| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250g |
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| Other Sizes |
| Targets |
Nardosinone does not directly target a specific protein with a defined IC50, Ki, EC50, or DC50 in this study. It enhances neurite outgrowth by amplifying both mitogen-activated protein (MAP) kinase-dependent and -independent signaling pathways downstream of dbcAMP and staurosporine. The compound itself does not affect MAP kinase phosphorylation. [1]
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| ln Vitro |
In PC12D cells, naredosinone (0.1–100 microM) concentration-dependently promotes neurite outgrowth triggered by staurosporine (10 nM) and dibutyryl cyclic AMP (dbcAMP, 0.3 mM). In the MAP kinase-dependent signaling pathway, nandosinone amplifies the downstream actions of MAP kinase [1].
Nardosinone alone (up to 100 μM) did not induce neurite outgrowth in PC12D cells. However, it enhanced dbcAMP (0.3 mM)-induced neurite outgrowth in a concentration-dependent manner (0.1–100 μM), shifting the dbcAMP concentration-response curve leftward and increasing the maximum response. [1] Nardosinone (0.1–100 μM) also potentiated staurosporine (10 nM)-induced neurite outgrowth concentration-dependently, shifting the staurosporine concentration-response curve leftward and increasing the maximum response. [1] The MAP kinase kinase inhibitor PD98059 (20 μM) partially blocked nardosinone-induced enhancement of dbcAMP (0.3 mM)- or staurosporine (10 nM)-mediated neurite outgrowth. PD98059 alone did not affect dbcAMP or staurosporine-induced neurite outgrowth. [1] Western blot analysis showed that nardosinone alone did not increase dual phosphorylation of MAP kinase 1/2. dbcAMP markedly increased MAP kinase 1/2 phosphorylation, which was not affected by co-treatment with nardosinone (100 μM). Staurosporine (10 nM or 30 nM) had little effect on MAP kinase phosphorylation, and nardosinone did not alter the phosphorylation levels in the presence of staurosporine. [1] |
| Cell Assay |
PC12D cells were maintained in DMEM supplemented with 5% fetal calf serum, 10% horse serum, and 2 mM glutamine at 37°C in a humidified 5% CO2 atmosphere. For neurite outgrowth assays, cells were dissociated by incubation with 1 mM EGTA in phosphate-buffered saline (PBS) for 1 h, then seeded at 2×10^4 cells/well in 24-well plates coated with poly-L-lysine. After 24 h, the medium was replaced with test medium containing 1% fetal calf serum, 2% horse serum, and various concentrations of nardosinone, dbcAMP, or staurosporine. After 48 h, cultures were fixed with 2% glutaraldehyde in PBS. Neurite outgrowth was observed under a phase-contrast microscope. Processes with lengths equivalent to at least one cell body diameter were scored as neurites. The proportion of neurite-bearing cells to total cells (≥100 cells) in randomly selected areas was calculated. The effects were compared with positive controls (50 nM staurosporine or 1 mM dbcAMP). [1]
For Western blot analysis, PC12D cells were treated with or without nardosinone (100 μM) in the presence or absence of staurosporine or dbcAMP. Cells were lysed with SDS-containing lysis buffer, boiled, sonicated, and proteins separated by SDS-PAGE. After transfer to polyvinylidene difluoride membrane, blots were blocked and incubated with anti-active MAP kinase 1/2 antibody, followed by HRP-conjugated secondary antibody. Signals were visualized with chemiluminescent substrate. Blots were then stripped and reprobed with anti-total MAP kinase 1/2 antibody. Protein content was determined using a BCA assay. [1] |
| References | |
| Additional Infomation |
Reports have indicated that spikenard contains spikenard ketone, and relevant data is available for reference.
Nardosinone is the first reported enhancer of neurite outgrowth-promoting activity of dbcAMP and staurosporine. It enhances both MAP kinase-dependent and -independent signaling pathways, likely by amplifying a downstream step of MAP kinase in the MAP kinase-dependent pathway. The compound may become a useful pharmacological tool for studying the mechanism of action of various neuritogenic substances, including NGF, dbcAMP, and staurosporine. It has potential implications for understanding signal transduction controlling neurite outgrowth and for therapeutic strategies in neurodegenerative diseases such as Alzheimer's disease and dementia. [1] |
| Molecular Formula |
C15H22O3
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|---|---|
| Molecular Weight |
250.3334
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| Exact Mass |
250.156
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| Elemental Analysis |
C, 71.97; H, 8.86; O, 19.17
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| CAS # |
23720-80-1
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| PubChem CID |
168136
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
330.2±32.0 °C at 760 mmHg
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| Melting Point |
108-110℃
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| Flash Point |
142.0±25.2 °C
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| Vapour Pressure |
0.0±0.7 mmHg at 25°C
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| Index of Refraction |
1.522
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| LogP |
3.04
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
18
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| Complexity |
424
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| Defined Atom Stereocenter Count |
4
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| SMILES |
O1[C@]2([H])C([H])([H])C(C3=C([H])C([H])([H])C([H])([H])[C@@]([H])(C([H])([H])[H])[C@]3(C([H])([H])[H])[C@]2([H])C(C([H])([H])[H])(C([H])([H])[H])O1)=O
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| InChi Key |
KXGHHSIMRWPVQM-JWFUOXDNSA-N
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| InChi Code |
InChI=1S/C15H22O3/c1-9-6-5-7-10-11(16)8-12-13(15(9,10)4)14(2,3)18-17-12/h7,9,12-13H,5-6,8H2,1-4H3/t9-,12-,13+,15+/m1/s1
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| Chemical Name |
(3aR,9R,9aR,9bS)-1,1,9,9a-tetramethyl-3a,4,7,8,9,9b-hexahydronaphtho[2,1-c]dioxol-5-one
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| Synonyms |
Nardosinone
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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) |
DMSO : ~250 mg/mL (~998.68 mM)
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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 | 3.9947 mL | 19.9736 mL | 39.9473 mL | |
| 5 mM | 0.7989 mL | 3.9947 mL | 7.9895 mL | |
| 10 mM | 0.3995 mL | 1.9974 mL | 3.9947 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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