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.
|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|
|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.
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|VDR agonist 2
VDR agonist 2 is a VDR (vitamin D receptor) agonist that can effectively inhibit TGF-β1-induced activation of hepatic stellate cells (HSC).
Atocalcitol, a vitamin D3 analogue, is used in the study for psoriasis.
Elocalcitol (BXL-628) is a selective, orally active vitamin D receptor (VDR) agonist. Elocalcitol shows anti-inflammatory activity. Elocalcitol inhibits growth of prostate cancer cells.
ZK168281 is a 25-carboxylic ester 1α,25(OH)2D3 analog and a pure VDR antagonist with a Kd value of 0.1 nM. ZK168281 is an effective inhibitor of the coactivator (CoA) interaction of its receptor.
MeTC7 is a Vitamin-D receptor (VDR) antagonist. MeTC7 has potent VDR inhibition activity with an IC50 value of 2.9 μM. MeTC7 shows good antitumor effects.
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