| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Other Sizes |
| Targets |
Erinacine A targets multiple signaling pathways and molecular targets. It induces apoptosis by activating both extrinsic and intrinsic apoptotic pathways in cancer cells. Its targets include the Bcl-2 family, NF-κB, Akt, Caspase, Histone Acetyltransferase, NO Synthase, JNK, p38 MAPK, and PI3K. In neuronal cells, it inhibits iNOS expression and nitrotyrosine production to exert neuroprotective effects. The compound also reduces proliferation, invasiveness, and oxidative stress production while inducing cell cycle arrest.
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|---|---|
| ln Vitro |
In vitro, Erinacine A (30 μM; 3-24 hours) activates exogenous and endogenous apoptosis pathways in DLD-1 colorectal cancer cells while down-regulating anti-apoptotic proteins. It induces cancer cell death by activating extrinsic and intrinsic apoptosis pathways. The compound inhibits the expression of NO synthase (iNOS) and the production of nitrotyrosine, exerting anti-inflammatory and neuroprotective effects. These in vitro activities support its potential for cancer and neurodegenerative disease research.
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| ln Vivo |
In vivo, Erinacine A demonstrates significant neuroprotective and anticancer effects. In a senescence-accelerated mouse (SAM) model of transient stroke, single-dose intraperitoneal injections (1, 5, and 10 mg/kg) reduced neuronal cell death and inhibited the expression of inflammatory cytokines in brain tissue. In a DLD-1 xenograft mouse model, Erinacine A (1, 2, and 5 mg/kg, intraperitoneal injection once daily for 5 days) significantly inhibited tumor growth, resulting in a significant reduction in tumor size. It also reduces ischemic brain damage.
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| Enzyme Assay |
Typical in vitro enzyme/receptor binding assays for Erinacine A are not extensively documented. For studying its mechanism of action, assays measuring apoptosis pathway activation are employed. These include caspase activity assays, assessment of Bcl-2 family protein expression by Western blot, and evaluation of NF-κB and Akt signaling pathways. iNOS activity and nitrotyrosine production can be measured to assess anti-inflammatory and neuroprotective effects. These cell-free systems allow for characterization of the compound's molecular targets.
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| Cell Assay |
Cellular assays for Erinacine A typically involve treating cancer cell lines such as DLD-1 colorectal cancer cells with the compound at concentrations up to 30 μM for 3-24 hours. Apoptosis is evaluated by assessing activation of extrinsic and intrinsic pathways, and expression of anti-apoptotic proteins is measured by Western blot. For neuroprotection studies, neuronal cells are treated with the compound, and iNOS expression and nitrotyrosine production are measured. Cell viability is assessed by MTT or similar assays.
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| Animal Protocol |
In vivo animal experiments for Erinacine A typically involve rodent models. For neuroprotection, a senescence-accelerated mouse model of transient stroke is used, with single-dose intraperitoneal injections at 1, 5, and 10 mg/kg. Neuronal cell death and inflammatory cytokine expression in brain tissue are assessed. For anticancer activity, a DLD-1 xenograft mouse model is used, with intraperitoneal injections at 1, 2, and 5 mg/kg once daily for 5 days. Tumor growth inhibition and tumor size reduction are measured.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Erinacine A are limited. As a diterpenoid with a molecular weight of 432.55 g/mol, it would be expected to have moderate lipophilicity and potential for oral bioavailability. The compound is soluble in ethanol at 8 mg/mL (18.49 mM). However, detailed ADME parameters including Cmax, Tmax, half-life, and bioavailability are not available in the consulted sources. The compound is intended for research use only.
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| Toxicity/Toxicokinetics |
Toxicological data for Erinacine A are limited. In animal studies, the compound was well-tolerated at doses up to 10 mg/kg in the stroke model and up to 5 mg/kg in the xenograft model. As a natural compound from Hericium erinaceus, it is generally considered to have low toxicity. However, comprehensive toxicological studies have not been reported. Standard laboratory safety precautions should be followed when handling the compound.
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| References |
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| Additional Infomation |
See also: Erinacine A (note moved to).
Erinacine A is a cyathane diterpenoid from Hericium erinaceus with neuroprotective, anticancer, anti-inflammatory, and antioxidant activities. Its most distinguished feature is the ability to stimulate nerve growth factor (NGF) synthesis. It has been studied for potential treatments for neurodegenerative diseases such as Alzheimer's and Parkinson's. The compound is extensively used in dietary supplement and functional food formulations targeting cognitive enhancement and neuroprotection. It is a research compound and is not approved for any clinical indication. |
| Molecular Formula |
C25H36O6
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|---|---|
| Molecular Weight |
432.549748420715
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| Exact Mass |
432.251
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| CAS # |
156101-08-5
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| PubChem CID |
9867477
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| Appearance |
Light yellow to yellow solid
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| Melting Point |
74 - 76 °C
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| LogP |
2
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
31
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| Complexity |
826
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
LPPCHLAEVDUIIW-NLLUTMDRSA-N
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| InChi Code |
InChI=1S/C25H36O6/c1-14(2)16-7-8-24(3)9-10-25(4)17(20(16)24)6-5-15(12-26)11-19(25)31-23-22(29)21(28)18(27)13-30-23/h5-6,12,14,18-19,21-23,27-29H,7-11,13H2,1-4H3/t18-,19+,21+,22-,23+,24-,25-/m1/s1
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| Chemical Name |
(3aR,5aR,6S)-3a,5a-dimethyl-1-propan-2-yl-6-[(2S,3R,4S,5R)-3,4,5-trihydroxyoxan-2-yl]oxy-2,3,4,5,6,7-hexahydrocyclohepta[e]indene-8-carbaldehyde
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| Synonyms |
Erinacine A
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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 | 2.3119 mL | 11.5594 mL | 23.1187 mL | |
| 5 mM | 0.4624 mL | 2.3119 mL | 4.6237 mL | |
| 10 mM | 0.2312 mL | 1.1559 mL | 2.3119 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04065061 | Completed | Dietary Supplement: Placebo Dietary Supplement: Erinacine A -enriched Hericium Erinaceus Mycelia |
fMRI Vision Supplement |
Chung Shan Medical University | May 22, 2015 | Not Applicable |
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