1. GPCR/G Protein
    Neuronal Signaling
  2. Neurokinin Receptor
  3. Fezolinetant

Fezolinetant (Synonyms: ESN-364)

Cat. No.: HY-19632 Purity: 98.29% ee.: 98.04%
Handling Instructions

Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes.

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

Fezolinetant Chemical Structure

Fezolinetant Chemical Structure

CAS No. : 1629229-37-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 307 In-stock
Estimated Time of Arrival: December 31
1 mg USD 120 In-stock
Estimated Time of Arrival: December 31
5 mg USD 390 In-stock
Estimated Time of Arrival: December 31
10 mg USD 570 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1140 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1740 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2740 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

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Description

Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes.

In Vivo

Fezolinetant (ESN364, 1 mg/kg, iv bolus) reversibly inhibits the regular, pulsatile secretion of LH in the ovarectomized ewe. ESN364 represses the pulse pattern of LH in all treated animals. ESN364 (5 mg/kg, p.o.) lowers plasma LH, but not FSH, in the castrated monkey. ESN364 (10, 25, 50 mg/kg, orally) also blocks the LH surge and decreases ovarian hormone levels throughout the menstrual cycle in monkeys[1].

Clinical Trial
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (139.51 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7903 mL 13.9513 mL 27.9026 mL
5 mM 0.5581 mL 2.7903 mL 5.5805 mL
10 mM 0.2790 mL 1.3951 mL 2.7903 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.98 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.98 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.98 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

On the day of the experiment, the NK3R antagonist ESN364 is formulated in physiological saline with 9% 2-hydroxypropyl-β-cyclodextrin at a concentration of 2 mg/mL. At 240 minutes after the initiation of blood sampling, ESN364 (1 mg/kg, n=5) or vehicle (n=5) is administered by an iv bolus injection at a dose volume of 0.5 mL/kg through the jugular cannulae, and the injected material is flushed into the animal with 5 mL of heparinized saline. Blood sampling resumes at the indicated intervals following this iv administration.

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

References
Molecular Weight

358.39

Formula

C₁₆H₁₅FN₆OS

CAS No.

1629229-37-3

SMILES

O=C(N1[[email protected]](C)C2=NN=C(C3=NC(C)=NS3)N2CC1)C4=CC=C(F)C=C4

Shipping

Room temperature in continental US; may vary elsewhere

Purity: 98.29% ee.: 98.04%

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Product Name:
Fezolinetant
Cat. No.:
HY-19632
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Fezolinetant

Cat. No.: HY-19632