Vadadustat (PG-1016548, AKB-6548) | HIF-PHD inhibitor

Chemical Structure : Vadadustat

CAS No.: 1000025-07-9

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Vadadustat (PG-1016548, PG1016548, AKB-6548)

货号: PC-42346Not For Human Use, Lab Use Only.

Vadadustat (PG-1016548, AKB-6548) is a novel, potent, orally active HIF prolyl-4-hydroxylase (HIF-PHD) inhibitor with pKi of for PHD1, PHD2, and PHD3, respecitvely.

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5 mg	￥980	In stock
10 mg	￥1480	In stock
25 mg	￥2580	In stock
50 mg	￥4280	In stock
100 mg		Get quote

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生物&药学活性

Vadadustat (PG-1016548, AKB-6548) is a novel, potent, orally active HIF prolyl-4-hydroxylase (HIF-PHD) inhibitor with pKi of for PHD1, PHD2, and PHD3, respecitvely.
Vadadustat is competitive with 2-OG and not strongly affected by local iron levels.
In Hep 3B cells, Vadadustat treatment increased HIF-1α with a half-maximal EC50 of 44 μM and 67 μM over 6 and 24 hours, respectively, and increased HIF-2α with an EC50 of 51 μM and 54 μM over 6 and 24 hours, respectively.
In the HUVEC line, vadadustat treatment increased HIF-1α with an EC50 of 25 μM and 71 μM over 6 and 24 hours, respectively, and increased HIF-2α with an EC50 of 21 μM and 38 μM over 6 and 24 hours, respectively.
At concentrations above 3 μM, vadadustat significantly increased EPO secretion by Hep 3B cells, reaching greater levels of EPO release at 30 μM, but not VEGF secretion.
Vadadustat is in development for the treatment of anemia in both nondialysis-dependent (NDD) and dialysis-dependent CKD.
Vadadustat (PG-1016548, AKB-6548) induces endogenous erythropoietin synthesis and enhances iron mobilization.

物理化学性质&存储条件

分子量	306.70114
分子式	C14H11ClN2O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	DMSO: ≥ 33 mg/mL
Chemical Name/SMILES	Glycine, N-[[5-(3-chlorophenyl)-3-hydroxy-2-pyridinyl]carbonyl]-

参考文献

1. Shalwitz R, et al. J Am Soc Nephrol. 2011;22:45A.
2. Pergola PE, et al. Kidney Int. 2016 Nov;90(5):1115-1122.
3. Martin ER, et al. Am J Nephrol. 2017;45(5):380-388.
4, Anna Zuk, et al. J Pharmacol Exp Ther. 2022 Oct;383(1):11-24.

Vadadustat (PG-1016548, PG1016548, AKB-6548)

生物&药学活性

物理化学性质&存储条件

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Vadadustat (PG-1016548, PG1016548, AKB-6548)

生物&药学活性

物理化学性质&存储条件

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