SIN 14
SIN 14, a derivative of Sinomenine (HY-15122), is an orally active HO-1 activator (KD = 17.2 μM). SIN 14 binds to the catalytic core domain of HO-1 and induces HO-1 activation in catalysis. SIN 14 significantly increases HO-1 stability. SIN 14 has anti-inflammatory effects and inhibits M1 macrophage polarization while promoting M2 polarization in LPS (Lipopolysaccharides)(HY-D1056)-induced RAW264.7 cells. SIN 14 inhibits inflammatory mediator production (eg: NO, IL-6, IL-1β and CCL2, inhibits production of ROS and down-regulates the expression of COX-2 and iNOS. SIN 14 can inhibit RA-related inflammatory edema in collagen-induced arthritis (ClA) mice.
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- CAS 番号: 3064262-80-9
- 分子式: C19H18ClNO4
- 分子量:359.80
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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HO-1 17.2 μM (Kd) |
iNOS |
COX-2 |
IL-6 |
IL-1β |
SIN 14 (2.5-10 μM, 24 h) can inhibit NO release in LPS-induced RAW 264.7 (IC50 = 4.97 μM), BMDM (IC50 = 3.88 μM), and BV-2 cells (IC50 = 3.88 μM)[1].
SIN 14 (2.5-10 μM, 24 h) significantly suppresses the release of inflammatory factors, including NO, IL-6, IL-1β, and CCL2, and down-regulates the expression of COX-2 and iNOS upon LPS-induced RAW 264.7 cells[1].
SIN 14 (50 μM) inhibits inflammatory cells migration and aggregation induced by CuSO4 in Tg (zlyz: EGFP) transgenic zebrafish line[1].
SIN 14 (10 μM, 24 h) inhibits M1 macrophage polarization while promoting M2 polarization in LPS-induced RAW264.7 cells[1].
SIN 14 (10 μM, 4 h or 20 min) significantly increases HO-1 stability (4 h) and enhances HO-1 resistance to pronase-induced proteolysis (20 min)[1].
SIN 14 (2.5-10 μM, 24 h) can inhibit NO production and TNF-α release, and these effects were reduced in HO-1 siRNA-transfected cells[1].
SIN 14 (10 μM, 24 h) inhibits ROS levels in LPS-induced RAW 264.7 cells by activating HO-1 (detected with the DCFH-DA probe (HY-D0940))[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LPS induced-RAW 264.7 cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Significantly inhibited CXCL10 release and enhanced the expression of IL-10, inhibited M1 macrophage polarization.
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Cell Line:LPS induced-RAW 264.7 cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Enhanced the expression of CD206, Arg-1, promoted M2 polarization
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male DBA/1 mice, 7-8 weeks old, weighing 18-20 g, were injected with bovine type II collagen and Complete Freund's Adjuvant (CFA)(HY-153808). 21 days later, they were boosted with bovine type II collagen and Incomplete Freund's Adjuvant (IFA)(HY-153808A) for 16 days of induction[1].
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Dosage:10 mg/kg, 50 mg/kg
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Administration:p.o., once daily for 36 days
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Result:Alleviated joint swelling in both the forelimbs and hindlimbs.
Showed significant improvements in BV/TV, BMD and Tb.Th, showed notable reduction in Tb.Sp.
Decreased cartilage and bone damage as well as reduced pannus formation.
Effectively curbed the abnormal proliferation of synovial cells and alleviated damage to both cartilage and bone.
The mean paw area was markedly restored compared to the model mice.
Significantly decreased the number of TRAP-positive cells in the ankle joints compared to the CIA group, indicating the inhibitory effect on RA-related osteoclast differentiation.
Decreased 8-OHdG expression in the joint tissues.
化学情報
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CAS 番号 3064262-80-9
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分子量 359.80
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分子式 C19H18ClNO4
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SMILES
O=C1OC2=C(C3=CC=C2OC)[C@]([C@@]4([H])[C@@H]5C3)(CCN5C)C1=C(Cl)C(C4)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)