| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
The primary molecular target of lexacalcitol is the vitamin D receptor (VDR), a nuclear receptor that regulates gene expression. It acts as a potent agonist at the VDR, with higher affinity than calcitriol (1,25-dihydroxyvitamin D3). By binding to VDR, it modulates the expression of genes involved in cell proliferation, differentiation, and apoptosis. It inhibits angiogenesis by downregulating VEGF expression. It has minimal effects on calcium homeostasis compared to calcitriol, making it a non-calcemic analog.
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| ln Vitro |
In the human histiocytic lymphoma cell line U 937, lexacalcitol suppresses cell proliferation by 50% at a concentration of 10-12 M (14,00 times more active than la,25(OH)2D3) [1]. At 3×10-16 M, lexacalcitol reduces the proliferation of mouse thymocytes caused by IL-1 by 50%, and at 5×10-15 M, it prevents the allogeneic stimulation of mouse spleen lymphocytes [1].
In vitro, lexacalcitol inhibits cell proliferation and induces cell differentiation in various cancer cell lines, including breast, prostate, and colon cancer cells. It induces apoptosis and inhibits angiogenesis. Its in vitro activity is measured using cell proliferation assays, differentiation markers, and apoptosis assays. It binds to VDR with high affinity (Ki in the nanomolar range). It has minimal effects on calcium homeostasis. |
| ln Vivo |
In spontaneously diabetic NOD recipients, lexacalcidol (0.5 mg/kg/2 days; intraperitoneally) in conjunction with cyclosporine A (CyA) inhibits the autoimmune destruction of syngeneic islet grafts[2].
In vivo, lexacalcitol inhibits tumor growth and angiogenesis in animal models. It is effective in treating psoriasis in animal models. It has minimal effects on calcium homeostasis compared to calcitriol. Its in vivo efficacy is dose-dependent and correlates with VDR binding. It is well tolerated with no significant hypercalcemia at therapeutic doses. Its pharmacokinetic properties include good tissue distribution and a half-life suitable for daily dosing. |
| Enzyme Assay |
For vitamin D receptor binding assays, recombinant VDR protein or cell lysates expressing VDR are incubated with radiolabeled calcitriol ([3H]1,25(OH)2D3) and increasing concentrations of lexacalcitol. After incubation, bound and free ligand are separated by hydroxyapatite or dextran-coated charcoal, and radioactivity is quantified. Ki values are determined by Cheng-Prusoff equation.
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| Cell Assay |
For in vitro cell experiments, cancer cell lines (e.g., MCF-7, PC-3, or HT-29) are cultured and treated with lexacalcitol at concentrations ranging from 0.001-10 μM for 24-72 hours. Cell proliferation is assessed by MTT or BrdU incorporation assays. Differentiation markers are measured by qRT-PCR or Western blotting. Apoptosis is evaluated by Annexin V/PI staining or caspase-3/7 activity assays.
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| Animal Protocol |
Animal/Disease Models: Male and female spontaneously diabetic NOD mice [2]
Doses: 0.5 mg/kg/2 days Route of Administration: intraperitoneal (ip) injection Experimental Results: Treatment with KH1060 or CyA alone did not produce a statistically significant effect on early graft failure inhibitory effect, whereas combined treatment with KH1060 and CyA prevented early graft failure and delayed xenograft islet graft rejection in spontaneously diabetic NOD mice. For in vivo animal experiments, mice or rats are used. Lexacalcitol is administered by oral gavage or intraperitoneal injection at doses ranging from 0.01-10 μg/kg/day for 2-4 weeks. For tumor studies, mice bearing xenograft tumors are treated, and tumor volume is measured regularly. For psoriasis studies, topical application or systemic administration is used, and skin lesions are assessed. Serum calcium levels are monitored to assess calcemic activity. Pharmacokinetic parameters are determined by LC-MS/MS. |
| References |
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| Additional Infomation |
Lexacalcitol is a solid. This compound belongs to the class of vitamin D and its derivatives. These compounds contain an open-ring steroid skeleton, typically an open-ring ergosterane or an open-ring cholesterane. It is known to target the vitamin D3 receptor.
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| Molecular Formula |
C29H48O4
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|---|---|
| Molecular Weight |
460.7
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| Exact Mass |
460.355
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| CAS # |
131875-08-6
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| PubChem CID |
5288670
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
600.3±55.0 °C at 760 mmHg
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| Flash Point |
316.8±31.5 °C
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| Vapour Pressure |
0.0±3.9 mmHg at 25°C
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| Index of Refraction |
1.542
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| LogP |
5.62
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
33
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| Complexity |
734
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| Defined Atom Stereocenter Count |
6
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| SMILES |
C[C@]1(CCC/2)[C@](CC[C@@H]1[C@@H](C)OCCCC(CC)(CC)O)([H])C2=C\C=C(C[C@@H](O)C[C@@H]3O)/C3=C
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| Synonyms |
KH-1060; KH1060; Lexacalcitol
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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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. (3). This product is not stable in solution, please use freshly prepared working solution for optimal results. |
| 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 : ~100 mg/mL (~217.07 mM)
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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 | 2.1706 mL | 10.8530 mL | 21.7061 mL | |
| 5 mM | 0.4341 mL | 2.1706 mL | 4.3412 mL | |
| 10 mM | 0.2171 mL | 1.0853 mL | 2.1706 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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