CYP2R1 Activators
CYP2R1 activators are a class of chemicals that enhance the enzymatic activity of the cytochrome P450 2R1 (CYP2R1) enzyme, a member of the cytochrome P450 superfamily of enzymes. These enzymes are known for their role in the hydroxylation of various substrates, including the conversion of vitamin D into its more active forms, a process critical for maintaining calcium homeostasis and bone health. CYP2R1 specifically is involved in the hydroxylation of vitamin D3 at the 25-position, producing 25-hydroxyvitamin D3, which is the major circulating form of vitamin D measured in serum to assess an individual's vitamin D status.
Activators of CYP2R1 can either directly interact with the active site of the enzyme, inducing a conformational change that increases its catalytic efficiency, or they may bind to allosteric sites that enhance the enzyme's activity indirectly. Direct activators typically mimic the structural elements of the natural substrate, facilitating the binding and proper orientation of the substrate within the active site for the hydroxylation reaction. These activators could also stabilize the enzyme in a conformation that is more favorable for catalysis. Indirect activators, on the other hand, might increase the expression levels of CYP2R1 by modulating the transcription factors involved in the enzyme's synthesis. They could also affect the stability and turnover of the enzyme or enhance the electron transfer from reducing agents to CYP2R1, thereby increasing its catalytic activity. These activators could further influence the interaction of CYP2R1 with its redox partner proteins, such as cytochrome P450 reductase, which is necessary for the transfer of electrons to CYP2R1 during the hydroxylation process.
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Vitamin A | 68-26-8 | sc-280187 sc-280187A | 1 g 10 g | $377.00 $2602.00 | ||
Retinol is a form of vitamin A that is known to stimulate CYP2R1 expression. Retinol can be oxidized into retinoic acid, which acts as a ligand for nuclear receptors that regulate the transcription of CYP2R1. | ||||||
Lithocholic acid | 434-13-9 | sc-215262 sc-215262A | 10 g 25 g | $83.00 $272.00 | 1 | |
Lithocholic acid is a secondary bile acid that can induce the expression of CYP2R1. It serves as a ligand for nuclear receptors like FXR, which regulate the transcription of CYP2R1. | ||||||
Rosiglitazone | 122320-73-4 | sc-202795 sc-202795A sc-202795C sc-202795D sc-202795B | 25 mg 100 mg 500 mg 1 g 5 g | $118.00 $320.00 $622.00 $928.00 $1234.00 | 38 | |
Rosiglitazone is a PPAR-gamma agonist that can induce the expression of CYP2R1. PPAR-gamma is a nuclear receptor that regulates the transcription of various genes, including CYP2R1. | ||||||
Rifampicin | 13292-46-1 | sc-200910 sc-200910A sc-200910B sc-200910C | 1 g 5 g 100 g 250 g | $95.00 $322.00 $663.00 $1438.00 | 6 | |
Rifampicin is an antibiotic that can induce CYP2R1 expression. It serves as a ligand for PXR, a nuclear receptor that regulates the transcription of various CYP450 enzymes, including CYP2R1. | ||||||
Pioglitazone | 111025-46-8 | sc-202289 sc-202289A | 1 mg 5 mg | $54.00 $123.00 | 13 | |
Pioglitazone is a PPAR-gamma agonist that can induce the expression of CYP2R1. PPAR-gamma is a nuclear receptor that regulates the transcription of various genes, including CYP2R1. | ||||||
Troglitazone | 97322-87-7 | sc-200904 sc-200904B sc-200904A | 5 mg 10 mg 25 mg | $108.00 $200.00 $426.00 | 9 | |
Troglitazone is a PPAR-gamma agonist that can induce the expression of CYP2R1. PPAR-gamma is a nuclear receptor that regulates the transcription of various genes, including CYP2R1. | ||||||
Pregnenolone | 145-13-1 | sc-204860 sc-204860A sc-204860B sc-204860C | 5 g 25 g 100 g 500 g | $85.00 $145.00 $340.00 $1100.00 | ||
Pregnenolone is a steroid hormone that can induce CYP2R1 expression. It serves as a precursor for the synthesis of various steroid hormones, which can act as ligands for nuclear receptors that regulate the transcription of CYP2R1. | ||||||
Cholesterol | 57-88-5 | sc-202539C sc-202539E sc-202539A sc-202539B sc-202539D sc-202539 | 5 g 5 kg 100 g 250 g 1 kg 25 g | $26.00 $2754.00 $126.00 $206.00 $572.00 $86.00 | 11 | |
Cholesterol is a sterol that can induce CYP2R1 expression. It acts as a substrate for CYP2R1, which converts cholesterol into 25-hydroxycholesterol. This metabolite can act as a ligand for nuclear receptors that regulate the transcription of CYP2R1. | ||||||
Progesterone | 57-83-0 | sc-296138A sc-296138 sc-296138B | 1 g 5 g 50 g | $20.00 $51.00 $292.00 | 3 | |
Progesterone is a steroid hormone that can induce CYP2R1 expression. It can act as a ligand for nuclear receptors that regulate the transcription of CYP2R1. | ||||||