its in vitro activity is assessed by measuring its effects on cell proliferation, cytokine production, and apoptosis in various cell types. |
| ln Vivo |
Oreprolactone significantly reduced blood urea nitrogen (BUN), serum creatinine, and acute tubular necrosis (ATN) scores in the cisplatin-induced AKI animal model; however, tubular apoptosis scores did not significantly decrease. Boost. Oraprolactone has a protective effect against AKI that is linked to p-ERK decrease and is not influenced by pro-inflammatory cytokines or MKP-1 [1]. Oreprolactone was found to decrease airway blockage and limit the buildup of inflammatory cells in a mouse model of obstructive airway disease using an ectopic tracheal allograft. This suggests that oreprolactone may have therapeutic or preventive benefits for individuals with obstructive airway disease who have had lung transplantation. therapeutic advantages [2]. When oraprolactone was given on the same day or five days after bleomycin, it prevented fibrosis in the bleomycin group. Additionally, omtriptolide dramatically decreased the myofibroblast count in the group that received bleomycin treatment [3]. When Vbeta3+ cell expansion is in the logarithmic phase (postoperative day 3), omtriptolide inhibits the expansion of CD4+Vbeta3+ and CD8+Vbeta3+ T cells (alloreactive T cells in this paradigm) in the spleen in vivo. They arrived at 64.09% and 34.02%, respectively. transplant) [4].
In vivo activity of Omtriptolide has been demonstrated in animal models of inflammation and autoimmune diseases. As a water-soluble prodrug of triptolide, it provides improved bioavailability and efficacy compared to the parent compound. Its in vivo activity is assessed by measuring reductions in inflammation, suppression of immune responses, and inhibition of tumor growth in relevant animal models. |
| Enzyme Assay |
The in vitro enzyme/receptor binding (cell-free) assay for Omtriptolide involves studying its interaction with molecular targets involved in its mechanism of action. As a prodrug of triptolide, its activity is mediated through the inhibition of NF-κB activation and other signaling pathways. Cell-free assays may measure the compound's effects on enzyme activities or protein-protein interactions involved in these pathways.
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| Cell Assay |
In vitro cellular assays for Omtriptolide are performed using various cell types, including immune cells and cancer cells. These assays measure the compound's ability to inhibit cell proliferation, suppress cytokine production, and induce apoptosis. The prodrug is converted to triptolide in cells, which exerts the pharmacological effects. These assays demonstrate the compound's anti-inflammatory, antiproliferative, and proapoptotic activities.
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| Animal Protocol |
In vivo animal studies for Omtriptolide are conducted in models of inflammation, autoimmune diseases, and cancer. These studies typically involve oral or parenteral administration of the compound, followed by assessment of disease severity, immune responses, and tumor growth. The prodrug formulation provides improved water solubility and bioavailability compared to triptolide, resulting in enhanced efficacy.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Omtriptolide are characterized by improved water solubility compared to triptolide, supporting systemic administration. As a prodrug, it is converted to the active compound triptolide in vivo, which exerts the pharmacological effects. The prodrug design improves the bioavailability and pharmacokinetic profile of triptolide, allowing for more predictable dosing and reduced toxicity.
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| Toxicity/Toxicokinetics |
Toxicology studies of Omtriptolide have been conducted to evaluate its safety profile. As a prodrug of triptolide, which has known toxicity concerns, the prodrug design aims to improve the therapeutic index by reducing systemic toxicity while maintaining efficacy. Preclinical toxicology studies include acute and repeat-dose toxicity assessments, as well as evaluations of organ-specific toxicity.
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| References |
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| Additional Infomation |
Omtriptolide (PG490-88) is a water-soluble derivative prodrug of triptolide, a diterpene triepoxide with immunosuppressive and anti-inflammatory activities. It has been investigated for the treatment of various inflammatory and autoimmune diseases, as well as cancer. The compound is also known as PG-490-88 and has been assigned the INN name Omtriptolide.
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| Molecular Formula |
C24H28O9
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|---|---|
| Molecular Weight |
460.479
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| Exact Mass |
460.173
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| CAS # |
195883-06-8
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| PubChem CID |
6918522
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| Appearance |
White to off-white solid powder
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| Density |
1.49
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| Melting Point |
109-111ºC
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| LogP |
1.518
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
33
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| Complexity |
1050
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| Defined Atom Stereocenter Count |
9
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| 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]2OC(=O)CCC(=O)O)O7)COC6=O)C
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| InChi Key |
HROMYAWHLUOUPY-AHCCQAQQSA-N
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| InChi Code |
InChI=1S/C24H28O9/c1-10(2)22-17(32-22)18-24(33-18)21(3)7-6-11-12(9-29-19(11)28)13(21)8-14-23(24,31-14)20(22)30-16(27)5-4-15(25)26/h10,13-14,17-18,20H,4-9H2,1-3H3,(H,25,26)/t13-,14-,17-,18-,20+,21-,22-,23+,24+/m0/s1
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| Chemical Name |
4-[[(1S,2S,4S,5S,7S,8R,9R,11S,13S)-1-methyl-17-oxo-7-propan-2-yl-3,6,10,16-tetraoxaheptacyclo[11.7.0.02,4.02,9.05,7.09,11.014,18]icos-14(18)-en-8-yl]oxy]-4-oxobutanoic acid
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| Synonyms |
PG-490-88; PG490-88
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| 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: 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)
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| Solubility (In Vitro) |
H2O : ~1.39 mg/mL (~3.02 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 3.33 mg/mL (7.23 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1716 mL | 10.8582 mL | 21.7165 mL | |
| 5 mM | 0.4343 mL | 2.1716 mL | 4.3433 mL | |
| 10 mM | 0.2172 mL | 1.0858 mL | 2.1716 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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