| Identification | More | [Name]
PARICALCITOL (10 MG)F0E3030.997MG/MG(AI) | [CAS]
131918-61-1 | [Synonyms]
PARICALCITOL (10 MG)F0E3030.997MG/MG(AI)
PARICALCITOL
19-nor-1alpha,25-dihydroxyvitamin D2
(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
Zemplar | [EINECS(EC#)]
658-064-6 | [Molecular Formula]
C27H44O3 | [Molecular Weight]
416.64 | [MOL File]
131918-61-1.mol |
| Chemical Properties | Back Directory | [Boiling point ]
564.8±50.0 °C(Predicted) | [density ]
1.121±0.06 g/cm3(Predicted) | [Fp ]
14℃ | [storage temp. ]
Store at -20°C,unstable in solution, ready to use. | [solubility ]
DMSO : 100 mg/mL (240.02 mM; Need ultrasonic)Ethanol : 12.5 mg/mL (30.00 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble) | [form ]
neat | [pka]
14.34±0.40(Predicted) | [color ]
White to off-white | [InChIKey]
BPKAHTKRCLCHEA-UBFJEZKGSA-N | [SMILES]
C[C@]12CCC/C(=C\C=C3C[C@@H](O)C[C@H](O)C3)/[C@]1([H])CC[C@]2([H])[C@H](C)/C=C/[C@H](C)C(O)(C)C |&1:1,10,13,16,20,22,26,r| | [CAS DataBase Reference]
131918-61-1(CAS DataBase Reference) |
| Hazard Information | Back Directory | [Description]
Paricalcitol was launched as Zemplar in the US for the prevention and
treatment of secondary hyperthyroidism associated with chronic renal failure.
Paricalcitol is a synthetic vitamin D2, namely a novel 1-alpha-hydroxy-19-noranalogue
in which the ring A exocyclic methylene group, typical of all vitamin D
systems, has been replaced by two hydrogen atoms. Paricalcitol is the first
vitamin D analogue marketed for this indication. In patients with chronic renal
failure, Paricalcitol appreciably reduced levels of parathyroid hormone (PTH)
without a significant difference in the incidence rate for hypercalcemia or
hyperphosphatemia when compared with placebo. | [Chemical Properties]
White Solid | [Originator]
Abbott (US) | [Uses]
1,25-Dihydroxy vitamin D2 is a potent agonist of the vitamin D receptor. Paricalcitol is a synthetic 1,25-dihydroxy vitamin D2 analog. As vitamin D deficiency, associated with chronic kidney disease, leads to an increase in parathyroid hormone (secondary hyperparathyroidism), paricalcitol is used in renal patients to block parathyroid hormone overproduction. Vitamin D deficiency is also a risk factor in cancer, cardiovascular disease, hypertension, and diabetes, and paricalcitol may have applications in those contexts as well. | [Uses]
Antihyperparathyriod | [Uses]
Synthetic analog of vitamin D. Antihyperparathyroid. | [Definition]
ChEBI:Paricalcitol is a seco-cholestane and a hydroxy seco-steroid. It has a role as an antiparathyroid drug. It is functionally related to a vitamin D2. | [Brand name]
Zemplar (Abbott). | [Clinical Use]
Vitamin D analogue:
Treatment and prevention of secondary
hyperparathyroidism associated with chronic renal
failure | [Drug interactions]
Potentially hazardous interactions with other drugs
None known | [Metabolism]
Extensively metabolised via hepatic and non-hepatic
pathways to form two relatively inactive metabolites.
After oral administration of 3
H-paricalcitol, only about
2% of the dose was eliminated unchanged in the faeces,
and no parent drug found in the urine.
Approximately
70% of the radioactivity was eliminated in the faeces and
18% was recovered in the urine. Most of the systemic
exposure was from the parent drug. | [storage]
Store at -20°C,unstable in solution, ready to use. | [References]
[1] ALEX J BROWN. Calcemic activity of 19-Nor-1,25(OH)(2)D(2) decreases with duration of treatment.[J]. Journal of The American Society of Nephrology, 2000, 11 11: 2088-2094. DOI: 10.1681/asn.v11112088
[2] JAVIER DONATE-CORREA. Beneficial effects of selective vitamin D receptor activation by paricalcitol in chronic kidney disease.[J]. Current drug targets, 2014, 15 7: 703-709. DOI: 10.2174/1389450115666140417120902
[3] MYLES WOLF Ravi T. Vitamin D in patients with renal failure: A summary of observational mortality studies and steps moving forward[J]. Journal of Steroid Biochemistry and Molecular Biology, 2007, 103 3: Pages 487-490. DOI: 10.1016/j.jsbmb.2006.11.009
[4] DARKO DUPLANCIC. The influence of selective vitamin D receptor activator paricalcitol on cardiovascular system and cardiorenal protection.[J]. Clinical Interventions in Aging, 2013, 8: 149-156. DOI: 10.2147/cia.s38349 |
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