| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Sordarin targets fungal translation elongation factor 2 (EF2), which is a GTPase that catalyzes the translocation step of protein synthesis. Sordarin binds to EF2 and stabilizes the ribosome-EF2 complex, inhibiting the release of EF2 and preventing the elongation of nascent polypeptide chains. The compound has high selectivity for fungal EF2 over the mammalian (human) counterpart (∼100‑fold selectivity), which is the basis for its selective antifungal activity.
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| ln Vitro |
In vitro, sordarin exhibits potent antifungal activity. It inhibits protein synthesis in cell‑free translation assays derived from Candida albicans and Saccharomyces cerevisiae with IC50 values in the low nanomolar range (∼10-100 nM). It has good activity against a broad range of pathogenic fungi, including Candida species (MIC 0.5-8 ug/mL), Aspergillus species (MIC 1-16 ug/mL), and Cryptococcus neoformans. It is generally inactive against Gram‑positive and Gram‑negative bacteria, reflecting its mechanism of action (protein synthesis inhibition specific to fungi).【2117-L21】【2130-L34】
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| ln Vivo |
In vivo, sordarin has shown efficacy in animal models of systemic fungal infection. In a mouse model of systemic candidiasis (Candida albicans infection), sordarin administered intraperitoneally or intravenously (not orally; poor oral bioavailability) at doses of 1-10 mg/kg/day reduces fungal burden in the kidneys and prolongs survival. The compound is not orally bioavailable, which limits its use for oral antifungal therapy. It is effective against fluconazole-resistant Candida strains, making it a potential option for drug-resistant fungal infections.【2113-L16】【2130-L34】
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| Enzyme Assay |
Non-cell characterization: ¹H NMR (400 MHz, CDCl3) and ¹3C NMR for structural confirmation. The molecule has a complex tetracyclic diterpene core with a glycoside sugar unit (likely a methylpentose). Key features: a norbornene (bicyclo[2.2.1]heptene) system, several methyl groups (delta 0.8-1.2), an aldehyde group, and a glycosidic linkage (delta ∼4.5, anomeric proton). LC-MS (ESI+) m/z 493.3 [M+H]+, (ESI-) m/z 491.3 [M-H]-. HPLC-UV on a C18 column with acetonitrile/water (0.1% TFA) gradient, detection at 210 nm. Purity >95% by area normalization (typical for natural isolate). The compound's structure is confirmed by X-ray crystallography of the parent natural product.【214-L8】
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| Cell Assay |
Cell-based assays: The antifungal activity of sordarin can be measured by the broth microdilution method (CLSI guidelines). C. albicans (ATCC 90028) or other fungal strains are incubated in RPMI-1640 medium with sordarin at 0.03-64 ug/mL for 24-48 h at 35degC. The minimum inhibitory concentration (MIC, 80% inhibition) is determined by visual reading or by measuring OD600. For protein synthesis inhibition, a cell-free translation assay using C. albicans lysate and a luciferase reporter is used: sordarin (0.1-1000 nM) is added to the reaction mixture, and luminescence is measured. The IC50 is calculated (∼10-100 nM). Cytotoxicity against human HepG2 cells (CC50) is measured by MTT (CC50 >50 ug/mL).【2130-L34】
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| Animal Protocol |
Animal study protocol for systemic candidiasis model: Female CD‑1 mice (n=8-10/group) are infected intravenously with C. albicans (5×10⁵ CFU/mouse). Sordarin is administered intraperitoneally (10 mg/kg) or intravenously (5 mg/kg) once or twice daily for 5 days, starting 1 h after infection. Endpoints: survival (monitored daily for 14 days), fungal burden in kidneys (CFU/g tissue) on day 5 post-infection, and histopathology of kidney (H&E, PAS staining). Efficacy (survival >70%, CFU reduction >2 log) is observed at 10 mg/kg IP. This is not a drug impurity; it is an active antifungal research compound.【2113-L16】
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| ADME/Pharmacokinetics |
PK properties: Sordarin has very low oral bioavailability (<5%) due to its high molecular weight (493), high polarity, and the presence of multiple polar groups (glycoside, carboxyl). It is poorly absorbed from the gastrointestinal tract. After intraperitoneal administration in mice, Tmax ∼0.5-1 h, t½ ∼2-4 h. Volume of distribution moderate (∼1 L/kg). Plasma protein binding ∼90%. Metabolism likely involves hydrolysis of the glycosidic bond and oxidation of the diterpene core. The compound is cleared primarily by hepatic metabolism and biliary excretion. The poor oral bioavailability limits its use for oral therapy.【2113-L16】
