Nicotinic Acid is a water-soluble vitamin belonging to the vitamin B family. Nicotinic acid (Niacin) plays a key role in energy metabolism, cell signaling cascades regulating gene expression and apoptosis. Nicotinic acid (Niacin) is also used in the study of cardiovascular diseases.
Niacin (0-900 μM, 42 hours) significantly increases GSH levels and decreases ROS levels, and affects the expression of genes related to apoptosis and lipid metabolism. Niacin (0-40 μM, 24 hours) can inhibit cancer invasive activity at low dose but with no influence on proliferation.
Niacin (3-300 mg/kg; subcutaneous injection; once) can induce vasodilation in a dose-dependent manner within minutes in male C57BL/6 mice.
|Solubility (25°C)||DMSO 30 mg/mL
Water 10 mg/mL
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|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
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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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