α-msh

α-MSH (MSH, amide) is amide stimulates melanocortin 1 receptor that results in the activation of adenylyl cyclase.

α-Melanocyte-stimulating hormone (α-MSH) is a 13-amino acid peptide hormone produced by post-translational processing of proopiomelanocortin (POMC) in the pituitary gland, as well as in keratinocytes, astrocytes, monocytes, and gastrointestinal cells.1It is an agonist of melanocortin receptor 3 (MC3R) and MC4R that induces cAMP production in Hepa cells expressing the human receptors (EC50s = 0.16 and 56 nM, respectively).2α-MSH (100 pM) reducesS. aureuscolony formation andC. albicansgerm tube formationin vitro.3It inhibits endotoxin-, ceramide-, TNF-α-, or okadaic acid-induced activation of NF-κB in U937 cells.1α-MSH reduces IL-6- or TNF-α-induced ear edema in mice.4It also prevents the development of adjuvant-induced arthritis in rats and increases survival in a mouse model of septic shock. Increased plasma levels of α-MSH are positively correlated with delayed disease progression and reduced death in patients with HIV.1 1.Catania, A., Airaghi, L., Colombo, G., et al.α-melanocyte-stimulating hormone in normal human physiology and disease statesTrends Endocrinol. Metab.11(8)304-308(2000) 2.Miwa, H., Gantz, I., Konda, Y., et al.Structural determinants of the melanocortin peptides required for activation of melanocortin-3 and melanocortin-4 receptorsJ. Pharmacol. Exp. Ther.273(1)367-372(1995) 3.Cutuli, M., Cristiani, S., Lipton, J.M., et al.Antimicrobial effects of a-MSH peptidesJ. Leukoc. Biol.67(2)233-239(2000) 4.Lipton, J.M., Ceriani, G., Macaluso, A., et al.Antiiinflammatory effect of the neuropeptide a-MSH in acute, chronic, and systemic inflammationAnn. N.Y. Acad. Sci.25(741)137-148(1994)

(Nle4)-α-MSH, a synthetic analogue of the melanocyte-stimulating hormone α-MSH, exhibits the capability to reversibly darken frog skin. Additionally, it demonstrates sustained activity following exposure to heat and alkali treatment [1].

(D-Phe7)-α-MSH, an α-MSH analogue, [1].

Ac-[Nle4,D-Phe7]-α-MSH (4-10)-NH2, a melanotropin derivative and melanocyte-stimulating hormone, activates tyrosinase and demonstrates a thermoregulatory effect in rat models [1][2].

Acetyl-α-MSH (11-13), the acetylated C-terminal tripeptide of α-MSH, exhibits antipyretic and anti-inflammatory effects [1] [2].

a-MSH, amide Acetate as an endogenous neuropeptide. It is an endogenous melanocortin receptor 4 (MC4R) agonist with anti-inflammatory and antipyretic activities. α-MSH is a post-translational derivative of pro-opiomelanocortin (POMC)

β-Endorphin (β-EP) is an endogenous opioid neuropeptide with diverse biological activities. It is produced via piomelanocortin cleavage in the pituitary gland, hypothalamus, and in lymphocytes, then migrates to its sites of action which include plasma, gut, skin, placenta, cerebrospinal fluid, and cardiac tissues. β-EP induces concentration-dependent decreases in electrically stimulated contraction of the mouse vas deferens that can be reversed by the μ-opioid antagonist CTP and δ-opioid antagonist ICI 174,864. In vivo, β-EP (5 μg, i.c.v.) slows gastrointestinal transit in mice. β-EP (0.5 or 5 μg, i.c.v.) stimulates food intake in rats for 4 to 6 hours, however, this effect is not prolonged with continuous infusion. It antagonizes the appetite-suppressive effects of α-melanocyte-stimulating hormone (α-MSH) for the first three days post administration. β-EP also reduces paralytic demyelination induced by the murine coronavirus MHV-JHM in immunocompetent, but not irradiated or immune-incompetent, mice and rats.

Nonapeptide-1 (Melanostatine-5) acetate salt is a peptide hormone that functions as a selective and competitive antagonist of the melanocortin 1 receptor (MC1R) with a binding affinity (K i) of 40 nM. It effectively inhibits α-MSH-induced increases in intracellular cyclic AMP (cAMP) and melanosome dispersion in melanocytes, with inhibitory concentrations (IC 50) of 2.5 nM and 11 nM, respectively. By inhibiting melanin synthesis, Nonapeptide-1 acetate salt is used in research related to skin pigmentation, adrenal gland steroid production regulation, and skin cancer [1] [2] [3].

