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Libvatrep

Chemical Structure : Libvatrep

CAS No.: 871814-52-7

Libvatrep (SAF312)

Catalog No.: PC-38676Not For Human Use, Lab Use Only.

Libvatrep (SAF312) is a potent, selective non-competitive inhibitor/antagonist of the transient receptor potential cation channel subfamily V member 1 (TRPV1), shows potential for treatment of ocular surface pain.

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Biological Activity

Libvatrep (SAF312) is a potent, selective non-competitive inhibitor/antagonist of the transient receptor potential cation channel subfamily V member 1 (TRPV1), shows potential for treatment of ocular surface pain.
SAF312 is >150-fold selective for TRPV1 when tested against a panel of 18 TRP channels.
SAF312 inhibited capsaicin, low pH 2-(n-morpholino)ethanesulfonic acid (MES, pH 5.5), anandamide (AEA), and N-arachidonoyl dopamine (NADA) stimulated human TRPV1 with IC50 values of 12, 16, 7.3 and 36 nM, respectively in a selective, non-competitive, and reversible manner.

Physicochemical Properties

M.Wt 305.337
Formula C18H15N3O2
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

4-(7-hydroxy-2-isopropyl-4-oxoquinazolin-3(4H)-yl)benzonitrile

References

1. Quint Medley, et al. ARVO Annual Meeting Abstract, June 2021. In-vitro and In-vivo pharmacology of SAF312 as a TRPV1 inhibitor for ocular surface pain.

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