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Merck
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Key Documents

SML3629

Sigma-Aldrich

HS-276

≥98% (HPLC)

同義詞:

HS 276, HS276, N1-[6-(1-Piperidinylmethyl)-1-propyl-1H-benzimidazol-2-yl]-1,3-benzenedicarboxamide

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About This Item

經驗公式(希爾表示法):
C24H29N5O2
CAS號碼:
分子量::
419.52
分類程式碼代碼:
12352200
NACRES:
NA.77

品質等級

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 2 mg/mL, clear (Warmed)

儲存溫度

2-8°C

SMILES 字串

O=C(C1=CC=CC(C(NC2=NC3=C(N2CCC)C=C(CN4CCCCC4)C=C3)=O)=C1)N

生化/生理作用

HS-276 is an orally active, potent and selective TGF-β-activated kinase-1 (TAK-1; TAK1) inhibitor (Ki = 2.5 nM; IC50 = 8.25 nM) that significantly reduced cytokines production in THP-1 human macrophages upon LPS/IFNγ treatment (IC50 = 138 nM/TNF, 201 nM/IL-6, and 234 nM/IL-1β). HS-276 effectively attenuates arthritic-like symptoms in the CIA mouse rheumatoid arthritis (RA) model (10-30 mg/kg/d p.o. or 25 mg/kg/d i.p.).

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


分析證明 (COA)

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Scott Scarneo et al.
ACS chemical biology, 17(3), 536-544 (2022-03-03)
Selective targeting of TNF in inflammatory diseases such as rheumatoid arthritis (RA) has provided great therapeutic benefit to many patients with chronic RA. Although these therapies show initially high response rates, their therapeutic benefit is limited over the lifetime of

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