2. Metabolic Enzyme/Protease NF-κB Immunology/Inflammation
  3. Heme Oxygenase (HO) Reactive Oxygen Species (ROS) NO Synthase COX Interleukin Related
  4. SIN 14

SIN 14 是青藤碱 (HY-15122) 的衍生物，是一种口服有效的 HO-1 激活剂 (KD = 17.2 μM)。SIN 14 与 HO-1 的催化核心结构域结合，并在催化过程中诱导 HO-1 活化。SIN 14 显著提高 HO-1 的稳定性。SIN 14 具有抗炎作用，在 LPS (Lipopolysaccharides)(HY-D1056) 诱导的 RAW264.7 细胞中抑制 M1 巨噬细胞极化，同时促进 M2 极化。SIN 14 抑制炎症介质 (例如：NO、IL-6、IL-1β 和 CCL2) 的产生，抑制 ROS 的产生，并下调 COX-2 和 iNOS 的表达。SIN 14 可抑制胶原诱导性关节炎 (CLA) 小鼠的 RA 相关炎症水肿。

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SIN 14

SIN 14 Chemical Structure

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SIN 14 相关抗体

Top Publications Citing Use of Products

查看 Heme Oxygenase (HO) 亚型特异性产品:

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HO-1 HO-2

查看 NO Synthase 亚型特异性产品:

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nNOS iNOS eNOS

查看 COX 亚型特异性产品:

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COX COX-1 COX-2 COX-3

查看 Interleukin Related 亚型特异性产品:

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1].

IC50 & Target[1]

HO-1

17.2 μM (Kd)

iNOS

 

COX-2

 

IL-6

 

IL-1β

 

体外研究
(In Vitro)

SIN 14 (2.5-10 μM，24 小时) 可抑制 LPS 诱导的 RAW 264.7 (IC50 = 4.97 μM)、BMDM (IC50 = 3.88 μM) 和 BV-2 细胞 (IC50 = 3.88 μM) 中的 NO 释放[1]。
SIN 14 (2.5-10 μM，24 小时) 显著抑制 LPS 诱导的 RAW 264.7 细胞中 NO、IL-6、IL-1β 和 CCL2 等炎症因子的释放，并下调 COX-2 和 iNOS 的表达[1]。
SIN 14 (50 μM) 可抑制 Tg (zlyz: EGFP) 转基因斑马鱼系中 CuSO4 诱导的炎症细胞迁移和聚集[1]。
在 LPS 诱导的 RAW264.7 细胞中，SIN 14 (10 μM，24 小时) 抑制巨噬细胞 M1 极化，同时促进 M2 极化[1]。
SIN 14 (10 μM，4 小时或 20 分钟) 显著提高 HO-1 的稳定性 (4 小时)，并增强 HO-1 对蛋白酶诱导的蛋白酶解的抵抗力 (20 分钟)[1]。
SIN 14 (2.5-10 μM，24 小时) 可抑制 NO 的产生和 TNF-α 的释放，而这些作用在 HO-1 siRNA 转染的细胞中被减弱[1]。
SIN 14 (10 μM，24 小时) 通过激活 HO-1 (用 DCFH-DA 探针 (HY-D0940) 检测) 来抑制 LPS诱导的 RAW 264.7 细胞中的 ROS 水平[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

SIN 14 相关抗体:

Real Time qPCR[1]

Cell Line: LPS induced-RAW 264.7 cells
Concentration: 10 μM
Incubation Time: 24 h
Result: Significantly inhibited CXCL10 release and enhanced the expression of IL-10, inhibited M1 macrophage polarization.

Immunofluorescence[1]

Cell Line: LPS induced-RAW 264.7 cells
Concentration: 10 μM
Incubation Time: 24 h
Result: Enhanced the expression of CD206, Arg-1, promoted M2 polarization
体内研究
(In Vivo)

SIN 14 (10 mg/kg、50 mg/kg，口服，每日一次，36天) 可减轻CIA DBA/1小鼠前后肢关节肿胀，有效抑制软骨损伤进展，促进骨侵蚀修复[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].
Dosage: 10 mg/kg, 50 mg/kg
Administration: p.o., once daily for 36 days
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.
分子量

375.85

Formula

C20H22ClNO4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

SIN 14 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SIN 14SIN14SIN-14Heme Oxygenase (HO)Reactive Oxygen Species (ROS)NO SynthaseCOXInterleukin RelatedHeme OxygenaseNitric oxide synthasesNOSCyclooxygenaseILRheumatoid ArthritisHeme Oxygenase-1HO-1Collagen-induced arthritisCIAROSCOX-2iNOS Macrophage polarizationInflammationAllosteric regulationInhibitorinhibitorinhibit

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