1. NF-κB Stem Cell/Wnt MAPK/ERK Pathway Immunology/Inflammation
  2. NF-κB ERK JNK p38 MAPK Interleukin Related
  3. CLP-d2

CLP-d2 是一种多靶点抗炎剂、破骨细胞生成抑制剂及免疫调节剂,具有优于 Daptomycin (HY-B0108) 的药代动力学特征,以及良好的安全性。CLP-d2 通过降低 c-FosNFATc1 的表达水平,减少 IκBαp65ERKJNK 的磷酸化水平,抑制 NF-κBMAPK 信号通路,进而减少 IL-6TNF-αIL-1β 等促炎细胞因子的分泌,发挥抗炎活性。CLP-d2 抑制小鼠关节内破骨细胞生成,减轻骨侵蚀与关节肿胀,减少滑膜增生和炎症细胞浸润,降低血清类风湿因子 (RF) 水平。CLP-d2 可用于类风湿关节炎的相关研究。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Custom Peptide Synthesis

CLP-d2

CLP-d2 Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CLP-d2 is a multi-target anti-inflammatory agent, osteoclastogenesis inhibitor and immunomodulator with superior pharmacokinetic properties to Daptomycin (HY-B0108) and good safety profiles. CLP-d2 inhibits the NF-κB and MAPK signaling pathways by reducing the expression levels of c-Fos and NFATc1, and decreasing the phosphorylation levels of IκBα, p65, ERK and JNK, thereby reducing the secretion of pro-inflammatory cytokines such as IL-6, TNF-α and IL-1β to exert anti-inflammatory activity. CLP-d2 inhibits intra-articular osteoclastogenesis in mice, alleviates bone erosion and joint swelling, reduces synovial hyperplasia and inflammatory cell infiltration, and decreases serum rheumatoid factor (RF) levels. CLP-d2 is applicable to related research on rheumatoid arthritis[1].

IC50 & Target

p65

 

IL-6

 

IL-1β

 

I-kappaBalpha

 

体外研究
(In Vitro)

CLP-d2 (10 μg/mL;24 h) 可强效抑制 LPS 刺激的 RAW264.7 细胞中 IL-6、TNF-α 和 IL-1β 的分泌及基因转录,其中对 IL-6 的抑制作用最强[1]

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

RT-PCR[1]

Cell Line: RAW264.7 cells
Concentration: 10 μg/mL
Incubation Time: 24 h
Result: Inhibits secretion and gene transcription of IL-6, TNF-α, and IL-1β in LPS-stimulated RAW264.7 cells, with the greatest inhibition of IL-6 (93.7% reduction in gene level)
体内研究
(In Vivo)

CLP-d2 (10 mg/kg;i.v.;每 2 天 1 次;持续 40 天) 在胶原诱导性关节炎小鼠中发挥抗类风湿性关节炎作用,可使关节炎评分降低 45.9%,并显著抑制炎症通路与关节破坏[1]
CLP-d2 (10 mg/kg;i.v.;单剂量) 在 Balb/c 小鼠中表现出良好的药代动力学参数,与达托霉素相比,其 AUC0-t更大、T1/2更长[1]

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

Animal Model: DBA/1J male mice (6−7 weeks)[1]
Dosage: 10 mg/kg
Administration: i.v.; every 2 days; 40 days
Result: Increased body weight by 12% compared to the CIA group; reduced arthritis score by 45.9% compared to the CIA group; reduced serum RF levels by 46.0%, serum IL-6 levels by 54.2%, serum TNF-α levels by 25.9%, and serum IL-1β levels by 42.6% compared to the CIA group; reduced joint histopathological scores by 70.4% compared to the CIA group; reduced IL-6 IHC scores by 46.4%, IL-1β IHC scores by 59.2%, and TNF-α IHC scores by 49.3% compared to the CIA group; reduced p-IκBα IHC scores by 59.3%, p-p65 IHC scores by 58.6%, p-ERK IHC scores by 60.9%, p-JNK IHC scores by 58.6%, c-Fos IHC scores by 59.1%, and NFATc1 IHC scores by 66.6% compared to the CIA group; reduced bone erosion and paw swelling; inhibited p65 nuclear translocation and osteoclast generation in joints.
Animal Model: Balb/c mice[1]
Dosage: 10 mg/kg
Administration: i.v.; single dose
Result: Reported AUC(0-t) of 255.53 mg/L*h, T1/2 of 1.43 h, Tmax of 0.5 h, VZ of 0.08 L/kg, CLZ of 0.04 L/h/kg, and Cmax of 73.93 mg/L.
分子量

1725.76

Formula

C78H104N18O27

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
  • 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.

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称:

 

* 需求量:

* 客户姓名:

 

* Email:

* 电话:

 

* 公司或机构名称:

   留言给我们:

Bulk Inquiry

Inquiry Information

产品名称:
CLP-d2
目录号:
HY-P11617
需求量: