KISS1-305

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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.

For research use only. We do not sell to patients.

KISS1-305 Chemical Structure

CAS No. : 872717-97-0

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Description

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].

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	0.27 nM Compound: 1	Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay Agonist activity at human KISS1R expressed in CHO cells assessed as increase in calcium mobilization measured at 2 secs interval for 2 mins by fluo-4 NW dye based FLIPR assay	[PMID: 30598349]
CHO	EC₅₀	10 nM Compound: 4	Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay	[PMID: 24918545]
CHO	EC₅₀	2.6 nM Compound: 4	Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay	[PMID: 24918545]
CHO	IC₅₀	8.94 nM Compound: 26	Inhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assay Inhibition of human KISS1R expressed in CHO cells assessed as inhibition of KISS1R-mediated cell growth after 4 days by cell counting kit-8 assay	[PMID: 24047141]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Molecular Weight

1165.30

Formula

C₅₆H₇₆N₁₆O₁₂

CAS No.

872717-97-0

Sequence

{d-Try}-{d-Ala(Py)}-Asn-Ser-Phe-{Gly(aza)}-Leu-{Arg(Me)}-Phe-NH2

Sequence Shortening

{d-Try}-{d-Ala(Py)}-NSF-{Gly(aza)}-L-{Arg(Me)}-F-NH2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

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. [Content Brief]

KISS1-305 Related Classifications

Endocrinology

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KISS1-305872717-97-0Kisspeptin ReceptorOthersKiss1RGPR54proteasedegradationprototypepeptideprobeplasmatestosteronehormonec-FosInhibitorinhibitorinhibit

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