Calcipotriol

Short Summary : Vitamin D3 analog,regulates cell differentiation and proliferation

Category : Vitamin D Related|VD/VDR

Purity : 0.9996

CAS Number : 112965-21-6

Formula : C27H40O3

Molecular Weight : 412.62

SMILE : CC(C=CC(C1CC1)O)C2CCC3C2(CCCC3=CC=C4CC(CC(C4=C)O)O)C

Solubility : >16.7mg/mL in DMSO

Storage : Store at -20°C

Description : Calcipotriol is an analogue of vitamin D3. [1]
Calcipotriol is a ligand of VDR-like receptors and is used as a first-line topical agent in the treatment of psoriasis.[1-2] Calcipotriol is much less effective in causing hypercalcemia.[3] The vitamin D receptor is found on the cells of many different tissues including T cells of the immune system. T cells are known to play a role in psoriasis, and the binding of calcipotriol to VDR modulates the T cells gene transcription of cell differentiation and proliferation related genes. Calcipotriol induced apoptosis in eratinocytes isolated from psoriatic plaques at 100 nM for 20 h.[4] Calcipotriol also induced autophagy in both HeLa cells and keratinocytes.[2] Calcipotriol inhibited the proliferation of HL-60 and MCF-7 cells dose-dependently from 1 nM-1000 nM.[5] Calcipotriol is a potent inducer of terminal differentiation in cultured human keratinocytes.[3] Calcipotriol also decreased the mRNA expression/production of human cathelicidin antimicrobial protein (hCAP18) and LL37 peptide by IL-17A/IL-22-stimulated keratinocytes at 40 nM.[6]
References:1. M. R. Klaber, P. E. Hutchinson, A. Pedvis-Leftick, K. Kragballe, T. L. Reunala, P. C. Van de Kerkhof, M. K. Johnsson, L. Molin, M. S. Corbett and N. Downess, Br J Dermatol 1994, 131, 678-683. 2. R. C. Wang and B. Levine, J Invest Dermatol 2011, 131, 990-993. 3. K. Kragballe and I. L. Wildfang, Arch Dermatol Res 1990, 282, 164-167. 4. R. Tiberio, C. Bozzo, G. Pertusi, F. Graziola, M. Gattoni, P. Griffanti, P. Boggio, E. Colombo and G. Leigheb, Clin Exp Dermatol 2009, 34, e972-974. 5. M. Milczarek, M. Chodynski, B. Filip-Psurska, A. Martowicz, M. Krupa, K. Krajewski, A. Kutner and J. Wietrzyk, Cancers (Basel) 2013, 5, 1355-1378. 6. J. Sakabe, T. Umayahara, M. Hiroike, T. Shimauchi, T. Ito and Y. Tokura, Acta Derm Venereol 2014, 94, 512-516.

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