| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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Purity: ≥98%
Paricalcitol (trade name Zemplar) is a novel and potent vitamin D receptor (VDR) agonist created by Abbott Laboratories to prevent and treat secondary hyperparathyroidism, which is characterized by an excess of parathyroid hormone secreted and linked to chronic renal failure. An analog of vitamin D2's active form, 1,25-dihydroxyergocalciferol, is paricalcitol. Paricalcitol has been demonstrated to lower parathyroid hormone levels by binding to the vitamin D receptor. In leukemic cells, this agent also upregulates the expression of cyclin-dependent kinase inhibitors and the tumor-suppressor gene PTEN ('Phosphatase and Tensin homolog deleted on chromosome Ten').
| Targets |
vitamin D receptor
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|---|---|
| ln Vitro |
Comparing cells in HP medium with paricalcitol (3×10-8 M; HP + PC), a significant decrease in calcification was noted. Nuclear β-catenin is reduced by paricalcitol to levels comparable to those in control cells [1].
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| ln Vivo |
In TAC-pari mice, paricalcitol (300 ng/kg/day) significantly lowers the mRNA expression of ANP, fibronectin, and collagen III, and prevents LV dysfunction [2].
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| Animal Protocol |
Paricalcitol, a selective vitamin D receptor activator that activates the VDR, is administered to a subgroup of mice following TAC or sham surgery at a final dose of 300 ng/kg/day. A solution of 95% propylene glycol and 5% ethyl alcohol is used to dissolve paricalcitol. For five weeks in a row, mice receive three intraperitoneal injections of paricalcitol (or vehicle alone) on Mondays, Wednesdays, and Fridays. Included is a well-known anti-hypertrophic and anti-fibrotic medication called losartan, an angiotensin II receptor blocker (ARB). Losartan dissolved in drinking water at a concentration of 30 mg/kg/day has been demonstrated to be both feasible and effective in earlier experiments; mice are treated for five weeks in a row. Thus, eight groups in total are investigated. Ten individuals were involved in the study: Sham (n = 10), TAC (n = 10), Sham + losartan (Sham-los, n = 10), TAC + losartan (TAC-los, n = 10), Sham + paricalcitol (Sham-pari, n = 10), TAC + paricalcitol (TAC-pari, n = 10), Sham + paricalcitol + losartan (Sham-combi, n=10) and TAC + paricalcitol + losartan (TAC-combi, n = 10).
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| References |
[1]. Martinez-Moreno JM, et al. In vascular smooth muscle cells paricalcitol prevents phosphate-induced Wnt/beta-catenin activation. Am J Physiol Renal Physiol. 2012 Aug 8.
[2]. Meems LM, et al. The vitamin D receptor activator paricalcitol prevents fibrosis and diastolic dysfunction in a murine model of pressure overload. J Steroid Biochem Mol Biol. 2012 Jul 16;132(3-5):282-289 |
| Molecular Formula |
C27H44O3
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|---|---|
| Molecular Weight |
416.63646
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| Exact Mass |
416.33
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| Elemental Analysis |
C, 77.83; H, 10.64; O, 11.52
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| CAS # |
131918-61-1
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| Related CAS # |
131918-61-1
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| Appearance |
Solid powder
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| SMILES |
C[C@H](/C=C/[C@H](C)C(C)(C)O)[C@H]1CC[C@@H]\2[C@@]1(CCC/C2=C\C=C3C[C@H](C[C@@H](C3)O)O)C
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| InChi Key |
BPKAHTKRCLCHEA-UBFJEZKGSA-N
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| InChi Code |
InChI=1S/C27H44O3/c1-18(8-9-19(2)26(3,4)30)24-12-13-25-21(7-6-14-27(24,25)5)11-10-20-15-22(28)17-23(29)16-20/h8-11,18-19,22-25,28-30H,6-7,12-17H2,1-5H3/b9-8+,21-11+/t18-,19+,22-,23-,24-,25+,27-/m1/s1
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| Chemical Name |
(1R,3R)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(E,2R,5S)-6-hydroxy-5,6-dimethylhept-3-en-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]cyclohexane-1,3-diol
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| Synonyms |
paricalcitol-d6; Paricalcitol; Compound 49510; 19-Nor-1alpha,25-dihydroxyvitamin D2; Paracalcin; Abbott brand of paricalcitol; Zemplar
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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: 83~100 mg/mL (199.2~240.0 mM)
Ethanol: 12.5~13 mg/mL (30~31.2 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.00 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4002 mL | 12.0008 mL | 24.0015 mL | |
| 5 mM | 0.4800 mL | 2.4002 mL | 4.8003 mL | |
| 10 mM | 0.2400 mL | 1.2001 mL | 2.4002 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03415854 | Active Recruiting |
Drug: Paricalcitol (Zemplar) |
Pancreatic Cancer Adenocarcinoma |
HonorHealth Research Institute | January 31, 2018 | Phase 2 |
| NCT03520790 | Active Recruiting |
Drug: Paricalcitol Other: Placebo |
Pancreatic Cancer | Dana-Farber Cancer Institute | December 5, 2018 | Phase 1 Phase 2 |
| NCT02876211 | Recruiting | Drug: Paricalcitol Drug: Epoetin beta |
Anemia | Hospital Son Espases | December 2014 | Phase 4 |
| NCT04064827 | Recruiting | Drug: Paricalcitol | Chronic Kidney Disease (CKD) Secondary Hyperparathyroidism (SHPT) |
AbbVie | September 16, 2020 | Phase 3 |
| NCT05664880 | Recruiting | Drug: Paricalcitol Drug: Placebo |
Chronic Pancreatitis | Cedars-Sinai Medical Center | June 1, 2023 | Early Phase 1 |
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