JKC363 TFA is a selective melanocortin MC4 receptor antagonist that exhibits a 90-fold higher affinity for the MC4 receptor (IC50=0.5 nM) compared to the MC3 receptor (44.9 nM). This compound effectively inhibits the α-MSH-induced stimulation of TRH release. It also demonstrates an anti-hyperalgesic effect [1] [2].

Afamelanotide acetate is a synthetic α-melanocyte stimulating hormone analogue and first-in-class melanocortin-1 receptor agonist, used to for Erythropoietic Protoporphyria.

CCZ01048, an analogue of α-melanocyte-stimulating hormone (α-MSH), demonstrates a high binding affinity for the melanocortin 1 receptor (MC1R), with a Ki of 0.31 nM. It rapidly internalizes into B16F10 melanoma cells and exhibits notable in vivo stability, making it a promising candidate for PET imaging of malignant melanoma [1].

CCZ01048 TFA, an α-MSH analogue, demonstrates a strong binding affinity for the melanocortin 1 receptor (MC1R), displaying a K i value of 0.31 nM. It exhibits rapid internalization into B16F10 melanoma cells and maintains high in vivo stability. CCZ01048 TFA holds potential as an effective agent for PET imaging of malignant melanoma [1].

Bremelanotide Acetate (PT-141 Acetate) is an agonist of melanocortin receptor (MCR) .

(p-Iodo-Phe7)-ACTH (4-10), a derivative of adrenocorticotrophic hormone (ACTH) produced by the anterior pituitary gland, functions as a melanocortin (MC) receptor antagonist and effectively inhibits α-melanocyte-stimulating hormone (α-MSH)-induced excessive grooming behavior in rats [1].

Acetyl-ACTH (2-24) (human, bovine, rat), a proopiomelanocortin (POMC) peptide fragment, includes adrenocorticotrophin (ACTH) precursor of α-MSH and serves as an agonist at the MC-1 receptor [1].

Acetyl-ACTH (3-24) (human, bovine, rat), a segment derived from the proopiomelanocortin (POMC) peptide, functions as an agonist at the MC-1 receptor [1]. Encompassing adrenocorticotrophin (ACTH), a precursor to α-MSH, it illustrates its role within the spectrum of POMC peptides.

Acetyl-ACTH (4-24) (human, bovine, rat), a proopiomelanocortin (POMC) peptide fragment, functions as an agonist at the MC-1 receptor [1]. This compound encompasses a sequence present in adrenocorticotrophin (ACTH), the precursor for α-MSH, illustrating its significant role in the POMC peptide family.

Tetrapeptide, an α-MSH analogue, stimulates melanin production and mitigates DNA damage by attenuating reactive oxidative species generation and augmenting DNA photoproduct repair [1].

Melanotan I is a non-specific melanocortin receptor (MCR) agonist, an α-melanocyte-stimulating hormone (α-MSH) analog, which is injected subcutaneously to increase the amount of melanin in the skin Melanotan I is used as an adjunct to tanning Melanotan I has been used for the prevention of sunlight-induced skin cancers Melanotan I has been used in the study of melanoma and for male erectile dysfunction Melanotan I may be used to prevent sun-induced skin cancer and may be used to study melanoma and male erectile dysfunction.

Nonapeptide-1 acetate salt (158563-45-2 free base) (Melanostatine-5 acetate salt) , a peptide hormone, is a potent α-Melanocyte-stimulating hormone (α-MSH) antagonist, with an IC50 of 11 nM. Nonapeptide-1 acetate salt (158563-45-2 free base) , a peptide hormone, is a potent α-Melanocyte-stimulating hormone (α-MSH) antagonist, with an IC50 of 11 nM.

Adrenocorticotropic Hormone (ACTH) (1-10), human, is a fragment of adrenocorticotropin hormone. It demonstrates weak α-melanocyte stimulating hormone (α-MSH) potency, which is only apparent at high doses (100 and 1000 nM).

Adrenocorticotropic Hormone (ACTH) (1-10), human acetate is a fragment of adrenocorticotropin hormone. Adrenocorticotropic Hormone (ACTH) (1-10), human acetate possesses a weak α-MSH potency only at 100 and 1000 nM.

ACTH 4-11 acetate is an adrenocorticotropin hormone fragment and possesses the same amino acid sequence as α-melanocyte stimulating hormone (MSH) does. ACTH 4-11 acetate exhibits a weak MSH potency only at high doses (100 and 1000 nM).