Melanocortin Receptor Antagonist

Melanocortin Receptor Antagonists (34):

Cat. No.	Product Name	Effect	Purity

HY-P0267

Melanotan (MT)-II	Antagonist	99.97%
Melanotan (MT)-II, a synthetic melanocortin receptor agonist, is an injectable peptide hormone used to promote tanning.

HY-P5971

TCMCB07	Antagonist	99.86%
TCMCB07, a cyclic nonapeptide peptide, is an orally active and brain-penetrant melanocortin receptor 4 (MC4R) antagonist. TCMCB07 plays an important role in cachexia. TCMCB07 has potential transport capabilities.

HY-107139

JNJ-10229570	Antagonist	98.0%
JNJ-10229570 is an antagonist of melanocortin receptor 1 (MC1R) and melanocortin receptor 5 (MC5R), which inhibits sebaceous gland differentiation and the production of sebum-specific lipids. JNJ-10229570 inhibits the binding of ¹²⁵I-NDP-α-MSH to cells expressing human MC1R and MC5R, with IC₅₀ values of 270 nM and 200 nM, respectively.

HY-P0097A

Nonapeptide-1 acetate salt	Antagonist
Nonapeptide-1 (Melanostatine-5) acetate salt, a peptide hormone, is a selective antagonist of MC1R (K_i: 40 nM). Nonapeptide-1 acetate salt is a competitive α-MSH antagonist that potently inhibits intracellular cAMP and melanosome dispersion induced by α-MSH in melanocytes (IC₅₀: 2.5 nM and 11 nM, respectively). Nonapeptide-1 acetate salt inhibits melanin synthesis, and can be used in the research of skin pigmentation and regulation of steroid production in the adrenal gland, skin cancer.

HY-P1726

MSG606	Antagonist	98.06%
MSG606 is a selective melanocortin 1 receptor (MC1R) antagonist. MSG606 can abolish the neuroprotective effects of BMS-470539 (HY-15616) (MC1R agonist). MSG606 can inhibit cancer cell proliferation and transition from the G1 to the S phase. MSG606 can delay pain hypersensitivity and reduce cholesterol levels. MSG606 can be used for the researches of cancer, inflammation, neurological and metabolic disease, such as breast cancer and subarachnoid hemorrhage (SAH).

HY-P1215A

HS024 TFA	Antagonist	99.80%
HS024 is a selective MC4 receptor antagonist, with K_is of 0.29, 3.29, 5.45, 18.6 nM for MC4, MC5, MC3, and MC1, respectively. HS024 increase food intake.

HY-148349

PF-07258669	Antagonist	98.44%
PF-07258669 is an orally active melanocortin-4 receptor (MC4R) antagonist that antagonizes MC4R with an IC₅₀ of 13 nM (K_i=0.46 nM). PF-07258669 can be used for the research of cachexia, anorexia, or anorexia nervosa.

HY-11030A

SNT-207858 free base	Antagonist	99.66%
SNT207858 free base is a selective, blood brain barrier penetrating, potent and orally active melanocortin-4 (MC-4) receptor antagonist. SNT207858 free base has an IC₅₀ of 22 nM (binding) and 11 nM (function) on the MC-4 receptor.

HY-P5971A

TCMCB07 TFA	Antagonist	99.69%
TCMCB07 TFA, a cyclic nonapeptide peptide, is an orally active and brain-penetrant melanocortin receptor 4 (MC4R) antagonist. TCMCB07 TFA plays an important role in cachexia.

HY-P1558

ACTH (11-24)	Antagonist	99.90%
ACTH (11-24) is an adrenocorticotropic hormone (ACTH) receptor antagonist. ACTH (11-24) is a fragment of adrenocorticotropic and induces cortisol release. ACTH (11-24) can be used for the research of central nervous system.

HY-P0097

Nonapeptide-1	Antagonist	99.04%
Nonapeptide-1 (Melanostatine-5), a peptide hormone, is a selective antagonist of MC1R (K_i: 40 nM). Nonapeptide-1 is a competitive α-MSH antagonist that potently inhibits intracellular cAMP and melanosome dispersion induced by α-MSH in melanocytes (IC₅₀: 2.5 nM and 11 nM, respectively). Nonapeptide-1 inhibits melanin synthesis, and can be used in the research of skin pigmentation and regulation of steroid production in the adrenal gland, skin cancer.

HY-P1209A

PG106 TFA	Antagonist	98.13%
PG106 TFA is a potent and selective human melanocortin 3 (hMC3) receptor antagonist (IC₅₀= 210 nM) and has noactivity at hMC4 receptors (EC₅₀=9900 nM) and hMC5 receptor.

HY-P4874

ACTH (7-38) (human)	Antagonist	99.57%
ACTH (7-38) (human) is the 7-38 fragment of human ACTH (1-39). human ACTH (1-39), known as a corticotropin inhibitory peptide (CIP), is an antagonist of the ACTH receptor and has no any corticosteroid activity.

HY-124740

ML00253764	Antagonist	99.70%
ML00253764 is a selective melanocortin receptor 4 (MC4R) antagonist, can induce apoptosis by inhibiting ERK1/2 and Akt phosphorylation, and has anticancer activity.

HY-P10571

GPS1573	Antagonist	99.31%
GPS1573 is a noncompetitive antagonist of melanocortin type 2 receptor (MC2R) that dose-dependently antagonizes ACTH-stimulated MC2R activity (IC₅₀=66 nM). GPS1573 can be used in the study of Cushing's disease due to its highly selective antagonism of MC2R.

HY-P1213

JKC363	Antagonist	99.55%
JKC363, a selective melanocortin MC4 receptor antagonist, has a 90-fold higher affinity at the MC4 receptor (IC₅₀=0.5 nM) than at the MC3 receptor (44.9 nM). JKC-363 blocks the stimulatory effect of α-MSH on TRH release. Anti-hyperalgesic effect.

HY-107627

MCL0020	Antagonist	99.93%
MCL0020 is a potent and selective melanocortin MC4 receptor antagonist, with an IC₅₀ of 11.63 nM. MCL0020 dose-dependently and significantly attenuates restraint stress-induced anorexia without affecting food intake.

HY-P1215

HS024	Antagonist
HS024 is a selective MC4 receptor antagonist, with K_is of 0.29, 3.29, 5.45, and 18.6 nM for MC4, MC5, MC3, and MC1, respectively. HS024 increase food intake.

HY-P99004

hMC1R agonist 1	Antagonist
(EC₅₀=3 nM). hMC1R agonist 1 shows at least 300-fold selectivity for hMC1R over hMC3R (b>EC₅₀=902 nM), hMC4R (b>EC₅₀=915 nM), and hMC5R (b>EC₅₀=>1000 nM). hMC1R agonist 1 has the potential for the therapeutic intervention of melanocortin family.

HY-P1216A

HS014 TFA	Antagonist	99.87%
HS014 TFA is a potent and selective melanocortin-4 (MC4) receptor antagonist, with K_is of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors respectively. HS014 TFA increases food intake in free-feeding rats.

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