Cart
sales@molnova.com
Fezolinetant
CAS No. 1629229-37-3
Fezolinetant( ESN-364 | ESN 364 )
Catalog No. M12438 CAS No. 1629229-37-3
A potent, selective, orally active neurokinin-3 receptor (NK3R) antagonist with pIC50/pKi of 7.7/7.6.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 138 | Get Quote |
|
| 5MG | 288 | Get Quote |
|
| 10MG | 419 | Get Quote |
|
| 25MG | 689 | Get Quote |
|
| 50MG | 963 | Get Quote |
|
| 100MG | 1305 | Get Quote |
|
| 200MG | Get Quote | Get Quote |
|
| 500MG | Get Quote | Get Quote |
|
| 1G | Get Quote | Get Quote |
|
Biological Information
-
Product NameFezolinetant
-
NoteResearch use only, not for human use.
-
Brief DescriptionA potent, selective, orally active neurokinin-3 receptor (NK3R) antagonist with pIC50/pKi of 7.7/7.6.
-
DescriptionA potent, selective, orally active neurokinin-3 receptor (NK3R) antagonist with pIC50/pKi of 7.7/7.6; exhibits high activity in LH inhibition, shows >2.5-log selectivity against NK1R and NK2R subtypes, proves >300-fold selective against related HPG axis receptors (KOR, GnRH, GnIH-R, GPR54).Other Indication Phase 2 Clinical(In Vitro):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.
-
In Vitro——
-
In Vivo——
-
SynonymsESN-364 | ESN 364
-
PathwayGPCR/G Protein
-
TargetNeurokinin Receptor
-
RecptorNeurokinin Receptor
-
Research AreaOther Indications
-
IndicationOther Disease
Chemical Information
-
CAS Number1629229-37-3
-
Formula Weight358.3954
-
Molecular FormulaC16H15FN6OS
-
Purity>98% (HPLC)
-
SolubilityDMSO : ≥ 50 mg/mL 139.51 mM
-
SMILESO=C(C1=CC=C(F)C=C1)N2[C@H](C)C3=NN=C(C4=NC(C)=NS4)N3CC2
-
Chemical Name[(8R)-5,6-Dihydro-8-methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)-1,2,4-triazolo[4,3-a]pyrazin-7(8H)-yl](4-fluorophenyl)methanone
Shipping & Storage Information
-
Storage(-20℃)
-
ShippingWith Ice Pack
-
Stability≥ 2 years
Reference
-
Eledoisin
Eledoisin is a specific agonist of NK2 and NK3 receptors.Eledoisin is an undecapeptide of mollusk origin, belonging to the tachykinin family of neuropeptides.Eledoisin increases the value recorded under basal conditions by 24.5±3.7%; this stimulation is significantly (P<0.01) lowered to 13.1±1.9% by the simultaneous presence of CP99994.
-
Neurokinin A(4-10)
Neurokinin A (4-10) is a tachykinin NK2 receptor agonist. A structure-activity study of the neurokinin A (NKA) fragment NKA(4-10) was performed to investigate the importance of amino acid residues for receptor efficacy, potency and affinity at the NK2 receptor in human colon circular muscle.
-
Elinzanetant
Elinzanetant is a dual antagonist of neurokinin (NK) receptors 1 and 3 and modulates reproductive hormone secretion.
