GFB-8438 | Selective TRPC5 inhibitor

CAS:
 2304549-73-1
Catalog Number:
 10-4270

Available Options

Size:PriceQuantity 
5 mg$60.00
25 mg$225.00

GFB-8438 (2304549-73-1) is a potent (IC50 = 180 nM Qpatch and 280 nM whole cells) and selective inhibitor of TRPC4 and 5.1 It displayed excellent selectivity against other TRP family members as well as NaV1.5, 50 kinases and 87 other receptor targets along with good pharmacokinetic properties. GFB-8438 protected mouse podocytes from injury induced by protamine sulfate and demonstrated efficacy in a hypertensive DOCA-salt rat model suggesting potential therapeutic use for the treatment of chronic kidney disease.

References/Citations:

  1. Yu et al. (2019), Discovery of a Potent and Selective TRPC5 Inhibitor, Efficacious in a Focal Segmental Glomerulosclerosis Model; ACS Med. Chem. Lett. 10 1579
CAS:
2304549-73-1
Catalog Number:
10-4270
Activity:
Potent and selective TRPC5 inhibitor
Chemical Names:
4-Chloro-5-(3-oxo-4-[[2-(trifluoromethyl)phenyl]methyl]piperazin-1-yl)-2,3-dihydropyridazin-3-one
Molecular Weight:
386.76
Molecular Formula:

C16H14ClF3N4O2

Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
Off-white solid
Purity:

>98% by HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee