2. GPCR/G Protein
  3. GnRH Receptor
  4. Ganirelix acetate

Ganirelix acetate  (Synonyms: Ganirest)

Cat. No.: HY-109532 Purity: 99.19%
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Ganirelix acetate (Ganirest) is a competitive and selective gonadotropin-releasing hormone (GnRH) antagonist. Ganirelix acetate blocks endogenous GnRH-induced release of luteinizing hormone (LH) and follicle-stimulating hormone. Ganirelix acetate antagonizes Prostaglandin E2 (HY-101952)-induced detrusor overactivity and enhances Carbachol (HY-B1208)-induced detrusor contraction. Ganirelix acetate is applicable to research related to female infertility and detrusor overactivity.

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

Ganirelix acetate

Ganirelix acetate Chemical Structure

CAS No. : 129311-55-3

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Based on 1 publication(s) in Google Scholar

Other Forms of Ganirelix acetate:

Ganirelix acetate Related Antibodies

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  • Purity & Documentation

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Description

Ganirelix acetate (Ganirest) is a competitive and selective gonadotropin-releasing hormone (GnRH) antagonist. Ganirelix acetate blocks endogenous GnRH-induced release of luteinizing hormone (LH) and follicle-stimulating hormone. Ganirelix acetate antagonizes Prostaglandin E2 (HY-101952)-induced detrusor overactivity and enhances Carbachol (HY-B1208)-induced detrusor contraction. Ganirelix acetate is applicable to research related to female infertility and detrusor overactivity[1][2].

IC50 & Target

GnRH[1]
Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
3.6 nM
Compound: 3 (Ganirelix)
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]
In Vitro

Ganirelix (1 nM-1 μM) acetate has no effect on Carbachol-induced or nerve-induced detrusor contractions in isolated bladder preparations from female rats[2].

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

Ganirelix acetate Related Antibodies
In Vivo

Ganirelix (0.1 mg/kg; subcutaneous injection; daily; for 14 consecutive days) acetate reduces plasma LH levels in female rats, significantly attenuates Prostaglandin E2-induced detrusor overactivity, and enhances detrusor contractions induced by high concentrations of Carbachol[2].
Ganirelix (1.4 mg/L; intravesical administration; single dose) acetate regulates normal micturition function in female rats by prolonging micturition intervals, increasing voided volume and bladder capacity, while reducing basal urodynamic pressure, threshold urodynamic pressure and maximum urodynamic pressure parameters; its reduction in flow pressure does not reach statistical significance[2].

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

Animal Model: Sprague-Dawley (female, 225-300 g, intravesical infusion of 50 μM prostaglandin E2-induced detrusor overactivity)[2]
Dosage: 0.1 mg/kg
Administration: s.c.; daily; 14 days
Result: Reduced plasma luteinising hormone (LH) levels to 0.48 ng/mL.
Reduced micturition interval (MI) by 22%.
Reduced micturition volume (MV) by 23%.
Reduced bladder capacity (BC) by 21% (.
Increased threshold pressure (TP) by 16%.
Increased flow pressure (FP) by 16%.
Enhanced maximal carbachol-induced contraction force to 231% of 60 mM K+-induced contractions at 10 μM Carbachol.
Showed no significant differences in body weight, bladder weight, or baseline urodynamic parameters compared to controls.
Animal Model: Sprague-Dawley (female, 225-300 g)[2]
Dosage: 1.4 mg/L; 0.14 mg/L
Administration: intravesical; single dose
Result: Increased micturition interval (MI) to 7.06 min at 1.4 mg/L.
Increased micturition volume (MV) to 1.17 mL at 1.4 mg/L.
Increased bladder capacity (BC) to 1.17 mL 1.4 mg/L.
Reduced basal pressure (BP) to 21.5 cm H2O at 1.4 mg/L.
Reduced threshold pressure (TP) to 34.9 cm H2O at 1.4 mg/L.
Reduced maximum pressure (MP) to 126.0 cm H2O at 1.4 mg/L.
Reduced flow pressure (FP) with no statistical significance at 1.4 mg/L.
Showed no effect on any measured urodynamic parameters at 0.14 mg/L.
Molecular Weight

1690.42

Formula

C84H121ClN18O17
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC(C=C1)=CC=C1C[C@H](NC([C@H](CO)NC([C@@H](CC2=CN=CC=C2)NC([C@H](NC([C@H](NC(C)=O)CC3=CC4=CC=CC=C4C=C3)=O)CC5=CC=C(Cl)C=C5)=O)=O)=O)C(N[C@H](CCCC/N=C(NCC)/NCC)C(N[C@@H](CC(C)C)C(N[C@@H](CCCC/N=C(NCC)/NCC)C(N6[C@@H](CCC6)C(N[C@H](C)C(N)=O)=O)=O)=O)=O)=O.CC(O)=O.CC(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (29.58 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.5916 mL 2.9578 mL 5.9157 mL
5 mM 0.1183 mL 0.5916 mL 1.1831 mL
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 (protect from light, stored under nitrogen). 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)

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 50 mg/mL (29.58 mM); Clear solution; Need ultrasonic

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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 (protect from light, stored under nitrogen). 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 0.5916 mL 2.9578 mL 5.9157 mL 14.7892 mL
5 mM 0.1183 mL 0.5916 mL 1.1831 mL 2.9578 mL
10 mM 0.0592 mL 0.2958 mL 0.5916 mL 1.4789 mL
15 mM 0.0394 mL 0.1972 mL 0.3944 mL 0.9859 mL
20 mM 0.0296 mL 0.1479 mL 0.2958 mL 0.7395 mL
25 mM 0.0237 mL 0.1183 mL 0.2366 mL 0.5916 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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Ganirelix acetate Related Classifications

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:

Ganirelix129311-55-3GanirestGnRH ReceptorGonadotropin releasing hormone receptorGNRHRGnRH receptorProstaglandin E2CarbacholestradiolSprague-DawleyDetrusor overactivityfemale infertilityInhibitorinhibitorinhibit

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