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SML2756

Sigma-Aldrich

Bremelanotide acetate

≥98% (HPLC)

Sinonimo/i:

Ac-Nle-Asp-His-D-Phe-Arg-Trp-Lys (Asp-Lys), acetate salt, Acetyl-[Nle4, Asp5, D-Phe7, Lys10]-cyclo-α-melanocyte, PT 141 acetate, PT-141 acetate, PT141 acetate

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About This Item

Formula empirica (notazione di Hill):
C50H68N14O10 · xC2H4O2
Numero CAS:
1607799-13-2
Peso molecolare:
1025.16 (free base basis)
Codice UNSPSC:
12352200
NACRES:
NA.77

Livello qualitativo

100

Saggio

≥98% (HPLC)

Stato

powder

Condizioni di stoccaggio

desiccated

Colore

white to off-white

Condizioni di spedizione

wet ice

Temperatura di conservazione

−20°C

Stringa SMILE

[nH]1cncc1C[C@@H]2NC(=O)[C@H](CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](NC2=O)Cc5ccccc5)CCCN=C(N)N)Cc3c4c([nH]c3)cccc4)C(=O)O)NC(=O)[C@@H](NC(=O)C)CCCC.OC(=O)C

InChI

1S/C50H68N14O10.C2H4O2/c1-3-4-16-35(58-29(2)65)43(67)64-41-25-42(66)54-20-11-10-18-37(49(73)74)60-46(70)39(23-31-26-56-34-17-9-8-15-33(31)34)62-44(68)36(19-12-21-55-50(51)52)59-45(69)38(22-30-13-6-5-7-14-30)61-47(71)40(63-48(41)72)24-32-27-53-28-57-32;1-2
MAYUSRUHXFWITM-GBRHMYBBSA-N

Azioni biochim/fisiol

Brain-penetrant alpha-melanocyte-stimulating hormone (α-MSH)-derived melanocortin receptors (MC1R, MC3R, MC4R) agonist with in vivo sexual arousal efficacy.
Bremelanotide (PT-141) is a brain-penetrant, alpha-melanocyte-stimulating hormone (α-MSH)-derived cyclic heptapeptide agonist toward melanocortin receptors, including MC1R, MC3R and MC4R (affinty = 10 nM by competitive binding against 0.2 nM NDP-α-MSH using human MC4R-expressing HEK-293). Bremelanotide induces cAMP accumulation in hMC4R-expressing HEK-293 cells and exhibits in vivo sexual arousal efficacy among both male (50 μg/kg intranasally or 50-500 pg/kg via lateral ventricle injection) and female rats (100-200 μg/kg sc or 800 μg/kg via lateral ventricle injection) by activating neurons in brain regions responsible for sexual function.

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

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Certificati d'analisi (COA)

Lot/Batch Number

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K L Aughton et al.
British journal of pharmacology, 155(2), 236-243 (2008-07-01)
Hypothalamic neuropeptides centrally modulate sexual arousal. However, the role of neuropeptides in peripheral arousal has been ignored. Vascular and non-vascular smooth muscle relaxation in the vagina is important for female sexual arousal. To date, in vitro studies have focused on
P B Molinoff et al.
Annals of the New York Academy of Sciences, 994, 96-102 (2003-07-10)
PT-141, a synthetic peptide analogue of alpha-MSH, is an agonist at melanocortin receptors including the MC3R and MC4R, which are expressed primarily in the central nervous system. Administration of PT-141 to rats and nonhuman primates results in penile erections. Systemic

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