1. GPCR/G Protein
  2. Kisspeptin Receptor
  3. KISS1-305

KISS1-305 是一种原型肽和化学探针,是 Metastin/Kisspeptin 类似物。KISS1-305 具有激动 KISS1R 活性,抗血浆蛋白酶降解。

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KISS1-305 Chemical Structure

KISS1-305 Chemical Structure

CAS No. : 872717-97-0

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

细胞效力
(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]
体内研究
(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].

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. 
分子量

1165.30

Formula

C56H76N16O12

CAS 号
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

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
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  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

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产品名称:
KISS1-305
目录号:
HY-P2191
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