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Falecalcitriol

Calcitriol analog CAS# 83805-11-2

Falecalcitriol

Catalog No. BCC1570----Order now to get a substantial discount!

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Quality Control of Falecalcitriol

Number of papers citing our products

Chemical structure

Falecalcitriol

3D structure

Chemical Properties of Falecalcitriol

Cas No. 83805-11-2 SDF Download SDF
PubChem ID 5282190 Appearance Powder
Formula C27H38F6O3 M.Wt 524.58
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble in DMSO
Chemical Name (1R,3S,5Z)-5-[(2E)-2-[(1R,3aS,7aR)-7a-methyl-1-[(2R)-7,7,7-trifluoro-6-hydroxy-6-(trifluoromethyl)heptan-2-yl]-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexane-1,3-diol
SMILES CC(CCCC(C(F)(F)F)(C(F)(F)F)O)C1CCC2C1(CCCC2=CC=C3CC(CC(C3=C)O)O)C
Standard InChIKey XPYGGHVSFMUHLH-UUSULHAXSA-N
Standard InChI InChI=1S/C27H38F6O3/c1-16(6-4-13-25(36,26(28,29)30)27(31,32)33)21-10-11-22-18(7-5-12-24(21,22)3)8-9-19-14-20(34)15-23(35)17(19)2/h8-9,16,20-23,34-36H,2,4-7,10-15H2,1,3H3/b18-8+,19-9-/t16-,20-,21-,22+,23+,24-/m1/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Falecalcitriol

DescriptionFalecalcitriol(Fulstan; Hornel) is an analog of calcitriol; has a higher potency both in vivo and in vitro systems, and longer duration of action in vivo.

References:
[1]. Ito H, Ogata H, Yamamoto M, Takahashi K, Shishido K, Takahashi J, Taguchi S, Kinugasa E. Comparison of oral falecalcitriol and intravenous calcitriol in hemodialysis patients with secondary hyperparathyroidism: a randomized, crossover trial. Clin Nephro [2]. Tokunaga M, Tamura M, Kabashima N, Serino R, Shibata T, Matsumoto M, Miyamoto T, Miyazaki M, Furuno Y, Takeuchi M, Abe H, Okazaki M, Otsuji Y. Falecalcitriol for conventional vitamin D therapy-resistant secondary hyperparathyroidism in a continuous ambul [3]. Iwao Y, Yamaguchi Y, Fujii K, Toba Y, Asada M, Nagano N, Yamamoto H, Hyoma K, Yamada S, Hirano H, Tone Y, Ohtani H, Saika Y, Fujii R. Long-term suppressive effect of falecalcitriol on parathyroid hormone secretion in secondary hyperparathyroidism in hemo [4]. Morii H. Falecalcitriol as a new therapeutic agent for secondary hyperparathyroidismClin Calcium. 2005 Jan;15(1):29-33. [5]. Ohtsuka N, Urayama K. Pharmacological action and clinical effects of falecalcitriol, a highly potent derivative of active vitamin D3.Nihon Yakurigaku Zasshi. 2002 Dec;120(6):427-36. [6]. Jean-Pierre Bégué, Danièle Bonnet-Delpon.Recent advances (1995-2005) in fluorinated pharmaceuticals based on natural products. Journal of Fluorine Chemistry.Volume 127, Issue 8, August 2006, Pages 992-1012

Falecalcitriol Dilution Calculator

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Falecalcitriol Molarity Calculator

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Preparing Stock Solutions of Falecalcitriol

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.9063 mL 9.5314 mL 19.0629 mL 38.1257 mL 47.6572 mL
5 mM 0.3813 mL 1.9063 mL 3.8126 mL 7.6251 mL 9.5314 mL
10 mM 0.1906 mL 0.9531 mL 1.9063 mL 3.8126 mL 4.7657 mL
50 mM 0.0381 mL 0.1906 mL 0.3813 mL 0.7625 mL 0.9531 mL
100 mM 0.0191 mL 0.0953 mL 0.1906 mL 0.3813 mL 0.4766 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Falecalcitriol

Falecalcitriol is an analog of calcitriol. It has a higher potency both in vivo and in vitro systems, and longer duration of action in vivo.

