Eldecalcitol is an analog of 1,25-dihydroxyvitamin D3 that improves bone mineral density. Eldecalcitol is orally bioactive, which binds to vitamin D receptors and binding protein for the goal of achieving greater specificity to bind calcium for its absorption. This greater affinity is 2.7-fold that of the active vitamin D form of calcitriol. Eldecalcitol (0-50 nM; 24 h) displays no cytotoxicity, and (0.5-50 nM; 24 h) reduces cell death induced by LPS (5 μg/mL). Eldecalcitol (5 nM; 24 h) inhibits the LPS-induced pyroptosis by activating Nrf2 and its effector molecule HO-1. Eldecalcitol (0.5-50 nM; 24 h) exhibits anti-pyroptotic ability, and decreases NLRP3, caspase-1, and IL-1β expression dose-dependently. Eldecalcitol (0.04-40 nM; 0-48 h) inhibits the proliferation and migration of SCC-15 and CAL-27 cells.
| Molecular Weight | 490.72 |
| Formula | C30H50O5 |
| CAS Number | 104121-92-8 |
| Solubility (25°C) | Methanol 8 mg/mL DMSO 3 mg/mL (ultrasonic and warming and heat to 60°C) |
| Storage | 4°C, protect from light, sealed |
| 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.
[3] Yuko Noguchi, et al. Eldecalcitol for the treatment of osteoporosis
[4] T Matsumoto, et al. Eldecalcitol for the treatment of osteoporosis
[5] Mark Sanford, et al. Eldecalcitol: a review of its use in the treatment of osteoporosis
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