Date published: 2026-1-9

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GPR63 Activators

GPR63 activators, as a chemical class, include a variety of compounds that have the capacity to modulate intracellular second messenger systems, particularly those involving cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP). These molecules are pivotal in the transduction of signals from G protein-coupled receptors (GPCRs) to their intracellular targets. Agents like forskolin, isoproterenol, and various prostaglandins can directly or indirectly stimulate the production of cAMP, which is a common downstream effector of many GPCRs, and thereby can alter the activity of a broad range of receptors, potentially including GPR63.

Compounds that inhibit phosphodiesterases, such as IBMX, rolipram, zaprinast, sildenafil, cilostazol, vardenafil, and milrinone, prevent the degradation of cAMP and cGMP, thereby sustaining their signaling and promoting the activity of pathways that are modulated by these cyclic nucleotides. Given the ubiquitous nature of these second messengers in signaling pathways, it is plausible that these compounds can, in a non-selective manner, enhance GPR63 signaling.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Isoproterenol Hydrochloride

51-30-9sc-202188
sc-202188A
100 mg
500 mg
$28.00
$38.00
5
(0)

A beta-adrenergic agonist that increases cAMP levels, possibly influencing GPR63 activity through cAMP-mediated G protein signaling pathways.

IBMX

28822-58-4sc-201188
sc-201188B
sc-201188A
200 mg
500 mg
1 g
$260.00
$350.00
$500.00
34
(1)

Non-specific inhibitor of phosphodiesterases, which increases cAMP by preventing its degradation, potentially modulating GPR63 signaling.

Rolipram

61413-54-5sc-3563
sc-3563A
5 mg
50 mg
$77.00
$216.00
18
(1)

Selective inhibitor of phosphodiesterase 4, increasing cAMP levels and potentially enhancing GPR63 signaling through the cAMP pathway.

Forskolin

66575-29-9sc-3562
sc-3562A
sc-3562B
sc-3562C
sc-3562D
5 mg
50 mg
1 g
2 g
5 g
$78.00
$153.00
$740.00
$1413.00
$2091.00
73
(3)

Directly activates adenylyl cyclase, increasing cAMP levels, which can modulate G protein-coupled receptor signaling including potentially GPR63.

Zaprinast (M&B 22948)

37762-06-4sc-201206
sc-201206A
25 mg
100 mg
$105.00
$250.00
8
(2)

Inhibits phosphodiesterases 5, 6, and 9, increasing cAMP and cGMP levels which could potentially modulate GPR63 activity.

PGE1 (Prostaglandin E1)

745-65-3sc-201223
sc-201223A
1 mg
10 mg
$31.00
$145.00
16
(4)

Activates adenylate cyclase via its receptor, potentially increasing cAMP levels and indirectly affecting GPR63 signaling.

Cilostazol

73963-72-1sc-201182
sc-201182A
10 mg
50 mg
$109.00
$322.00
3
(1)

Inhibits phosphodiesterase 3, increasing cAMP levels, and may influence GPR63 signaling through the cAMP signaling pathway.

Vardenafil

224785-90-4sc-362054
sc-362054A
sc-362054B
100 mg
1 g
50 g
$526.00
$735.00
$16653.00
7
(1)

A phosphodiesterase 5 inhibitor that increases cGMP, potentially influencing cAMP and affecting GPR63 activity.

Milrinone

78415-72-2sc-201193
sc-201193A
10 mg
50 mg
$165.00
$697.00
7
(0)

Inhibits phosphodiesterase 3, leading to increased cAMP levels and potentially modulating GPR63 activity via cAMP-dependent pathways.