KISS1-305
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.
- CAS No.: 872717-97-0
- Formula: C56H76N16O12
- Molecular Weight:1165.30
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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Cell Line
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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] |
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.
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Animal Model:Adult male Sprague Dawley Crl:CD(SD) rats (8-10 wk of age)[1]
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Dosage:4 nmol/h
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Administration:s.c.
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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.
Chemical Information
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CAS No. 872717-97-0
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Molecular Weight 1165.30
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Formula C56H76N16O12
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Sequence
{d-Try}-{d-Ala(Py)}-Asn-Ser-Phe-{Gly(aza)}-Leu-{Arg(Me)}-Phe-NH2
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Sequence Shortening
{d-Try}-{d-Ala(Py)}-NSF-{Gly(aza)}-L-{Arg(Me)}-F-NH2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)