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Calcitriol

Cat. No. M2174
Calcitriol Structure
Synonym:

1,25-Dihydroxyvitamin D3

Size Price Availability Quantity
2mg USD 90  USD100 In stock
5mg USD 211.5  USD235 In stock
10mg USD 427.5  USD475 In stock
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Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 416.64
Formula C27H44O3
CAS Number 32222-06-3
Purity 98.41%
Solubility DMSO 56 mg/mL
Storage -20°C, protect from light, dry, sealed
References

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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Keywords: Calcitriol, 1,25-Dihydroxyvitamin D3 supplier, Estrogen Receptor, inhibitors

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