SKI2496
SKI2496 is an orally active GnRH receptor antagonist (IC50: 0.25 nM for hGnRHR, 13.2 nM for monkey GnRHR, 279.2 nM for rat GnRHR) . SKI2496 blocks Ca2+ flux with an IC50 value of 0.76 nM. SKI2496 inhibits ERK1/2 phosphorylation with an IC50 value of 2.6 nM. SKI2496 inhbits serum LH concentrations, and can be used for research of sex hormone-dependent disorders[1].
Product Specifications
CAS Number
1308378-95-1
UNSPSC
12352005
Target
ERK; GnRH Receptor
Type
Reference compound
Related Pathways
GPCR/G Protein; MAPK/ERK Pathway; Stem Cell/Wnt
Field of Research
Endocrinology
Assay Protocol
https://www.medchemexpress.com/ski2496.html
Smiles
O=C(O)CCCN[C@H](C1=CC=CC=C1)CN(C(N(CC2=C(C(F)(F)F)C=CC=C2F)C(C)=C3N4CCN(CC5=CC=C(C(F)(F)F)O5)CC4)=O)C3=O
Molecular Formula
C35H36F7N5O5
Molecular Weight
739.68
References & Citations
[1]Kim SM, et al. Discovery of an Orally Bioavailable Gonadotropin-Releasing Hormone Receptor Antagonist. J Med Chem. 2016 Oct 13;59 (19) :9150-9172.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Frequently Asked Questions
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