Size | Price | Stock | Qty |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
Trifarotene (CD5789; trade name Aklief) is a gamma retinoic acid receptor (RAR) agonist under approved in 2019 as a topical cream for the treatment of skin disorders, including acne vulgaris, cutaneous t-cell lymphoma and lamellar ichthyosis. It has Kdapp of 2, 15 and 500 nM for RARγ, RARβ and RARα, respectively. It has Kdapp of 2, 15 and 500 nM for RARγ, RARβ and RARα, respectively.
ln Vitro |
In remodeling human skin (RHE), trifarotene (CD5789) (3.3 μL 0.33 cm2; 24 hours) is involved in keratinization, desquamation, epidermalization, and cellular labeling. The average EC50 of all combined target genes for trifarotene is 0.0048% [2].
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ln Vivo |
It has been demonstrated that trifarotene (0.001%-0.01% in cream, 25 mg per mouse) is completely efficacious (98% decrease) when administered at 0.01% in comedogenic dosages [2].
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Animal Protocol |
Animal/Disease Models: Rhino mouse[2]
Doses: 0.001%, 0.0025%, 0.005% and 0.01% cream, the dose is 25 mg/mouse (5 cm2 surface of back skin, calculated as 5 mg/cm2) one time/day; 11 days Experimental Results: Epidermal thickness increased by 275% (66 μm) and transepidermal water loss (TEWL) increased by 285% (26 g/h/m2). |
References |
[1]. Etienne Thoreau, et al. Structure-based design of Trifarotene (CD5789), a potent and selective RARγ agonist for the treatment of acne. Bioorg Med Chem Lett. 2018 Jun 1;28(10):1736-1741.
[2]. J Aubert, et al. Nonclinical and human pharmacology of the potent and selective topical retinoic acid receptor-γ agonist trifarotene. Br J Dermatol. 2018 Aug;179(2):442-456. |
Molecular Formula |
C29H33NO4
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Molecular Weight |
459.586
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Exact Mass |
459.241
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CAS # |
895542-09-3
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Related CAS # |
895542-09-3;
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SMILES |
O=C(C1=CC=C(C2=CC=C(OCCO)C(C3=CC=C(N4CCCC4)C(C(C)(C)C)=C3)=C2)C=C1)O
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InChi Key |
MFBCDACCJCDGBA-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C29H33NO4/c1-29(2,3)25-19-23(10-12-26(25)30-14-4-5-15-30)24-18-22(11-13-27(24)34-17-16-31)20-6-8-21(9-7-20)28(32)33/h6-13,18-19,31H,4-5,14-17H2,1-3H3,(H,32,33)
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Chemical Name |
3''-(tert-butyl)-4'-(2-hydroxyethoxy)-4''-(pyrrolidin-1-yl)-[1,1'
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Synonyms |
CD5789 CD-5789 CD 5789
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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) |
DMSO : ~250 mg/mL (~543.97 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.53 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL 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: ≥ 2.08 mg/mL (4.53 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1759 mL | 10.8793 mL | 21.7585 mL | |
5 mM | 0.4352 mL | 2.1759 mL | 4.3517 mL | |
10 mM | 0.2176 mL | 1.0879 mL | 2.1759 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.