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
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M.Wt
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426.86
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Formula
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C20H19ClN6O3
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. Terrett JA, et al. J Med Chem. 2024 Mar 3. doi: 10.1021/acs.jmedchem.3c02121.
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