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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Lactate Dehydrogenase (LDH)-CHK-336
CHK-336

Chemical Structure : CHK-336

CAS No.: 2743436-86-2

CHK-336 (CHK336)

货号: PC-24437Not For Human Use, Lab Use Only.

CHK-336 is a potent and selective, orally active, liver-targeted inhibitor of lactate dehydrogenase (LDH) with IC50 of 0.4 nM in human enzyme assays, and IC50 of 80-131 nM in cryopreserved hepatocyte assays across species.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

CHK-336 is a potent and selective, orally active, liver-targeted inhibitor of lactate dehydrogenase (LDH) with IC50 of 0.4 nM in human enzyme assays, and IC50 of 80-131 nM in cryopreserved hepatocyte assays across species.
CHK-336 demonstrated a favourable liver-distribution profile in mice, rats, and monkeys.
CHK-336 inhibited conversion of 13C2-glycolate to 13C2-oxalate in a dose-dependent manner in rat pharmacodynamic models.
CHK-336 produced robust and dose-dependent reductions in urinary oxalate to the normal range in primary hyperoxaluria 1 (PH1) mouse model, also induced a significant reduction in urinary oxalate in a PH2 mouse model.

物理化学性质&存储条件

分子量 530.56
分子式 C24H20F2N4O4S2
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

10 mM in DMSO

Chemical Name/SMILES

4-Thiazolecarboxylic acid, 2-[4-[[4-(aminosulfonyl)-3-fluorophenyl]methyl]-5-(cyclopropylmethyl)-3-(4-fluorophenyl)-1H-pyrazol-1-yl]-

参考文献

1. Cox JH, et al. J Am Soc Nephrol. 2025 Apr 7. doi: 10.1681/ASN.0000000690.

2. J. COX, et al.Kidney International Reports. Volume 6, Issue 4, Supplement, April 2021, Page S192

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