| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
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| 500mg |
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| Other Sizes |
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| ln Vitro |
Half of the T98G cell replication is inhibited by dithranol (1.1 μM) [2]. In HaCaT cells, dithranol (0.1-0.5 μg/mL; 2-4 hours) stimulates the synthesis of interleukin-10 mRNA in a concentration-regulated manner [3].
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|---|---|
| Cell Assay |
RT-PCR[3]
Cell Types: HaCaT cells Tested Concentrations: 0.1 μg/mL, 0.25 μg/mL, 0.5 μg/mL Incubation Duration: 2 hrs (hours), 4 hrs (hours) Experimental Results: Increased mRNA production of IL-10 receptor in HaCaT cells. . |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Anthralin penetrates damaged skin and psoriatic lesions faster and to a greater extent than normal skin, likely due to increased vascularity of psoriatic lesions. Metabolism / Metabolites Anthralin is administered topically. Although the extent of systemic absorption after topical application has not been determined, no traces of anthraquinone metabolites were detected in the urine of treated subjects in a limited clinical study of anthralin cream,. Anthralin does not inhibit hepatic microsomal enzyme activity. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Topical anthralin has not been studied during breastfeeding. Anthralin has suspected mutagenic properties, so it should only be used if the potential benefit to the mother justifies potential risk to the infant. If anthralin is used, ensure that the infant's skin does not come into direct contact with the areas of maternal skin that have been treated and the infant does not ingest the product from the mother's skin. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
| References |
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| Additional Infomation |
Pharmacodynamics
Anthralin is a natural anthraquinone derivative, anti-psoriatic and anti-inflammatory agent. It controls skin growth by reducing the synthesis of DNA and the mitotic activity in the hyperplastic epidermis, normalizing the rate of cell proliferation and keratinization. |
| Molecular Formula |
C14H10O3
|
|---|---|
| Molecular Weight |
226.2274
|
| Exact Mass |
226.062
|
| CAS # |
1143-38-0
|
| PubChem CID |
2202
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| Appearance |
Yellow to orange solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
464.1±45.0 °C at 760 mmHg
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| Melting Point |
178-181 °C(lit.)
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| Flash Point |
248.6±25.2 °C
|
| Vapour Pressure |
0.0±1.2 mmHg at 25°C
|
| Index of Refraction |
1.710
|
| LogP |
4.16
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
0
|
| Heavy Atom Count |
17
|
| Complexity |
287
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
NUZWLKWWNNJHPT-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C14H10O3/c15-10-5-1-3-8-7-9-4-2-6-11(16)13(9)14(17)12(8)10/h1-6,15-16H,7H2
|
| Chemical Name |
1,8-dihydroxy-10H-anthracen-9-one
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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)
|
| Solubility (In Vitro) |
DMSO : ~12.5 mg/mL (~55.25 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 1 mg/mL (4.42 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 1 mg/mL (4.42 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1 mg/mL (4.42 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.4203 mL | 22.1014 mL | 44.2028 mL | |
| 5 mM | 0.8841 mL | 4.4203 mL | 8.8406 mL | |
| 10 mM | 0.4420 mL | 2.2101 mL | 4.4203 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 |
| NCT03348462 | Completed | Drug: ethosomal preparation of anthralin Drug: liposomal preparation of anthralin |
Psoriasis Vulgaris | Assiut University | 2017-11-30 | Phase 4 |
| NCT02752672 | Completed | Psoriasis | Medical University of Graz | 2016-03 | ||
| NCT01429870 | Withdrawn | Drug: Steroid active treatment | Psoriasis | University of Zurich | 2011-08 | Phase 4 |
| NCT04133506 | Active, not recruiting | Drug: Aspirin 300mg | Eczema | NHS Lothian | 2021-11-04 | |
| NCT01903317 | Withdrawn | Other: Topical Therapy Other: Phototherapy and Systemic Therapy Other: Biologic Therapy |
Psoriasis | University of California, Irvine | 2013-06 |
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