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| 10mg |
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| 25mg |
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| Targets |
Rhodojaponin III binds to NF-κB-inducing kinase (NIK) with a binding energy of -7.2 kcal/mol (determined by molecular docking) [1]
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|---|---|
| ln Vitro |
Rhodojaponin III inhibited LPS-induced nitric oxide (NO) production in RAW264.7 mouse macrophages with an IC₅₀ value of 7 μM (assessed by Griess assay) [1]
It dose-dependently reduced the production of pro-inflammatory cytokines (IL-6, IL-1β, TNF-α) in LPS-stimulated RAW264.7 cells [1] It suppressed LPS-induced COX-2 and iNOS protein expression in macrophage cells [1] The compound directly interacted with NIK, inhibiting the NIK/NF-κB pathway activation and preventing nuclear translocation of NF-κB, thereby reducing transcription of inflammatory genes [1] It also reduced phosphorylation of IKKα and NF-κB p65 in LPS-stimulated cells [1] |
| Cell Assay |
RAW264.7 cells were cultured in DMEM medium supplemented with 10% fetal bovine serum and 1% penicillin-streptomycin at 37°C in a 5% CO₂ incubator until 80-90% confluent [1]
Cells were seeded in 96-well plates at 1 × 10⁵ cells/well, allowed to attach overnight, pretreated with Rhodojaponin III (1, 5, 10, 20 μM) for 2 h, then stimulated with LPS (1 μg/mL) for 24 h; control groups included untreated cells and LPS-treated cells without the compound [1] For NO measurement: 100 μL of culture supernatant was mixed with 100 μL of Griess reagent, incubated at room temperature for 15 min, absorbance was measured at 540 nm, and NO concentration was calculated using a sodium nitrite standard curve [1] For cytokine assay: Culture supernatants were collected, and IL-6, IL-1β, TNF-α levels were measured by ELISA [1] For Western blot: Cells were lysed in RIPA buffer with protease and phosphatase inhibitors, protein concentration was determined by BCA assay, equal amounts of protein (30-50 μg) were separated by SDS-PAGE, transferred to PVDF membranes, blocked with 5% non-fat milk, incubated with primary antibodies (COX-2, iNOS, p-IKKα, IKKα, p-NF-κB p65, NF-κB p65, β-actin) overnight at 4°C, followed by HRP-conjugated secondary antibodies for 1 h at room temperature, and protein bands were visualized by ECL detection system [1] |
| Toxicity/Toxicokinetics |
Rhodioloside III exhibited high acute toxicity in mice, with an intraperitoneal LD₅₀ of 0.271 mg/kg [1]. Due to toxicity issues, its therapeutic window is limited [1].
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| References | |
| Additional Infomation |
Rhodojaponin III has been reported in Elliottia paniculata, Rhododendron japonoheptamerum, and other organisms with relevant data. Rhodojaponin III is a purine-type diterpenoid isolated from the leaves of Rhododendron molle [1]. Its anti-inflammatory activity is structure-dependent, with the purine skeleton being essential for its activity [1]. Despite its significant anti-inflammatory effects, its clinical development is limited due to its high toxicity [1]. Its interaction with NIK provides a novel mechanism for anti-inflammatory therapy [1].
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| Molecular Formula |
C20H32O6
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|---|---|
| Molecular Weight |
368.4645
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| Exact Mass |
368.219
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| CAS # |
26342-66-5
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| PubChem CID |
21151017
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
557.3±50.0 °C at 760 mmHg
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| Melting Point |
285-287 °C
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| Flash Point |
290.9±30.1 °C
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| Vapour Pressure |
0.0±3.4 mmHg at 25°C
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| Index of Refraction |
1.632
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| LogP |
1.09
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
26
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| Complexity |
667
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| Defined Atom Stereocenter Count |
11
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| SMILES |
C[C@]1(C[C@@]23C[C@H]([C@]4([C@@H]([C@H]5[C@@H](C4(C)C)O5)[C@]([C@@H]2CC[C@@H]1[C@H]3O)(C)O)O)O)O
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| InChi Key |
VUMZHZYKXUYIHM-GLHQSWFFSA-N
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| InChi Code |
InChI=1S/C20H32O6/c1-16(2)15-12(26-15)13-18(4,24)10-6-5-9-14(22)19(10,8-17(9,3)23)7-11(21)20(13,16)25/h9-15,21-25H,5-8H2,1-4H3/t9-,10+,11-,12+,13+,14-,15+,17-,18-,19+,20-/m1/s1
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| Chemical Name |
(1S,3R,4R,6R,8S,9S,10R,11R,14R,15R,17R)-5,5,10,15-tetramethyl-7-oxapentacyclo[12.2.1.01,11.04,9.06,8]heptadecane-3,4,10,15,17-pentol
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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: 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
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|---|---|
| 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 | 2.7140 mL | 13.5700 mL | 27.1400 mL | |
| 5 mM | 0.5428 mL | 2.7140 mL | 5.4280 mL | |
| 10 mM | 0.2714 mL | 1.3570 mL | 2.7140 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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