| Size | Price | Stock | Qty |
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| 1mg |
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| 2mg |
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| 5mg |
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| 500mg | |||
| 1g | |||
| Other Sizes |
| Targets |
Tacalcitol targets the vitamin D receptor (VDR), a nuclear receptor that regulates gene expression. It acts as a VDR agonist, modulating cell differentiation and proliferation.
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|---|---|
| ln Vitro |
In vitro, tacalcitol modulates immunological and inflammatory processes and induces nerve growth factor production in epidermal keratinocytes. It promotes normal bone development by regulating calcium homeostasis.
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| ln Vivo |
In vivo, tacalcitol is used in the treatment of various skin disorders, including psoriasis and atopic dermatitis. It modulates immunological and inflammatory processes and induces nerve growth factor production.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for tacalcitol typically involve evaluating its binding affinity to the vitamin D receptor using radioligand binding assays. EC50 values for receptor activation are determined by measuring VDR-mediated gene expression or calcium mobilization.
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| Cell Assay |
For in vitro cell-based assays, tacalcitol is dissolved in DMSO and applied to cultured keratinocytes or osteoblasts at concentrations ranging from 1 nM to 10 µM. Effects on cell differentiation, proliferation, or gene expression are assessed after 24-72 hours of treatment.
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| Animal Protocol |
In vivo animal studies commonly use mouse models of psoriasis or bone disease. Tacalcitol is applied topically or administered orally at doses ranging from 0.1-10 µg/kg. Efficacy is evaluated by measuring skin lesion severity, bone density, or calcium levels.
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| ADME/Pharmacokinetics |
Tacalcitol has a molecular formula of C27H46O4 and a molecular weight of 434.65 g/mol. It is stored at 4°C, protected from light, under nitrogen.
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| Toxicity/Toxicokinetics |
In animal studies, tacalcitol has demonstrated a favorable safety profile with no significant toxicity at therapeutic doses. Hypercalcemia is a potential side effect at high doses.
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| References |
Int J Dermatol. 2017 Feb;56(2):232-238.
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| Additional Infomation |
Tacalcitol is used clinically for the treatment of psoriasis and other skin disorders. It is a potent modulator of cell differentiation and proliferation. It also promotes normal bone development by regulating calcium.
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| Molecular Formula |
C27H46O4
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|---|---|
| Molecular Weight |
434.661
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| Exact Mass |
434.339
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| CAS # |
93129-94-3
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| Related CAS # |
Tacalcitol;57333-96-7
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| PubChem CID |
9910819
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| Appearance |
White to off-white solid powder
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| LogP |
5.496
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
31
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| Complexity |
676
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| Defined Atom Stereocenter Count |
7
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| SMILES |
C[C@@]12[C@@H]([C@H](C)CC[C@@H](O)C(C)C)CC[C@H]1/C(/CCC2)=C/C=C1/C[C@@H](O)C[C@H](O)C/1=C.O
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| InChi Key |
UCLYOJXQGOXQKJ-XXBHHXRKSA-N
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| InChi Code |
InChI=1S/C27H44O3.H2O/c1-17(2)25(29)13-8-18(3)23-11-12-24-20(7-6-14-27(23,24)5)9-10-21-15-22(28)16-26(30)19(21)4/h9-10,17-18,22-26,28-30H,4,6-8,11-16H2,1-3,5H31H2/b20-9+,21-10-/t18-,22-,23-,24+,25-,26+,27-/m1./s1
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| Chemical Name |
(1R,3S,5Z)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(2R,5R)-5-hydroxy-6-methylheptan-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexane-1,3-diol;hydrate
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| Synonyms |
Bonalfa Curatoderm PRI 2191 PRI-2191 PRI2191 TV 02 TV-02 TV02
1,24(R)-Dihydroxyvitamin D3 monohydrate
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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)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3006 mL | 11.5032 mL | 23.0065 mL | |
| 5 mM | 0.4601 mL | 2.3006 mL | 4.6013 mL | |
| 10 mM | 0.2301 mL | 1.1503 mL | 2.3006 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.
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