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Bremelanotide Acetate

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Bremelanotide Acetate Basic information

Product Name:
Bremelanotide Acetate
Synonyms:
  • α-MSH (PT-141),Bremelanotide
  • Bremelanotide acetate (PT-141 acetate)
  • 189691-06-3 (free base)
  • PT-141 ACETATE;189691-06-3 (FREE BASE)
  • Bremelanotide Acetate
  • Melanocortin Receptor,inhibit,PT141,Bremelanotide Acetate,MC Receptor,PT 141,Inhibitor,PT-141
  • Bremelanotide Acetate, 10 mM in DMSO
  • Bremelanotide acetate - Bio-X ?
CAS:
1607799-13-2
MF:
C52H72N14O12
MW:
1085.23
Mol File:
1607799-13-2.mol
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Bremelanotide Acetate Chemical Properties

storage temp. 
Store at -20°C
solubility 
DMF: 10 mg/ml; DMSO: 10 mg/ml; Ethanol: 10 mg/ml; PBS (pH 7.2): 5 mg/ml
form 
A solid
color 
White to off-white
Sequence
Ac-[Nle}-Asp-His-{d-Phe}-Arg-Trp-Lys (Lactam bridge: Asp4-Lys7)
InChIKey
MAYUSRUHXFWITM-UKGCEBKRNA-N
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Bremelanotide Acetate Usage And Synthesis

Description

Bremelanotide Acetate (PT-141 Acetate), a synthetic peptide analogue of α-MSH, is an agonist at melanocortin receptors including the MC3R and MC4R for the treatment of sexual dysfunction.. In Vivo: Bremelanotide Acetate (50-200 μg/kg; s.c.; once) significantly increases proceptive solicitations in females primed with Estradiol benzoate+Progesterone or Estradiol benzoate alone in bilevel chambers.

Uses

Bremelanotide is a novel drug candidate for the treatment of male and female sexual dysfunction. Bremelanotide has shown promise in effectively treating erectile dysfunction (ED) without the cardiovascular effects found in ED drugs currently available. Bremelanotide works through a mechanism of action involving the central nervous system rather than directly on the vascular system. As a result, it may offer significant safety and efficacy benefits over currently available products.

Mechanism of action

Bremelanotide Acetate works by activating melanocortin receptors in the central nervous system, primarily the melanocortin 4 receptor (MC4R). The melanocortin system is known to play a critical role in a variety of physiological processes, including energy homeostasis, inflammation, and sexual function.

Side effects

The most common adverse reactions reported include nausea, flushing, injection site reactions, and headache.

in vivo

Bremelanotide Acetate (50-200 μg/kg; s.c.; once) significantly increases proceptive solicitations in females primed with Estradiol benzoate+Progesterone or Estradiol benzoate alone in bilevel chambers[2].

Animal Model:Ovariectomized Long–Evans rats[2]
Dosage:50, 100, 200 μg/kg
Administration:s.c.; once
Result:Significantly increased proceptive solicitations in females primed with Estradiol benzoate+Progesterone or Estradiol benzoate alone in bilevel chambers.

IC 50

MC3R; MC4R

Bremelanotide AcetateSupplier

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