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References on Falecalcitriol

[Long-term suppressive effect of falecalcitriol on parathyroid hormone secretion in secondary hyperparathyroidism in hemodialysis patients].[Pubmed:16679628]

Clin Calcium. 2006 May;16(5):847-51.

Alfacarcidol and calcitriol are widely used to treat secondary hyperparathyroidism associated with chronic renal failure, but it is often not possible to administer doses high enough to sufficiently inhibit parathyroid hormones because of the risk of hypercalcemia and hyperphosphatemia. We administered Falecalcitriol (Hornel) Tablets) to patients with poorly controlled secondary hyperparathyroidism. The usefulness of Falecalcitriol was demonstrated by the fact that control of intact-PTH was maintained for up to 24 months without a clear increase in serum Ca x serum inorganic phosphorus (iP), iP, and ALP levels.

Comparison of oral falecalcitriol and intravenous calcitriol in hemodialysis patients with secondary hyperparathyroidism: a randomized, crossover trial.[Pubmed:19473635]

Clin Nephrol. 2009 Jun;71(6):660-8.

BACKGROUND: Falecalcitriol is a novel vitamin D analog, which has a greater potential to suppress parathyroid hormone (PTH) and a longer half-life. There are few studies to compare clinical effects of oral Falecalcitriol treatment with those of intravenous calcitriol treatment. METHODS: Twenty-one patients with moderate to severe SHPT were included in a random 2 x 2 crossover trial with the two vitamin D analogs (12 weeks for each treatment). The primary endpoint measure was a decrease in serum intact PTH (iPTH) level, and the secondary outcome measures included changes in serum calcium (Ca), phosphate (P), and metabolic bone marker levels. RESULTS: Both treatments decreased iPTH and whole PTH (wPTH) levels by similar degrees (iPTH, -200.1 +/- 107.0 with Falecalcitriol vs. -200.8 +/- 114.9 pg/ml with calcitriol, p = 0.9895; wPTH, -137.1 +/- 73.1 with Falecalcitriol vs. -120.4 +/- 81.1 pg/ml with calcitriol, p = 0.5603). Serum Ca, P, and Ca x P product levels at the end of each treatment were comparable and the frequencies of hypercalcemia and hyperphosphatemia were also similar during each treatment period. Although intravenous calcitriol treatment significantly changed intact osteocalcin and cross-linked N-telopeptide of type I collagen after 12 weeks, oral Falecalcitriol treatment did not change any bone metabolic marker level. CONCLUSION: The present study showed that oral Falecalcitriol treatment is effective for PTH suppression, and Ca and P metabolism in hemodialysis patients with moderate to severe SHPT, as well as intravenous calcitriol administration.

[Falecalcitriol as a new therapeutic agent for secondary hyperparathyroidism].[Pubmed:15632470]

Clin Calcium. 2005 Jan;15(1):29-33.

The 26 and 27 positions of vitamin D molecular structure of calcitriol were fluorinated with 3 atoms of fluorine each and the new compound was named Falecalcitriol (F6). This new compound was found to be 10 to 100 times more active compared with calcitriol depending on the target organs. As a mechanism of strong action of F6 it was discovered that F6 is hydroxylated at 23 position which has almost the same activity as the mother compound. It was also demonstrated that the PTH suppressive effect was relatively stronger than the calcium absorption action from the intestine. Thus F6 was authorized to be applied to the treatment of secondary hyperparathyoroidism in hemodialysed patients as well as to the treatment of hypoparathyroidism.

Description

Falecalcitriol(Fulstan; Hornel) is an analog of calcitriol; has a higher potency both in vivo and in vitro systems, and longer duration of action in vivo.

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