CYP11B1 Activators
CYP11B1 activators constitute a diverse group of chemicals that modulate adrenal steroidogenesis by directly or indirectly targeting the enzyme CYP11B1. Direct activators, such as forskolin, angiotensin II, and ACTH (1-24), stimulate CYP11B1 activity through distinct mechanisms. Forskolin enhances intracellular cAMP levels, activating protein kinase A (PKA), which phosphorylates and activates CYP11B1, promoting cortisol synthesis. Angiotensin II, through its receptor (AT1R), increases calcium influx and activates protein kinase C (PKC), enhancing CYP11B1 activity in cortisol synthesis. ACTH (1-24) binds to its receptor (MC2R), initiating cAMP-dependent pathways that stimulate CYP11B1 and promote cortisol production. Indirect activators, including dexamethasone, dopamine, and prostaglandin E2, modulate CYP11B1 activity through various signaling pathways. Dexamethasone, a synthetic glucocorticoid, acts through negative feedback, suppressing ACTH production and subsequently modulating CYP11B1 activity. Dopamine, through dopamine receptors, inhibits adenylate cyclase, decreasing cAMP levels and modulating CYP11B1-mediated cortisol synthesis. Prostaglandin E2, through G protein-coupled receptor signaling, activates adenylate cyclase and PKA, stimulating CYP11B1 activity.
Other activators, such as isoflavone genistein, adenosine, and melatonin, exert their effects by influencing estrogen receptor signaling, adenosine receptor signaling, and melatonin receptor signaling, respectively. These compounds modulate cAMP levels, activating or inhibiting PKA, and ultimately affecting CYP11B1 activity in cortisol synthesis. The diverse mechanisms of action of these activators highlight the intricate regulation of adrenal steroidogenesis and provide valuable insights into potential strategies for conditions associated with cortisol dysregulation. Understanding the complexities of CYP11B1 activation by these compounds contributes to our knowledge of endocrine regulation and adrenal function.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Forskolin | 66575-29-9 | sc-3562 sc-3562A sc-3562B sc-3562C sc-3562D | 5 mg 50 mg 1 g 2 g 5 g | $76.00 $150.00 $725.00 $1385.00 $2050.00 | 73 | |
Forskolin serves as a direct activator of CYP11B1 by stimulating adenylate cyclase, increasing intracellular cAMP levels. Elevated cAMP levels activate protein kinase A (PKA), which in turn phosphorylates and activates CYP11B1, promoting the conversion of 11-deoxycortisol to cortisol. | ||||||
Angiotensin II, Human | 4474-91-3 | sc-363643 sc-363643A sc-363643B sc-363643C | 1 mg 5 mg 25 mg 100 mg | $50.00 $75.00 $260.00 $505.00 | 3 | |
Angiotensin II acts as an indirect activator of CYP11B1 by binding to its receptor (AT1R) and initiating signaling cascades. This results in increased calcium influx and activation of protein kinase C (PKC), ultimately enhancing CYP11B1 activity and cortisol synthesis in the adrenal glands. | ||||||
22(R)-hydroxycholesterol | 17954-98-2 | sc-205106 sc-205106A sc-205106B | 1 mg 5 mg 10 mg | $108.00 $350.00 $600.00 | 1 | |
22(R)-Hydroxycholesterol acts as a direct activator of CYP11B1 by serving as a substrate for the enzyme. This cholesterol derivative is converted by CYP11B1 into 22(R)-hydroxycortisol, a key intermediate in cortisol synthesis, thereby promoting the activity of CYP11B1 in the adrenal steroidogenesis pathway. | ||||||
Dexamethasone | 50-02-2 | sc-29059 sc-29059B sc-29059A | 100 mg 1 g 5 g | $76.00 $82.00 $367.00 | 36 | |
Dexamethasone acts as an indirect activator of CYP11B1 through negative feedback regulation. As a synthetic glucocorticoid, it binds to the glucocorticoid receptor (GR) and suppresses ACTH production, reducing the stimulation of CYP11B1 and ultimately modulating cortisol synthesis in the adrenal glands. | ||||||
Dopamine | 51-61-6 | sc-507336 | 1 g | $290.00 | ||
Dopamine acts as an indirect activator of CYP11B1 by modulating catecholamine signaling. By binding to dopamine receptors, it inhibits adenylate cyclase activity, decreasing cAMP levels and suppressing the PKA-mediated activation of CYP11B1, thereby influencing cortisol synthesis in adrenal cortical cells. | ||||||
PGE2 | 363-24-6 | sc-201225 sc-201225C sc-201225A sc-201225B | 1 mg 5 mg 10 mg 50 mg | $56.00 $156.00 $270.00 $665.00 | 37 | |
Prostaglandin E2 serves as an indirect activator of CYP11B1 through G protein-coupled receptor (EP receptors) signaling. Activation of EP receptors stimulates adenylate cyclase, leading to increased cAMP levels and subsequent activation of PKA, ultimately enhancing CYP11B1 activity in cortisol synthesis. | ||||||
Somatostatin | 51110-01-1 | sc-391009 sc-391009A | 1 mg 5 mg | $112.00 $525.00 | 9 | |
Somatostatin acts as an indirect activator of CYP11B1 by inhibiting adenylate cyclase activity. By binding to somatostatin receptors, it reduces cAMP levels, diminishing PKA activation and subsequently modulating CYP11B1 activity. This inhibition of CYP11B1 leads to altered cortisol synthesis in adrenal cortical cells. | ||||||
Genistein | 446-72-0 | sc-3515 sc-3515A sc-3515B sc-3515C sc-3515D sc-3515E sc-3515F | 100 mg 500 mg 1 g 5 g 10 g 25 g 100 g | $26.00 $92.00 $120.00 $310.00 $500.00 $908.00 $1821.00 | 46 | |
Genistein indirectly activates CYP11B1 by influencing estrogen receptor signaling. By binding to estrogen receptors, it initiates signaling cascades that increase cAMP levels and activate PKA, ultimately stimulating CYP11B1 and promoting cortisol synthesis in adrenal cortical cells. | ||||||
Adenosine | 58-61-7 | sc-291838 sc-291838A sc-291838B sc-291838C sc-291838D sc-291838E sc-291838F | 1 g 5 g 100 g 250 g 1 kg 5 kg 10 kg | $33.00 $47.00 $294.00 $561.00 $1020.00 $2550.00 $4590.00 | 1 | |
Adenosine serves as an indirect activator of CYP11B1 by modulating adenosine receptor signaling. By activating specific adenosine receptors, it inhibits adenylate cyclase activity, reducing cAMP levels and suppressing PKA-mediated activation of CYP11B1, influencing cortisol synthesis in adrenal cortical cells. | ||||||
(−)-Epinephrine | 51-43-4 | sc-205674 sc-205674A sc-205674B sc-205674C sc-205674D | 1 g 5 g 10 g 100 g 1 kg | $40.00 $102.00 $197.00 $1739.00 $16325.00 | ||
Epinephrine acts as an indirect activator of CYP11B1 by binding to adrenergic receptors and initiating signaling cascades. This results in increased calcium influx, activating PKC and ultimately enhancing CYP11B1 activity in cortisol synthesis. Epinephrine's action influences adrenal steroidogenesis by modulating CYP11B1 activity. | ||||||