Seocalcitol
Based on 2 publication(s) in Google Scholar
Seocalcitol is a vitamin D analog, binds vitamin D receptor protein from human osteosarcoma MG-63 cells with Kd of 0.27 nM.
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- Reinheit: 99.33%
- CAS. Nr.: 134404-52-7
- Formel: C30H46O3
- Molecular Weight:454.68
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Speicherung:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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Biologische Aktivität
Kd: 0.27 nM (vitamin D receptor)[1]
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Cell Line
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Type | Value | Description | References |
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| U-937 | IC50 |
3.0 x 10-11M
Compound: EB 1089
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Compound was tested in vitro to inhibit proliferation of U 937 human histiolytic lymphoma cells
Compound was tested in vitro to inhibit proliferation of U 937 human histiolytic lymphoma cells
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10.1016/S0960-894X(00)80126-2 |
| Vero | CC50 |
11 μM
Compound: EB1089
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Cytotoxicity against African green monkey Vero cells infected with ZIKV HPF2013 pretreated with virus for 1 hr followed by infection of cells with compound treated-virus for 30 hrs by MTS assay
Cytotoxicity against African green monkey Vero cells infected with ZIKV HPF2013 pretreated with virus for 1 hr followed by infection of cells with compound treated-virus for 30 hrs by MTS assay
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[PMID: 36623328] |
| Vero | CC50 |
11 μM
Compound: EB1089
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Cytotoxicity against African green monkey Vero cells infected with ZIKV MR766 pretreated with virus for 1 hr followed by infection of cells with compound treated-virus for 30 hrs by MTS assay
Cytotoxicity against African green monkey Vero cells infected with ZIKV MR766 pretreated with virus for 1 hr followed by infection of cells with compound treated-virus for 30 hrs by MTS assay
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[PMID: 36623328] |
| Vero | CC50 |
11.9 μM
Compound: EB1089
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Cytotoxicity against African green monkey Vero cells infected with USUV 3345 isolate Arb276 pretreated with virus for 1 hr followed by infection of cells with compound treated-virus for 20 hrs by MTS assay
Cytotoxicity against African green monkey Vero cells infected with USUV 3345 isolate Arb276 pretreated with virus for 1 hr followed by infection of cells with compound treated-virus for 20 hrs by MTS assay
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[PMID: 36623328] |
Seocalcitol (EB 1089) is a stimulators of osteoclast recruitment in murine bone marrow cultures, with EC50 at 0.1 nM. Seocalcitol stimulates bone resorption with an estimated EC50 at 0.03 nM[1]. Seocalcitol (EB 1089) elicites a dose-dependent induction of 24-hydroxylase mRNA in the kidney (EC50=0.4±0.13). In the kidney, Kd values for Seocalcitol is 0.48±0.04 nM. However, in the intestine, the Kd for Seocalcitol is 1.43±0.19 nM)[2]. Seocalcitol (0.1-10 nM) induces cell differentiation in a dosedependent manner. A higher differentiating activity is observed for 1 nM Seocalcitol (EB 1089) than for 1 nM VD3.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 134404-52-7
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Appearance Solid
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Molecular Weight 454.68
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Formel C30H46O3
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Color White to off-white
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SMILES
O[C@H]1C[C@@H](C(/C(C1)=C\C=C2[C@@]3(CC[C@@H]([C@]3(CCC\2)C)[C@@H](/C=C/C=C/C(CC)(CC)O)C)[H])=C)O
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Synonyms
EB 1089
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Publications (2)
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Journal Impact Factor
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Most Recent
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Virol Sin
Antiviral activity of vitamin D derivatives against severe fever with thrombocytopenia syndrome virus in vitro and in vivo. [Abstract]2024 Oct;39(5):802-811. PMID: 39168248 -
Oncotarget
2016 Sep 20;7(38):62240-62254. PMID: 27557496
Seocalcitol purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Sep 20;7(38):62240-62254. [Abstract]
P-RPS levels in cells incubated with various prostate cancer cell inhibitors. A. PC3, B. C4-2B. DPT: deoxypodophyllotoxin; EB1089(EB; 1,25-vitamin D3 analog); T0901317, LXR agonist.
Lösungsmittel & Löslichkeit
DMSO : ≥ 50 mg/mL (109.97 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
Vitamin D receptor protein is prepared from cultures of human osteosarcoma cell line MG-63. Suspensions of 5×107 cells/mL are homogenized, sonicated, and centrifuged at 30,000g for 1 h at 4°C. The presence of the 1α,25(OH)2D3 receptor is verified by sucrose density gradient analysis. The supernatants are adjusted to 2 mg protein/mL and used for binding studies. Samples of 500 μL are incubated with 10,000 dpm [3H]1α,25(OH)2D3 (180 Ci/mmol) and increasing concentrations of 1α,25(OH)2D3 or vitamin D3 analogs are added. After incubation for 60 min at 22°C, bound and free [3H]1α,25(OH)2D3 are separated on dextran-coated charcoal. Each compound is tested in three separate experiments[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
This fluorescent dye allowed to determine ROS release in HL60 cells, untreated or treated VD3 or Seocalcitol. Briefly, after treatment, HL60 cells are washed and re-suspended at 106 cells/mL in RPMI-1640 without FCS and phenol red. Then, 10 μM H2-DCFDA probe is added to each plate at a final volume of 2 mL. Cells are incubated for 45 min at 37°C in the dark. A second wash is made before the fluorescence analysis using spectrometer at 488 nm intensity excitation λex and 516 nm emission λem. Results, in arbitrary fluorescence units (AFU), are expressed according to the ratio [(AFU-treated cells)/(AFU control cells)]×100[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[4]
Six- to eight-week-old male BALB/c NU/Nu mice are inoculated subcutaneously with 106 SKHEP-1 cells into the right flank. Twenty-four hours after inoculation, mice are randomly assigned to a control group (n=10) or the treatment groups (n=10), receiving 0.02, 0.1 or 0.5 μg/kg per day of Seocalcitol (intraperitoneal or oral on alternate days). Control animals receive propylene glycol alone. Tumor size is measured using vernier calipers every third day and the volumes are estimated using the formula 0.5×length×(width)2. Animals receive sterile food and water.
