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Fezolinetant

Cat. No. M14021
Fezolinetant Structure
Synonym:

ESN-364

Size Price Availability Quantity
5mg USD 258  USD258 In stock
10mg USD 400  USD400 In stock
25mg USD 745  USD745 In stock
50mg USD 990  USD990 In stock
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Quality Control & Documentation
Biological Activity

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

Chemical Information
Molecular Weight 358.39
CAS Number 1629229-37-3
Solubility (25°C) DMSO 20 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Atsuo Tahara, et al. Effects of neurokinin 3 receptor antagonist fezolinetant on hot flash-like symptoms in ovariectomized rats

[2] Graeme L Fraser, et al. Randomized Controlled Trial of Neurokinin 3 Receptor Antagonist Fezolinetant for Treatment of Polycystic Ovary Syndrome

[3] Herman Depypere, et al. Fezolinetant in the treatment of vasomotor symptoms associated with menopause

[4] Janet S Carpenter. Fezolinetant findings can fuel future instrumentation inquiries

[5] Graeme L Fraser, et al. A phase 2b, randomized, placebo-controlled, double-blind, dose-ranging study of the neurokinin 3 receptor antagonist fezolinetant for vasomotor symptoms associated with menopause

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Keywords: Fezolinetant, ESN-364 supplier, Neurokinin Receptor, inhibitors, activators


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