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

Fezolinetant  (Synonyms: ESN-364)

Cat. No.: HY-19632 Purity: 98.64%
COA 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
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 429 In-stock
Solution
10 mM * 1 mL in DMSO USD 429 In-stock
Solid
1 mg USD 120 In-stock
5 mg USD 390 In-stock
10 mg USD 570 In-stock
25 mg USD 900 In-stock
50 mg USD 1400 In-stock
100 mg USD 2200 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • 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.

IC50 & Target

NK3

 

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].

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

Clinical Trial
Molecular Weight

358.39

Formula

C16H15FN6OS

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(N1[C@H](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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (55.81 mM; Need ultrasonic)

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 mg/mL (5.58 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2 mg/mL (5.58 mM); Clear solution

  • 3.

    Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

    Solubility: 1 mg/mL (2.79 mM); Suspended solution; Need ultrasonic

  • 4.

    Add each solvent one by one:  1% DMSO    99% Saline

    Solubility: ≥ 0.2 mg/mL (0.56 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 98.64%

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
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Fezolinetant 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.

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The dilution calculator equation

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This equation is commonly abbreviated as: C1V1 = C2V2

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