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GW788388

Chemical Structure : GW788388

CAS No.: 452342-67-5

GW788388 (GW 788388;GW-788388)

Catalog No.: PC-42525Not For Human Use, Lab Use Only.

GW788388 is a potent, selective, and orally active TGF-β type I receptor (ALK5) inhibitor with IC50 of 18 nM in binding assay.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GW788388 is a potent, selective, and orally active TGF-β type I receptor (ALK5) inhibitor with IC50 of 18 nM in binding assay.
GW788388 displays excellent selectivity over a panel of kinases (AMPK, Chk1, PDK1, etc.).
GW788388 has an IC50 of 93 nM in TGF-β cellular assay.
GW788388 presents activity in a PAN-induced model of kidney fibrosis by inhibiting collagen IA1 mRNA at doses of 3 and 10 mg/kg u.i.d.

Physicochemical Properties

M.Wt 425.4824
Formula C25H23N5O2
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

DMSO: ≥ 48 mg/mL

Chemical Name/SMILES

Benzamide, 4-[4-[3-(2-pyridinyl)-1H-pyrazol-4-yl]-2-pyridinyl]-N-(tetrahydro-2H-pyran-4-yl)-

References

1. Gellibert F, et al. J Med Chem. 2006 Apr 6;49(7):2210-21.

2. Petersen M, et al. Kidney Int. 2008 Mar;73(6):705-15.

3. de Oliveira FL, et al. PLoS Negl Trop Dis. 2012;6(6):e1696.

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