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RXFP2 agonist 6641

Chemical Structure : RXFP2 agonist 6641

CAS No.: 2971704-85-3

RXFP2 agonist 6641 (Compound 6641)

Catalog No.: PC-49427Not For Human Use, Lab Use Only.

RXFP2 agonist 6641 is a highly potent, selective and full allosteric agonist of relaxin/insulin-like family peptide receptor 2 (RXFP2) with EC50 of 0.38 uM, Emax=107% (hFXRP2).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

RXFP2 agonist 6641 is a highly potent, selective and full allosteric agonist of relaxin/insulin-like family peptide receptor 2 (RXFP2) with EC50 of 0.38 uM, Emax=107% (hFXRP2).
Compound 6641 is also activate the mouse RXFP2 receptor, does not activate either human or mouse RXFP1 receptors and RXFP3 or RXFP4 receptors.
Compound 6641 is an allosteric agonist of RXFP2 that requires the RXFP2 transmembrane domain for activity.
Compound 6641 (3-5 uM) induces gubernacular invagination in mouse embryos, induces osteoblast mineralization in human osteoblasts in vitro, specifically activates the mouse RXFP2 receptor in vivo.
Compound 6641 treatment (10 mg/kg, PO) promotes bone formation in vivo.

Physicochemical Properties

M.Wt 787.377
Formula C29H19F9IN3O5
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

(S)-8-(3,5-bis(trifluoromethyl)phenyl)-2-(2-(2-iodo-4-(trifluoromethoxy)phenoxy)acetyl)-1,3,4,12a-tetrahydrobenzo[e]pyrazino[1,2-a][1,4]diazepine-6,12(2H,11H)-dione

References

1. Esteban-Lopez M, et al. Commun Biol. 2022 Nov 4;5(1):1183.

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