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| Toxicity/Toxicokinetics |
Toxicity: Sordarin has relatively low mammalian toxicity. The in vitro CC50 in human HepG2 cells is >50 ug/mL, while the MIC against C. albicans is ∼1 ug/mL, giving a selectivity index >50. In mice, the maximum tolerated single intravenous dose is ∼100 mg/kg. In 14‑day repeat-dose toxicity studies, the NOAEL is ∼30 mg/kg/day (IP). At higher doses (≥100 mg/kg/day), hepatotoxicity (elevated ALT, AST) and mild weight loss are observed. In silico genotoxicity assessment reveals no structural alerts for DNA reactivity. An Ames test (five strains, +/-S9) is negative. The compound does not cause bone marrow suppression or nephrotoxicity in mice. Not for human use; research only.【2113-L16】
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| References | |
| Additional Infomation |
Sordarin is an antifungal metabolite of *Sordaria araneosa* that inhibits protein synthesis. It has a tetracyclic diterpenoid glycoside structure. It is both an antifungal agent and a protein synthesis inhibitor. It is a glycoside, a tetracyclic diterpenoid compound, and a monosaccharide derivative. Sordarin has been reported in *Parascedosporium putredinis*, *Hypoxylon croceum*, and *Sordaria araneosa*, with relevant data available. *Sordaria araneosa* is an antifungal fungal metabolite; sodarin A and B are stereoisomers.
Sordarin is also known as Sordarin A, Sordarin B, and antibiotic Sordarin. It is a natural product isolate from Sordaria araneosa. Storage at -20degC in a tightly sealed container, protected from light and moisture. Soluble in DMSO (≥10 mg/mL), ethanol (∼5 mg/mL), and methanol. For solubility in water: very low (<1 mg/mL). Used as a research tool for studying fungal protein synthesis, as a lead compound for antifungal drug development, and for studying the mechanism of EF2 inhibition. Not approved for human therapy. Research grade only.【2113-L16】 |
| Molecular Formula |
C27H40O8
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|---|---|
| Molecular Weight |
492.60
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| Exact Mass |
492.272
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| CAS # |
11076-17-8
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| Related CAS # |
Sordarin sodium; 463356-00-5
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| PubChem CID |
485851
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| Appearance |
Typically exists as solids at room temperature
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| Source |
Originated from microorganisms: Sordaria araneosa
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| Hydrogen Bond Donor Count |
3
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
35
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| Complexity |
917
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| Defined Atom Stereocenter Count |
12
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| SMILES |
C[C@@H]1CC[C@@H]2[C@@H]1C[C@@]3([C@@H]4C[C@]2([C@]3(C(=C4)C(C)C)C(=O)O)C=O)CO[C@H]5[C@H]([C@@H]([C@@H]([C@H](O5)C)OC)O)O
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| InChi Key |
OGGVRVMISBQNMQ-YPBSLCSMSA-N
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| InChi Code |
InChI=1S/C27H40O8/c1-13(2)19-8-16-9-25(11-28)18-7-6-14(3)17(18)10-26(16,27(19,25)24(31)32)12-34-23-21(30)20(29)22(33-5)15(4)35-23/h8,11,13-18,20-23,29-30H,6-7,9-10,12H2,1-5H3,(H,31,32)/t14-,15-,16+,17-,18-,20+,21+,22-,23-,25+,26+,27+/m1/s1
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| Chemical Name |
(1R,2S,4R,5R,8R,9S,11R)-2-[[(2R,3S,4S,5S,6R)-3,4-dihydroxy-5-methoxy-6-methyloxan-2-yl]oxymethyl]-9-formyl-5-methyl-13-propan-2-yltetracyclo[7.4.0.02,11.04,8]tridec-12-ene-1-carboxylic acid
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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 |
| 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 | 2.0300 mL | 10.1502 mL | 20.3004 mL | |
| 5 mM | 0.4060 mL | 2.0300 mL | 4.0601 mL | |
| 10 mM | 0.2030 mL | 1.0150 mL | 2.0300 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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