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首页-小分子抑制剂&激动剂-Immunology/Inflammation-NOD-like Receptor (NLR)-GDC-2394 sodium salt
GDC-2394 sodium salt

Chemical Structure : GDC-2394 sodium salt

CAS No.: 2238822-08-5

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GDC-2394 sodium salt (GDC2394 sodium)

货号: PC-24847Not For Human Use, Lab Use Only.

GDC-2394 sodium salt (GDC2394) is a potent and selective NLRP3 inhibitor with IC50 of 5.4 nM (IL-1β inhibition in PBMCs).

规格 价格 库存 数量
2 mg ￥1580 In stock
5 mg ￥2780 In stock
10 mg ￥4580 In stock
25 mg Get quote
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GDC-2394 sodium salt (GDC2394) is a potent and selective NLRP3 inhibitor with IC50 of 5.4 nM (IL-1β inhibition in PBMCs).
GDC-2394 inhibits NLRP3-induced caspase-1 activity with IC50 of 51 nM in in THP1 cells, but does not inhibit NLRC4-dependent inflammasome activation.
GDC-2394 inhibits NLRP3-dependent IL-1β release from mouse bone marrow-derived macrophages (BMDMs) with IC50 of 63 nM.
GDC-2394 inhibits LPS plus nigericin-induced ASC speck formation in THP-1 cells with IC50 of 48 nM.
GDC-2394 inhibits production of IL-1β in human and mouse WB in response to LPS priming and activation by ATP, and also LPS priming and activation by MSU crystals, calcium pyrophosphate dehydrate, and cholesterol crystals in HWB and macrophages.
GDC-2394 (25 mg/kg) significantly reduces joint swelling and pain scores, comparable to that achieved by IL-1β blockade, in rodent model of gouty arthritis induced by intra-articular injection of MSU crystals.

物理化学性质&存储条件

分子量 454.50
分子式 C20H25N5NaO4S
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

(S)-N-((1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)-6-(methylamino)-6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-3-sulfonamide, sodium salt

参考文献

1. Christopher McBride, et al. J Med Chem. 2022 Oct 24. doi: 10.1021/acs.jmedchem.2c01250.

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