Calcipotriol |
Catalog No.GC17682
One-Click Copy Product Info
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Calcipotriol es un análogo sintético de la vitamina D3 con alta afinidad por los receptores de vitamina D.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 112965-21-6
Sample solution is provided at 25 µL, 10mM.
Calcipotriol es un análogo sintético de la vitamina D3 con alta afinidad por los receptores de vitamina D [1]. Calcipotriol sse utiliza principalmente para tratar la psoriasis. También es eficaz en ciertas enfermedades queratóticas (ichthyosis) , así como en la esclerodermia localizada y el vitiligo, y tiene importantes funciones inmunomoduladoras [2].
In vitro, las células HL-60 tratadas con calcipotriol (10nM) durante 24h causaron apoptosis celular,pero causaron diferenciación celular a una dosis más alta (100nM)[3]. Calcipotriol (0.001-10μM) trató las células SCC13 durante 4 días, inhibió la proliferación celular dependiente de la dosis y estimuló la diferenciación celular, pero no indujo la apoptosis celular SCC13, e inhibió específicamente la activación autocrina de la vía de señalización EGFR [4].
In vivo, calcipotriol combinado con unguento BDP (40 mg, una vez al día, administrado tópicamente en la piel) trató a ratas con dermatitis similar a la psoriasis. En comparación con el grupo de tratamiento de vaselina, inhibió significativamente el engrosamiento de la piel del oído y la pérdida de agua transepidérmica[5]. Calcipotriol (0.1mg/kg) puede reducir la hinchazón de la articulación de la rodilla y aliviar la sinovitis a través de una sola inyección intraarticular en ratas ZIA [6].
References:
[1] Sakabe J, et al. Calcipotriol increases hCAP18 mRNA expression but inhibits extracellular LL37 peptide production in IL-17/IL-22-stimulated normal human epidermal keratinocytes[J].Acta Dermato-Venereologica, 2014, 94(5).
[2] Guilhou JJ. Le Calcipotriol [Calcipotriol]. Ann Dermatol Venereol. 2001 Mar;128(3 Pt 1):229-37. French. PMID: 11319386.
[3] Milczarek M, Chodyński M, Filip-Psurska B, et al. Synthesis and biological activity of diastereomeric and geometric analogs of calcipotriol, PRI-2202 and PRI-2205, against human HL-60 leukemia and MCF-7 breast cancer cells[J]. Cancers, 2013, 5(4): 1355-1378.
[4] Lee E A, Jeon S H, Yi J Y, et al. Calcipotriol inhibits autocrine phosphorylation of EGF receptor in a calcium-dependent manner, a possible mechanism for its inhibition of cell proliferation and stimulation of cell differentiation[J]. Biochemical and biophysical research communications, 2001, 284(2): 419-425.
[5] Satake K, Amano T, Okamoto T. Low systemic exposure and calcemic effect of calcipotriol/betamethasone ointment in rats with imiquimod-induced psoriasis-like dermatitis[J]. European Journal of Pharmacology, 2018, 826: 31-38.
[6] Huhtakangas J A, Huovinen J, Laaksonen S, et al. A single intra-articular dose of vitamin D analog calcipotriol alleviates synovitis without adverse effects in rats[J]. Plos one, 2021, 16(4): e0250352.
| Experimentos celulares [1]: | |
Líneas celulares | Células HL-60 |
Método de preparación | Las células HL-60 fieron preexpuestas al calcipotriol (0.1, 1, 10, 100 nM) durante 24h, y luego se incubaron con CIS durante las siguientes 48 horas. |
Condiciones de reacción | 0.1, 1, 10, 100 nM; 24 h |
Áreas de aplicación | Calcipotriol causó la apoptosis de las células HL-60 a una dosis de 10nM, pero en una dosis más alta (100nM) causó la diferenciación celular. |
| Experimentos con animales [2]: | |
Modelos animales | Ratas macho sin pelo HWY |
Método de preparación | Las ratas HWY recibieron una dosis tópica diaria de 10mg/oreja o 25mg/piel trasera de crema IMQ al 5% durante 4 días consecutivos para inducir dermatitis cutánea similar a la psoriasis. Los oídos fueron tratados con vaselina, BDP o Calcipotriol/BDP en dosis de 10mg/oreja y 40 mg/oreja 1 hora después de cada apñicación de IMQ. |
Forma de dosificación | 10mg, 40 mg; aplicar tópicamente sobre la piel |
Áreas de aplicación | En comparación con el grupo de tratamiento con vaselina, 40 mg/unguento de calcipotriol/BDP de oído inhibió significativamente el engrosamiento del oído y la pérdida de agua transepidérmica. |
References: | |
| Cas No. | 112965-21-6 | SDF | |
| Chemical Name | (1R,3S,5Z)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(E,2R,5S)-5-cyclopropyl-5-hydroxypent-3-en-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexane-1,3-diol | ||
| Canonical SMILES | CC(C=CC(C1CC1)O)C2CCC3C2(CCCC3=CC=C4CC(CC(C4=C)O)O)C | ||
| Formula | C27H40O3 | M.Wt | 412.62 |
| Solubility | ≥ 16.7 mg/mL in DMSO, ≥ 87.6 mg/mL in EtOH with gentle warming | Storage | -20°C, protect from light, stored under nitrogen,unstable in solution, ready to use. |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4235 mL | 12.1177 mL | 24.2354 mL |
| 5 mM | 484.7 μL | 2.4235 mL | 4.8471 mL |
| 10 mM | 242.4 μL | 1.2118 mL | 2.4235 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)