Calcipotriol |
| Catalog No.GC17682 |
Calcipotriol is a synthetic vitamin D3 analog with high affinity for vitamin D receptors.
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.
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Calcipotriol is a synthetic vitamin D3 analog with high affinity for vitamin D receptors[1]. Calcipotriol is mainly used to treat psoriasis. It is also effective in certain keratotic diseases (ichthyosis) as well as localized scleroderma and vitiligo, and has important immunomodulatory functions [2].
In vitro, calcipotriol (10nM) treated HL-60 cells for 24h caused cell apoptosis, but caused cell differentiation at a higher dose (100nM)[3]. Calcipotriol (0.001-10μM) treated SCC13 cells for 4 days, dose-dependently inhibited cell proliferation and stimulated cell differentiation, but did not induce SCC13 cell apoptosis, and specifically inhibited the autocrine activation of the EGFR signaling pathway [4].
In vivo, calcipotriol combined with BDP ointment (40 mg, once daily, administered topically on the skin) treated rats with psoriasis-like dermatitis. Compared with the vaseline treatment group, it significantly inhibited ear skin thickening and Transepidermal water loss[5]. Calcipotriol (0.1mg/kg) can reduce knee joint swelling and relieve synovitis through a single intra-articular injection in ZIA rats [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.
| Cell experiment [1]: | |
|
Cell lines |
HL-60 cells |
|
Preparation Method |
HL-60 cells were pre-exposed to calcipotriol (0.1, 1, 10, 100 nM) for 24h, and then incubated with CIS for the next 48h. |
|
Reaction Conditions |
0.1, 1, 10, 100 nM; 24 h |
|
Applications |
Calcipotriol caused the apoptosis of HL-60 cells at the dose of 10nM, but in a higher dose (100nM) caused cell differentiation. |
| Animal experiment [2]: | |
|
Animal models |
Male Hairless HWY rats |
|
Preparation Method |
HWY rats received a daily topical dose of 10mg/ear or 25mg/back skin of 5% IMQ cream for 4 consecutive days in order to induce psoriasis-like skin dermatitis. Ears were treated with Vaseline, BDP, or Calcipotriol/BDP at doses of 10mg/ear and 40 mg/ear 1 hour after each application of IMQ. |
|
Dosage form |
10mg, 40 mg; apply topically to skin |
|
Applications |
Compared with the vaseline treatment group, 40 mg/ear calcipotriol/BDP ointment significantly inhibited ear thickening and transepidermal water loss. |
|
References: [1] 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. |
|
| 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 | 0.4847 mL | 2.4235 mL | 4.8471 mL |
| 10 mM | 0.2424 mL | 1.2118 mL | 2.4235 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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 ddH2O, 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
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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