SB 525334

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SB 525334 是一种有效的选择性 TGF-β1 受体 (ALK5) 抑制剂，IC50 为 14,5 nM。

SB 525334 is a potent and selective inhibitor of TGF-β1 receptor (ALK5) inhibitor with IC50 of 14,5 nM, 4-fold less potent against ALK4 and inactive for ALK2, ALK3, and ALK6 (IC50>10 uM); blocks TGFβ1-induced phosphorylation and nuclear translocation of Smad2/3 in renal proximal tubule cells and inhibits TGFβ1-induced increases in PAI-1 and procollagen α1 mRNA expression in A498 renal epithelial carcinoma cells at 1 uM; significantly inhibits PAN-induced proteinuria in rat model of nephritis-induced renal fibrosis.

SB525334 (1 μM; for 15 minutes before stimulating with 0.625 ng/ml of TGF-β1, assesses after 6 days) inhibits TGF-β1-mediated proliferation of familial idiopathic pulmonary arterial hypertension (iPAH) pulmonary artery smooth muscle cells (PASMCs) at an IC50 of 295 nM . Cell Proliferation AssayCell Line:PASMC cells Concentration:1 μM Incubation Time:Pre-incubated for 15 minutes (before stimulating with 0.625 ng/ml of TGF-β1), assessed after 6 days Result:Inhibited TGF-β1-mediated proliferation of familial iPAH PASMCs at an IC50 of 295 nM.

SB525334 (3-30 mg/kg; p.o.; daily from days 17 to 35) significantly reverses pulmonary arterial pressure in a rat model of pulmonary arterial hypertension (PAH). Animal Model:Adult male Sprague-Dawley rats (MCT rat model of pulmonary hypertension)Dosage:3, 30 mg/kg Administration:Oral administration; daily from days 17 to 35 Result:Reduced the proportion of fully muscularized vessels to 28% at 3 mg/kg and returned fully muscularized vessel distribution beyond that seen at day 17 and approaching the phenotype observed in saline-exposed controls at 30 mg/kg.

SB-525334 | SB525334

TGF-beta/Smad

TGFBR

TGFβR1(ALK5)|ALK5|ALK4

Cancer

——

356559-20-1

343.4249

C21H21N5

>98% (HPLC)

DMSO: ≥ 46 mg/mL

CC1=CC=CC(C2=C(C3=CC=C4N=CC=NC4=C3)N=C(C(C)(C)C)N2)=N1

Quinoxaline, 6-[2-(1,1-dimethylethyl)-5-(6-methyl-2-pyridinyl)-1H-imidazol-4-yl]-

(-20℃)

With Ice Pack

≥ 2 years