ChemicalBook CAS DataBase List 872717-97-0

872717-97-0

Name	KISS1-305
CAS	872717-97-0
Molecular Formula	C56H76N16O12
Molecular Weight	1165.3
MOL File	872717-97-0.mol

Chemical Properties

density	1.41±0.1 g/cm3(Predicted)
pka	9.97±0.15(Predicted)
Water Solubility	Soluble to 1 mg/ml in water
Sequence	{d-Try}-{d-Ala(Py)}-Asn-Ser-Phe-{Gly(aza)}-Leu-{Arg(Me)}-Phe-NH2

Hazard Information

Uses

KISS1-305, the Metastin/Kisspeptin analog, is a prototype peptide and a chemical probe. KISS1-305 has suboptimal KISS1R agonistic activity, and resists plasma protease degradation[1].

Biological Activity

KISS1 305 is a potent Kisspeptin1 receptor agonist (EC50 = 10 nM). It binds with high affinity to rat and human KISS1 receptors with Ki values of 0.14 nM and 0.11 nM respectively. In vivo, chronic administration of KISS1 305 reduces plasma testosterone and genital organ weights in male rats.

in vivo

KISS1-305 (4 nmol/h; s.c.) shows suppression of pituitary-gonadal functions^[1].
KISS1-305 causes substantial elevations of plasma LH and testosterone, followed by abrupt reductions of both hormone levels.?KISS1-305 also reduced genital organ weight more profoundly than leuprolide. In mechanistic studies, chronic KISS1-305 administration only transiently induced c-Fos expression in GnRH neurons, suggesting that GnRH-neural response was attenuated over time^[1].

Animal Model:	Adult male Sprague Dawley Crl:CD(SD) rats (8-10 wk of age)^[1]
Dosage:	4 nmol/h
Administration:	s.c.
Result:	Both plasma T and LH levels were markedly increased on d 1 after the initiation of dosing and dramatically decreased thereafter to the lower limit of detection (LH: 0.08 ng/ml; T: 0.04 ng/ml) by d 6.?

storage

Store at -20°C

References

[1] Matsui H, et al.Chronic?administration?of the?metastin/kisspeptin?analog?KISS1-305?or the?investigational?agent?TAK-448?suppresses?hypothalamic?pituitary?gonadal?function?and?depletes?plasma?testosterone?in?adult?male?rats.Endocrinology.?2012 Nov;153(11):5297-308. DOI:10.1210/en.2012-1388

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