SKLB023 (SKLB-023)

Chemical Structure : SKLB023

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货号: PC-27622Not For Human Use, Lab Use Only.

SKLB023 is a potent small-molecule inhibitor of inducible nitric oxide synthase (iNOS) with IC50 of 8.66 uM, exhibits excellent anti-inflammatory activity in arthritis and antifibrotic effects in renal interstitial fibrosis.

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生物&药学活性

SKLB023 is a potent small-molecule inhibitor of inducible nitric oxide synthase (iNOS) with IC50 of 8.66 uM, exhibits excellent anti-inflammatory activity in arthritis and antifibrotic effects in renal interstitial fibrosis.
SKLB023 inhibits iNOS-mediated NO, and cyclooxygenase (COX)-2-derived PGE(2) production (IC(50) = 4.16 and 23.55 μM, respectively) on lipopolysaccharide (LPS)-induced RAW 264.7 cells.
SKLB023 inhibits the TGF-β1-induced activation of hepatic stellate cells (HSCs) LX-2 with IC50 of 36.06 and 19.48 μM after 24 and 48 h, respectively.
SKLB023 inhibits TGF-β1-induced Smad2/3 phosphorylation in vitro.
SKLB023 (50 mg/kg, oral administration) possessed protective properties in both carrageenan-induced paw edema and adjuvant-induced arthritis rat models.
SKLB023 blocks joint inflammation and cartilage destruction in arthritis models via suppression of nuclear factor-kappa B activation in macrophage.
SKLB023 hinders renal interstitial fibrosis in obstructive nephropathy by interfering TGF-beta1/Smad3 signaling.

物理化学性质&存储条件

分子量	388.82
分子式	C18H13ClN2O4S
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	(Z)-N-(3-Chlorophenyl)-2-(4-((2,4-dioxothiazolidin-5-ylidene) methyl) phenoxy) acet-amide

参考文献

1. Ma L, et al. J Med Chem 54: 2060–8.

2. Xie C, et al. PLoS One. 2013;8(2):e56349.

3. Zhang J, et al. RSC Adv. 2018 Sep 3;8(54):30919-30924.

4. Yu J, et al. RSC Adv. 2018 Sep 27;8(58):33338-33346.

SKLB023 (SKLB-023)

生物&药学活性

物理化学性质&存储条件

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SKLB023 (SKLB-023)

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