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GFB-8438 - 98%, high purity , CAS No.2304549-73-1, Channel blocker of TRPC5

  • Moligand™
  • ≥98%
Item Number
G412526
Grouped product items
SKUSizeAvailabilityPrice Qty
G412526-5mg
5mg
In stock
$117.90
G412526-10mg
10mg
In stock
$187.90
G412526-25mg
25mg
In stock
$375.90
G412526-50mg
50mg
In stock
$593.90
G412526-100mg
100mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$969.90

TRP Channel Inhibitors

View related series
TRPC5 Channel blocker

Basic Description

Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsGFB-8438 is a novel, potent, and subtype selective TRP channel subfamily C (TRPC) inhibitor that is equipotent against TRPC4 and TRPC5 with IC50 of 0.18 μM and 0.29 μM, and shows excellent selectivity against TRPC6, other TRP family members , NaV 1.5, as
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeCHANNEL BLOCKER
Mechanism of actionChannel blocker of TRPC5
Product Description

Information

GFB-8438 GFB-8438 is a novel, potent, and subtype selective TRP channel subfamily C (TRPC) inhibitor that is equipotent against TRPC4 and TRPC5 with IC50 of 0.18 μM and 0.29 μM, and shows excellent selectivity against TRPC6, other TRP family members , NaV 1.5, as well as limited activity against the hERG channel .


Targets

hERG channel ; TRPC4 (Cell-free assay); TRPC5 (Cell-free assay) ; 0.18 μM; 0.29 μM

Product Properties

ALogP1.445
HBD Count1
Rotatable Bond4

Associated Targets

STK10 Tchem Serine/threonine-protein kinase 10 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TRPM2 Tchem Transient receptor potential cation channel subfamily M member 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TRPM3 Tchem Transient receptor potential cation channel subfamily M member 3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TRPM4 Tchem Transient receptor potential cation channel subfamily M member 4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TRPV3 Tchem Transient receptor potential cation channel subfamily V member 3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TRPC3 Tchem Short transient receptor potential channel 3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TRPC4 Tchem Short transient receptor potential channel 4 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TRPC5 Tchem Short transient receptor potential channel 5 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TRPC6 Tchem Short transient receptor potential channel 6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TRPV1 Tclin Transient receptor potential cation channel subfamily V member 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TRPC7 Tchem Short transient receptor potential channel 7 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

SCN5A Tclin Sodium channel protein type 5 subunit alpha 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TRPA1 Tclin Transient receptor potential cation channel subfamily A member 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TRPV2 Tchem Transient receptor potential cation channel subfamily V member 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TRPV4 Tchem Transient receptor potential cation channel subfamily V member 4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TRPM8 Tclin Transient receptor potential cation channel subfamily M member 8 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TRPV5 Tchem Transient receptor potential cation channel subfamily V member 5 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name 5-chloro-4-[3-oxo-4-[[2-(trifluoromethyl)phenyl]methyl]piperazin-1-yl]-1H-pyridazin-6-one
INCHI 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)
InChi Key MITRKIWBJVJRAM-UHFFFAOYSA-N
Canonical SMILES C1CN(C(=O)CN1C2=C(C(=O)NN=C2)Cl)CC3=CC=CC=C3C(F)(F)F
Isomeric SMILES C1CN(C(=O)CN1C2=C(C(=O)NN=C2)Cl)CC3=CC=CC=C3C(F)(F)F
PubChem CID 138471783
Molecular Weight 386.76

Certificates

Certificate of Analysis(COA)

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To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section

5 results found

Lot NumberCertificate TypeDateItem
G2221042Certificate of AnalysisJun 11, 2022 G412526
G2221046Certificate of AnalysisJun 11, 2022 G412526
G2221047Certificate of AnalysisJun 11, 2022 G412526
G2221048Certificate of AnalysisJun 11, 2022 G412526
G2221049Certificate of AnalysisJun 11, 2022 G412526

Chemical and Physical Properties

SolubilitySolubility (25°C) In vitro DMSO: 77 mg/mL (199.08 mM); Ethanol: 4 mg/mL (10.34 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility77
DMSO(mM) Max Solubility199.089874857793
Water(mg / mL) Max Solubility<1

Safety and Hazards(GHS)

Pictogram(s) GHS07
Signal Warning
Hazard Statements

H315:Causes skin irritation

H319:Causes serious eye irritation

H335:May cause respiratory irritation

Precautionary Statements

P261:Avoid breathing dust/fume/gas/mist/vapors/spray.

P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing.

Related Documents

References

1. Yu M, Ledeboer MW, Daniels M, Malojcic G, Tibbitts TT, Coeffet-Le Gal M, Pan-Zhou XR, Westerling-Bui A, Beconi M, Reilly JF et al..  (2019)  Discovery of a Potent and Selective TRPC5 Inhibitor, Efficacious in a Focal Segmental Glomerulosclerosis Model..  ACS Med Chem Lett,  10  (11): (1579-1585).  [PMID:31749913]

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