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Org 214444-0

Chemical Structure : Org 214444-0

CAS No.: 914093-78-0

Org 214444-0 (Org214444-0)

Catalog No.: PC-20748Not For Human Use, Lab Use Only.

Org 214444-0 is a highly potent, selective, allosteric agonist of follicle stimulating hormone receptor (FSHR) with EC50 of 2.0/1.2 nM (human/rat FSHR) in cell-based assays.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Org 214444-0 is a highly potent, selective, allosteric agonist of follicle stimulating hormone receptor (FSHR) with EC50 of 2.0/1.2 nM (human/rat FSHR) in cell-based assays.
Org 214444-0 stimulates cAMP synthesis in cell line expressing human FSHR with EC50 of 5 nM in cAMP assays, Emax of 102%.
Org 214444-0 displays >200-fold selective over the human and rat LHR, and does not activate the human TSHR.
Org 214444-0 has also negligible antagonistic activity at the human and rat LHR and human TSHR at 1 uM.
Org 214444-0 is an allosteric agonist interacting with the transmembrane region of the FSHR.
When co-incubated with FSH, Org 214444-0 augments FSH's potency in binding (6.5-fold) and adenylyl cyclase/cAMP activation (3.5-fold) in a concentration-dependent manner.
Org 214444-0 induces FSHR internalization and is only marginally effective in stimulating phospholipase C.
Org 214444-0 stimulates cAMP and estradiol production in human granulosa cells in culture and supports the follicular phase in mature female rats.

Physicochemical Properties

M.Wt 664.56
Formula C30H32BrF2N3O5S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

CS(=O)(NC1=CC(F)=C(F)C=C1COC2=C(OCC)C=C([C@@H]3C(C#N)=C(C)NC4=C3C(C[C@@H](CCC)C4)=O)C=C2Br)=O

References

1. Chris J van Koppen, et al. Biochem Pharmacol. 2013 Apr 15;85(8):1162-70.

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