Rats[5]
Newborn Sprague-Dawley rat pups are randomly assigned to 1 of 6 treatment groups, consisting of daily intraperitoneal injections of the vitamin D analogue Seocalcitol (0.38 or 1.25 μg/kg body weight) alone, or in combination with all-trans retinoic acid (RA; 500 μg/kg body weight) and/or Dexamethasone (DEX; 0.25 μg/day) in a 3×2×2 factorial design. Seocalcitol and RA injections are conducted on P3 through P12, whereas Dexamethasone is administered on P4 through P12. Seocalcitol is prepared for injections in a quantity sufficient for all injections by dilution from a stock solution (4 mM in isopropanol) into the carrier Solutol HS 15 (BASF). Solutol-diluted Seocalcitol is stored as aliquots in sealed glass vials under nitrogen gas at 4°C, with daily injections conducted with freshly unsealed aliquots of Seocalcitol. Stock solutions of RA (50 mg/mL DMSO are stored under nitrogen at −80°C and prepared for injection by dilution of freshly thawed aliquots into cottonseed oil (2 μg/μL). A Dexamethasone stock solution (10 mg/mL ethanol) is stored under nitrogen at 4°C and prepared fresh for daily injections in 0.9% NaCl (0.25 μg/μL). All rats receive equivalent volumes of the 3 carrier solutions employed (solutol, cottonseed oil, 0.9% NaCl). Seocalcitol and RA are administered as a 2-phase solution via a 10 μL injection using a 20 μL glass-barreled syringe and a 28-gauge needle, whereas Dexamethasone is administered in a separate 10 μL injection.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (285 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Wiberg K, et al. Studies on two new vitamin D analogs, EB 1089 and KH 1060: effects on bone resorption and osteoclast recruitment in vitro. Bone. 1995 Oct;17(4):391-5. [Content Brief]
[2]. Roy S, et al. Comparative effects of 1,25-dihydroxyvitamin D3 and EB 1089 on mouse renal and intestinal 25-hydroxyvitamin D3-24-hydroxylase. J Bone Miner Res. 1995 Dec;10(12):1951-9 [Content Brief]
[3]. Bondza-Kibangou P, et al. Antioxidants and doxorubicin supplementation to modulate CD14 expression and oxidative stress induced by vitamin D3 and seocalcitol in HL60 cells. Oncol Rep. 2007 Dec;18(6):1513-9. [Content Brief]
[4]. Ghous Z, et al. Inhibition of hepatocellular cancer by EB1089: in vitro and in vivo study. Anticancer Res. 2008 Nov-Dec;28(6A):3757-61. [Content Brief]
[5]. Ormerod AK, et al. The calcitriol analogue EB1089 impairs alveolarization and induces localized regions of increased fibroblast density in neonatal rat lung. Exp Lung Res. 2008 May;34(4):155-82. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1993 mL | 10.9967 mL | 21.9935 mL | 54.9837 mL |
| 5 mM | 0.4399 mL | 2.1993 mL | 4.3987 mL | 10.9967 mL | |
| 10 mM | 0.2199 mL | 1.0997 mL | 2.1993 mL | 5.4984 mL | |
| 15 mM | 0.1466 mL | 0.7331 mL | 1.4662 mL | 3.6656 mL | |
| 20 mM | 0.1100 mL | 0.5498 mL | 1.0997 mL | 2.7492 mL | |
| 25 mM | 0.0880 mL | 0.4399 mL | 0.8797 mL | 2.1993 mL | |
| 30 mM | 0.0733 mL | 0.3666 mL | 0.7331 mL | 1.8328 mL | |
| 40 mM | 0.0550 mL | 0.2749 mL | 0.5498 mL | 1.3746 mL | |
| 50 mM | 0.0440 mL | 0.2199 mL | 0.4399 mL | 1.0997 mL | |
| 60 mM | 0.0367 mL | 0.1833 mL | 0.3666 mL | 0.9164 mL | |
| 80 mM | 0.0275 mL | 0.1375 mL | 0.2749 mL | 0.6873 mL | |
| 100 mM | 0.0220 mL | 0.1100 mL | 0.2199 mL | 0.5498 mL |
Seocalcitol Related Classifications
HY-32341 Related Classifications
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