MedKoo Cat#: 555685 | Name: GFB-8438

Description:

WARNING: This product is for research use only, not for human or veterinary use.

GFB-8438 is a potent TRPC5 inhibitor (IC50 = 150 nM). The inhibition of TRPC5 may provide a novel, effective, and safe approach for the treatment of FSGS and related proteinuric kidney diseases.

Chemical Structure

GFB-8438
GFB-8438
CAS#2304549-73-1

Theoretical Analysis

MedKoo Cat#: 555685

Name: GFB-8438

CAS#: 2304549-73-1

Chemical Formula: C16H14ClF3N4O2

Exact Mass: 386.0757

Molecular Weight: 386.76

Elemental Analysis: C, 49.69; H, 3.65; Cl, 9.17; F, 14.74; N, 14.49; O, 8.27

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
Synonym
GFB-8438; GFB 8438; GFB8438;
IUPAC/Chemical Name
4-chloro-5-(3-oxo-4-(2-(trifluoromethyl)benzyl)piperazin-1-yl)pyridazin-3(2H)-one
InChi Key
MITRKIWBJVJRAM-UHFFFAOYSA-N
InChi Code
InChI=1S/C16H14ClF3N4O2/c17-14-12(7-21-22-15(14)26)23-5-6-24(13(25)9-23)8-10-3-1-2-4-11(10)16(18,19)20/h1-4,7H,5-6,8-9H2,(H,22,26)
SMILES Code
O=C1CN(C2=C(Cl)C(NN=C2)=O)CCN1CC3=C(C(F)(F)F)C=CC=C3
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
The nonselective Ca2+-permeable transient receptor potential (TRP) channels play important roles in diverse cellular processes, including actin remodeling and cell migration. TRP channel subfamily C, member 5 (TRPC5) helps regulate a tight balance of cytoskeletal dynamics in podocytes and is suggested to be involved in the pathogenesis of proteinuric kidney diseases, such as focal segmental glomerulosclerosis (FSGS). As such, protection of podocytes by inhibition of TRPC5 mediated Ca2+ signaling may provide a novel therapeutic approach for the treatment of proteinuric kidney diseases.

Preparing Stock Solutions

The following data is based on the product molecular weight 386.76 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Discovery of a Potent and Selective TRPC5 Inhibitor, Efficacious in a Focal Segmental Glomerulosclerosis Model Maolin Yu*Mark W. Ledeboer*Matthew DanielsGoran MalojcicThomas T. TibbittsMarie Coeffet-Le GalXin-Ru Pan-ZhouAmy Westerling-BuiMaria BeconiJohn F. ReillyPeter MundelJean-Christophe Harmange ACS Medicinal Chemistry Letters, Articles ASAP (As Soon As Publishable)Subscribed Access Publication Date (Web):October 22, 2019