| Identification | Back Directory | [Name]
KISS1-305 | [CAS]
872717-97-0 | [Synonyms]
KISS1-305
L-Phenylalaninamide, D-tyrosyl-3-(4-pyridinyl)-D-alanyl-L-asparaginyl-L-seryl-L-phenylalanyl-2-azaglycyl-L-leucyl-N5-[imino(methylamino)methyl]-L-ornithyl- | [Molecular Formula]
C56H76N16O12 | [MOL File]
872717-97-0.mol | [Molecular Weight]
1165.3 |
| Chemical Properties | Back Directory | [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 | Back Directory | [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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