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
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Customer Review

Based on 1 publication(s) in Google Scholar

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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
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

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    40% PEG300    5% Tween-80    45% saline

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

  • 2.

    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

  • 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

Purity: 98.29% ee.: 98.04%

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