1. GPCR/G Protein
  2. GnRH Receptor
  3. Acyline

Acyline, a GnRH peptide analogue, is a GnRH antagonist that inhibits gonadotropin and testosterone (T) levels.

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Acyline

Acyline Chemical Structure

CAS No. : 170157-13-8

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Based on 1 publication(s) in Google Scholar

Other Forms of Acyline:

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Description

Acyline, a GnRH peptide analogue, is a GnRH antagonist that inhibits gonadotropin and testosterone (T) levels[1].

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
0.52 nM
Compound: 8
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
[PMID: 17402723]
HEK293 IC50
0.69 nM
Compound: 2
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
[PMID: 16759096]
HEK293 IC50
1.5 nM
Compound: 8
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
[PMID: 17402723]
HEK293 IC50
6.8 nM
Compound: 6 (Acyline)
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
[PMID: 11462984]
Mast cell EC50
461.4 μg/mL
Compound: 2
Histamine release in mast cells by ELISA
Histamine release in mast cells by ELISA
[PMID: 16759096]
In Vivo

Acyline (50 μg, s.c., twice daily, 5 days) can result in disruption of vaginal oestrus and reduce uterine weights in female Kiss1−/−and Gpr54−/− mice, as well as a decrease in LH concentrations of female Kiss1−/− mice[1].
Acyline (50 μg, s.c., once) can reduce FSH concentrations from pre-acyline 1.51 ng/mL to post-acyline 1.27 ng/mL in male Kiss1−/− mice and from pre-acyline 2.87 ng/mL to post-acyline 1.95 ng/mL in male Gpr54−/− mice[1].

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

Animal Model: Female Kiss1−/−and Gpr54−/− mice[1]
Dosage: 50 μg (1 mg/mL in PBS)
Administration: Subcutaneous injection; twice daily; 5 days
Result: 12 Kiss1−/− mice left oestrus within 4 days of 13 mice received acyline while only 2 of 17 mice received vehicle left oestrus. Also, 7 of 8 Gpr54−/− mice received acyline left oestrus compared to 1 of 7 received vehicle.
Reduced uterine weights of Kiss1−/−and Gpr54−/− mice in treated group compared to the vehicle group, and reduced serum LH concentrations in Kiss1−/− mice.
Clinical Trial
Molecular Weight

1533.21

Formula

C80H102ClN15O14

CAS No.
Appearance

Solid

Color

White to off-white

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 3.33 mg/mL (2.17 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.6522 mL 3.2611 mL 6.5223 mL
5 mM --- --- ---
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 0.6522 mL 3.2611 mL 6.5223 mL 16.3057 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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.

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Product Name:
Acyline
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HY-16027
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