B2141-1mg | Calcitriol [32222-06-3] Clinisciences

Background

Calcitriol is a form of Vitamin D, is converted to metabolites more potent and rapidly acting than other forms of Vitamin D [1].

Calcitriol has played an important role in mineral and skeletal homeostasis by regulating the differentiation, growth and the function of the cell immune system. In vitro studies, Calcitriol has been reported to dose-dependently inhibit the production of tumor necrosis factor-α(TNF-α) and interleukin-1β(IL-1β) in human peripheral blood cells (PBMC) stimulated by LPS. Furthermore, Calcitriol has been revealed to significantly reduced the basal intradialytic increases of TNF-αand IL-1βin vivo studies. Apart from these, Calcitriol has also been reported to modulate the cytokine production indirectly through the effect on calcium and PTH metabolism [2].

References:
[1] Holick MF, Schnoes HK, DeLuca HF. Identification of 1,25-dihydroxycholecalciferol, a form of vitamin D3 metabolically active in the intestine. Proc Natl Acad Sci U S A. 1971 Apr;68(4):803-4.
[2] Panichi V1, De Pietro S, Andreini B, Bianchi AM, Migliori M, Taccola D, Giovannini L, Tetta C, Palla R. Calcitriol modulates in vivo and in vitro cytokine production: a role for intracellular calcium. Kidney Int. 1998 Nov;54(5):1463-9.

Product Citation

1. Jie Zhou, et al. "Histone demethylase KDM7A regulates bone homeostasis through balancing osteoblast and osteoclast differentiation." Cell Death Dis. 2024 Feb 12;15(2):136. PMID: 38346941
2. Kumar A, Wilderman PR, et al. "Evidence of Allosteric Coupling between Substrate Binding and Adx Recognition in the Vitamin D Carbon-24 Hydroxylase CYP24A1." Biochemistry. 2020;59(15):1537-1548. PMID: 32259445

Chemical Properties

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	416.64
Cas No.	32222-06-3
Formula	C27H44O3
Solubility	insoluble in H2O; ≥20.83 mg/mL in DMSO; ≥43.5 mg/mL in EtOH
Chemical Name	(1R,3S,5Z)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(2R)-6-hydroxy-6-methylheptan-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexane-1,3-diol
SDF	Download SDF
Canonical SMILES	CC(CCCC(C)(C)O)C1CCC2C1(CCCC2=CC=C3CC(CC(C3=C)O)O)C
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment [1]:
Cell lines	Basal cell carcinoma (BCC) cell line ASZ001
Preparation method	The solubility of this compound in DMSO is > 20.8mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.
Reacting condition	10 nM, 48 h
Applications	In BCC ASZ001 cells, calcitriol significantly inhibited the Hh-signaling pathway and activated the Vdr-signaling pathway. Calcitriol suppressed cell proliferation but had no effect on apoptosis for caspase 3/7 activity was unchanged.
Clinical experiment [2]:
Clinical samples	Patients with recent-onset type 1 diabetes aged 11–35 years
Dosage form	0.25 μg/day, for 2 years
Application	At 6, 12, and 24 months, A1C, C-peptide, and insulin requirement values had no difference between calcitriol and placebo groups. These results indicated that at the doses used, calcitriol was not able to protect β-cell function in subjects with recent-onset type 1 diabetes and high C-peptide.
Other notes	Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
References: [1]. Uhmann A, Niemann H, Lammering B, et al. Antitumoral effects of calcitriol in basal cell carcinomas involve inhibition of hedgehog signaling and induction of vitamin D receptor signaling and differentiation[J]. Molecular cancer therapeutics, 2011, 10(11): 2179-2188. [2]. Bizzarri C, Pitocco D, Napoli N, et al. No Protective Effect of Calcitriol on β-Cell Function in Recent-Onset Type 1 Diabetes[J]. Diabetes care, 2010, 33(9): 1962-1963.

Quality Control

Purity = 99.73%

Calcitriol [32222-06-3]

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