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GFB-8438

Chemical Structure : GFB-8438

CAS No.: 2304549-73-1

GFB-8438 (GFB8438)

Catalog No.: PC-73245Not For Human Use, Lab Use Only.

GFB-8438 is a potent, selective TRPC5 inhibitor with IC50 of 0.18 uM (hTRPC5, Qpatch assay).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GFB-8438 is a potent, selective TRPC5 inhibitor with IC50 of 0.18 uM (hTRPC5, Qpatch assay).
GFB-8438 inhibited the whole cell current with an IC50 of 0.28 μM comparable to the IC50 in Qpatch assay.
GFB-8438 was equipotent against TRPC4 (IC50=0.29 uM) and TRPC5.
GFB-8438 showed excellent selectivity against TRPC6, other TRP family member (TRPC3/7, TRPA1, TRPV1/2/3/4/5, and TRPM2/3/4/8).
GFB-8438 protects mouse podocytes from injury induced by protamine sulfate (PS) in vitro.
GFB-8438 demonstrated robust efficacy in the hypertensive DOCA-salt rat model without affecting blood pressure.

Physicochemical Properties

M.Wt 386.76
Formula C16H14ClF3N4O2
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-chloro-5-(3-oxo-4-(2-(trifluoromethyl)benzyl)piperazin-1-yl)pyridazin-3(2H)-one

References

1. Maolin Yu, et al. ACS Med Chem Lett. 2019 Oct 22;10(11):1579-1585.

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