Date published: 2025-11-21

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MC1-R Activators

MC1-R activators comprise a group of molecules that stimulate the melanocortin 1 receptor, a key regulator of skin pigmentation. These activators include both natural ligands and synthetic analogues, as well as compounds that indirectly influence the receptor's signaling pathways. The primary function of MC1-R in melanogenesis makes these activators significant for their involvement in modulating skin pigmentation. Synthetic analogues of α-MSH, including NDP-MSH, Melanotan I, and Melanotan II, have been developed to mimic and potentiate the effects of natural ligands. These analogues bind to MC1-R with higher affinity and stability than α-MSH, leading to enhanced melanogenic responses. Bremelanotide, another synthetic peptide, demonstrates significant efficacy in activating MC1-R, contributing to its role in skin tanning processes.In addition to direct agonists, several compounds can indirectly activate MC1-R-mediated pathways. Forskolin, a plant-derived compound, elevates intracellular cAMP levels, thereby mimicking the downstream effects of MC1-R activation. Similarly, IBMX and PDE4 inhibitors like Rolipram increase cAMP levels by inhibiting phosphodiesterases, enzymes responsible for cAMP degradation. These increased cAMP levels can amplify the signaling cascade initiated by MC1-R activation, resulting in enhanced melanin synthesis. Furthermore, 8-Br-cAMP, a cAMP analogue, directly activates cAMP-dependent pathways, bypassing MC1-R but achieving similar outcomes in terms of melanogenesis. Histamine, under certain conditions, can modulate cAMP levels and indirectly influence MC1-R signaling, showcasing the interconnected nature of cellular signaling pathways. L-tyrosine, a melanin precursor, plays a supportive role in MC1-R mediated melanogenesis by providing the substrate necessary for melanin production. Overall, MC1-R activators represent a diverse class of compounds that either directly stimulate MC1-R or enhance its signaling pathways.
Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

α-Melanocyte stimulating hormone

581-05-5sc-364762
sc-364762A
sc-364762B
1 mg
5 mg
25 mg
$84.00
$210.00
$926.00
(0)

α-Melanocyte stimulating hormone (α-MSH) acts as a potent agonist for the MC1-R receptor, initiating a cascade of intracellular signaling pathways. Its unique peptide structure facilitates specific interactions with receptor binding sites, leading to the activation of adenylate cyclase and increased cAMP levels. This modulation of signaling pathways influences melanogenesis and skin pigmentation. Additionally, α-MSH exhibits distinct stability in physiological conditions, enhancing its functional efficacy in cellular environments.

BMS 470539 dihydrochloride

457893-92-4sc-362716
sc-362716A
sc-362716B
10 mg
50 mg
100 mg
$428.00
$1714.00
$3264.00
4
(0)

BMS 470539 dihydrochloride selectively targets the MC1-R receptor, exhibiting high affinity and specificity. Its unique structural features enable it to stabilize receptor conformation, promoting effective G-protein coupling. This interaction triggers downstream signaling cascades, notably enhancing intracellular calcium mobilization and influencing gene expression. The compound's robust binding kinetics and resistance to enzymatic degradation further contribute to its prolonged activity within cellular systems, making it a noteworthy candidate for exploring receptor dynamics.

Forskolin

66575-29-9sc-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
(3)

Forskolin indirectly activates MC1-R by elevating intracellular cAMP levels. Although it does not bind directly to MC1-R, its effect on cAMP levels can enhance MC1-R mediated signaling pathways.

IBMX

28822-58-4sc-201188
sc-201188B
sc-201188A
200 mg
500 mg
1 g
$159.00
$315.00
$598.00
34
(1)

IBMX, a nonspecific inhibitor of phosphodiesterases, indirectly activates MC1-R by preventing the breakdown of cAMP. Elevated cAMP levels can amplify the signaling downstream of MC1-R activation.

8-Bromo-cAMP

76939-46-3sc-201564
sc-201564A
10 mg
50 mg
$97.00
$224.00
30
(1)

8-Br-cAMP is a cAMP analogue that can mimic the intracellular effects of MC1-R activation. It bypasses the receptor and directly activates cAMP-dependent pathways, influencing melanogenesis.

Rolipram

61413-54-5sc-3563
sc-3563A
5 mg
50 mg
$75.00
$212.00
18
(1)

PDE4 inhibitors, such as Rolipram, increase cAMP levels by inhibiting its breakdown. This action indirectly activates the pathways downstream of MC1-R, enhancing melanin synthesis.

Histamine, free base

51-45-6sc-204000
sc-204000A
sc-204000B
1 g
5 g
25 g
$92.00
$277.00
$969.00
7
(1)

Histamine can indirectly influence MC1-R signaling by modulating cAMP levels in certain cellular contexts, thereby impacting melanogenesis.

L-Tyrosine

60-18-4sc-473512
sc-473512A
sc-473512B
sc-473512C
100 g
250 g
1 kg
5 kg
$51.00
$209.00
$1637.00
$8165.00
1
(1)

L-tyrosine, a precursor of melanin, can indirectly enhance MC1-R signaling by providing the necessary substrate for melanin synthesis. While it does not directly activate MC1-R, its availability is critical for the effectiveness of MC1-R mediated melanogenesis.