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GDC-6599

Chemical Structure : GDC-6599

CAS No.: 2376824-99-4

GDC-6599 (GDC6599, GDC 6599)

Catalog No.: PC-21908Not For Human Use, Lab Use Only.

GDC-6599 is a potent, selective transient receptor potential ankyrin 1 (TRPA1) antagonist with IC50 of 5.3 nM (hTRPA1), exhibits TRPA1 cell potency (IC50=20 nM) in the Ca2+ influx assay in CHO cells.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

GDC-6599 is a potent, selective transient receptor potential ankyrin 1 (TRPA1) antagonist with IC50 of 5.3 nM (hTRPA1), exhibits TRPA1 cell potency (IC50=20 nM) in the Ca2+ influx assay in CHO cells.
GDC-6599 displays cross-species potency against rat, dog, monkey and guinea pigs TRPA1 with IC50 of 18, 29, 22 and 46 nM, respectively.
GDC-6599 (3 mg/kg, p.o.) significantly reduced skin blood flow induced by topical application of TRPA1 agonist AITC in PD model.
GDC-6599 blocks aldehyde oxidase (AO)-mediated metabolism and ameliorates coagulation effects in vivo.

Physicochemical Properties

M.Wt 426.86
Formula C20H19ClN6O3
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

1-((3-((3R,5R)-5-(4-Chlorophenyl)tetrahydrofuran-3-yl)-1,2,4-oxadiazol-5-yl)methyl)-2,7-dimethyl-1,7-dihydro-6H-purin-6-one

References

1. Terrett JA, et al. J Med Chem. 2024 Mar 3. doi: 10.1021/acs.jmedchem.3c02121.

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