Cladophorol A
Cladophorol A is a cyclic GMP-AMP synthase (cGAS) inhibitor. Cladophorol A binds to the conserved adenosine nucleobase binding site within the cGAS active site to inhibit its catalytic activity. Cladophorol A effectively inhibits the overactivation of the cGAS-STING pathway with an IC50 of 370 nM. Cladophorol A inhibits asexual blood-stage Plasmodium falciparum with an EC50 of 0.7 μg/mL. Cladophorol A can be used for the researches of inflammatory disease and malaria.
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- CAS. Nr.: 146776-30-9
- Formel: C13H8O6
- Molecular Weight:260.20
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
In Vitro
Cladophorol A inhibits the cGAS-STING pathway in THP1-LuciaTM-ISG cells with an IRF-Luc IC50 of 370 nM, while exhibiting a cytotoxicity IC50 >30 μM[1].
Cladophorol-A (20 μM) enhances the stability of recombinant human cGAS protein[1].
Cladophorol-A (0.25-100 μM) directly inhibits the catalytic activity of recombinant human cGAS[1].
Cladophorol A (72 h) modestly inhibits asexual blood-stage Plasmodium falciparum (strain Dd2L) with an EC50 of 0.7 μg/mL[2].
Cladophorol A (18-22 h) does not inhibit the growth of methicillin-resistant Staphylococcus aureus, vancomycin-resistant Enterococcus faecium, Gram-negative pathogens, wild-type Candida albicans, or amphotericin B-resistant Candida albicans, with MIC values >50 μg/mL for all tested strains[2].
Cladophorol A exhibits weak cytotoxicity toward HEK293T cells with a CC50 of 9.4 μg/mL[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 146776-30-9
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Molecular Weight 260.20
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Formel C13H8O6
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SMILES
O=C1OC2=CC(O)=C(C=C2C3=C1C=C(O)C(O)=C3)O
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Structure Classification
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Initial Source
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (384.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (9.61 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
Verweise
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.8432 mL | 19.2160 mL | 38.4320 mL | 96.0799 mL |
| 5 mM | 0.7686 mL | 3.8432 mL | 7.6864 mL | 19.2160 mL | |
| 10 mM | 0.3843 mL | 1.9216 mL | 3.8432 mL | 9.6080 mL | |
| 15 mM | 0.2562 mL | 1.2811 mL | 2.5621 mL | 6.4053 mL | |
| 20 mM | 0.1922 mL | 0.9608 mL | 1.9216 mL | 4.8040 mL | |
| 25 mM | 0.1537 mL | 0.7686 mL | 1.5373 mL | 3.8432 mL | |
| 30 mM | 0.1281 mL | 0.6405 mL | 1.2811 mL | 3.2027 mL | |
| 40 mM | 0.0961 mL | 0.4804 mL | 0.9608 mL | 2.4020 mL | |
| 50 mM | 0.0769 mL | 0.3843 mL | 0.7686 mL | 1.9216 mL | |
| 60 mM | 0.0641 mL | 0.3203 mL | 0.6405 mL | 1.6013 mL | |
| 80 mM | 0.0480 mL | 0.2402 mL | 0.4804 mL | 1.2010 mL | |
| 100 mM | 0.0384 mL | 0.1922 mL | 0.3843 mL | 0.9608 mL |