Calcitriol is an Active metabolite of vitamin D3 that activates the vitamin D receptor. Calcitriol (also called 1,25-dihydroxyvitamin D3) is synthesized from 7-dehydrocholesterol in humans via a non-enzymatic photochemical reaction with 290-310 nm UV light in the skin. Calcitriol also inhibits the release of calcitonin, a hormone which reduces blood calcium primarily by inhibiting calcium release from bone. Calcitriol inhibits in vivo and in vitro cell proliferation in a wide range of cells including breast, prostate, colon, skin and brain carcinomas and myeloid leukemia cells. Calcitriol increases blood calcium levels ( [Ca2+] ) by promoting absorption of dietary calcium from the gastrointestinal tract and increasing renal tubular reabsorption of calcium thus reducing the loss of calcium in the urine. Calcitriol also stimulates release of calcium from bone by its action on the specific type of bone cells referred to as osteoblasts, causing them to release RANKL, which in turn activates osteoclasts.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO 56 mg/mL|
|Storage||-20°C, protect from light, dry, sealed|
Calcitriol in cancer treatment: from the lab to the clinic.
Beer TM, et al. Mol Cancer Ther. 2004 Mar;3(3):373-81. PMID: 15026558.
The in vitro effect of calcitriol on parathyroid cell proliferation and apoptosis.
Canalejo A, et al. J Am Soc Nephrol. 2000 Oct;11(10):1865-72. PMID: 11004217.
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