1. Protein Tyrosine Kinase/RTK Apoptosis Immunology/Inflammation
  2. VEGFR TNF Receptor Interleukin Related
  3. Conbercept

Conbercept  (Synonyms: 康柏西普单抗; KH902)

目录号: HY-P99830 纯度: 98.42%
COA 技术支持

Conbercept (KH902) 是一种重组融合蛋白,由 VEGFR-1 和 VEGFR-2 区域与人 IgG1 Fc 融合而成。Conbercept 是一种 VEGF 的抑制剂,其 IC50 为 8.8 pM。Conbercept 是一种可溶性受体诱饵,可阻断 VEGF-A (Kd = 0.5 pM)、VEGF-B (Kd = 8 pM)、VEGF-CPlGF (Kd = 0.5 pM) 的所有亚型。Conbercept 具有抗炎作用,可降低 VEGFTNF-αIL-6 的水平,并减少炎症细胞的浸润。Conbercept 在多项肿瘤学研究中减缓了肿瘤的生长。Conbercept 可用于息肉状脉络膜血管病变 (PCV)、糖尿病性黄斑水肿 (DME) 和病理性近视性脉络膜新生血管 (pmCNV) 等多种眼部疾病。

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CAS No. : 1227158-72-6

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1 mg ¥6000
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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Conbercept (KH902) is a recombinant fusion protein composed of VEGFR-1 (second domain) and VEGFR-2 (third and fourth domains) regions fused to human IgG1 Fc. Conbercept is a VEGF inhibitor (IC50 = 8.8 pM) and is a soluble receptor decoy that blocks all isoforms of VEGF-A (Kd = 0.5 pM), VEGF-B (Kd = 8 pM), VEGF-C, and PlGF (Kd = 5 pM). Conbercept has anti-inflammatory effects, can lower the levels of VEGF, TNF-α and IL-6, and reduce the infiltration of inflammatory cells. Conbercept decreases tumor growth in several oncology studies. Conbercept can be used for various eye diseases such as polypoidal choroidal vasculopathy (PCV), diabetic macular edema (DME) and pathologic myopia choroidal neovascularization (pmCNV)[1][2][3][4][5].

IC50 & Target[3]

VEGFR1

 

VEGFR2

 

IL-6

 

体外研究
(In Vitro)

Conbercept (0-586.9 pM, 4 天) 对 VEGF 诱导的 HUVEC 增殖具有抑制作用,EC50 值为 28 pM[3][5]
Conbercept 抑制 VEGF 诱导的 HUVEC 迁移和小管形成,并抑制高糖诱导的人视网膜内皮细胞迁移和出芽[3]

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

体内研究
(In Vivo)

Conbercept (10 mg/kg,静脉注射,隔日一次,连续 2 周) 显著减少 Ⅱ 型 Collagen (HY-NP010) 诱导的大鼠类风湿性关节炎 (CIA) 模型中的爪水肿体积和关节炎指数[1]
Conbercept (10-50 mg/kg,静脉注射,单次给药) 显著抑制二甲苯诱导的小鼠耳水肿[1]
Conbercept (0.64 mg,40 μL,玻璃体内注射,每周 4 次或每 2 周 2 次,连续 2 周) 在兔体内 81 天内对血管内皮生长因子 (VEGF) 具有抑制作用[3]
Conbercept (0.5 mg,玻璃体内注射,单次给药) 可有效预防实验性脉络膜新生血管 (CNV) 的形成,并且用于治疗猴模型中已存在的 CNV,且无毒性证据[3][5]
Conbercept 可抑制人肝细胞癌 (HepG2)、乳腺癌 (MCF-7)、胃癌 (A549) 和结直肠癌 (LoVo) 肿瘤异种移植模型中的肿瘤生长[3]

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

Animal Model: CIA model established in male Wistar rats (200 g, 4-6 weeks)[1]
Dosage: 10 mg/kg
Administration: Intravenous injection (i.v.), once every other day for 2 weeks
Result: Significantly reduced paw edema volume and significantly reduced ankle joint swelling in CIA rats.
Significantly reduced Arthritis Index (AI) scores.
Reduced serum VEGF levels, TNF-α, and IL-6 in rats.
Animal Model: Xylene-induced ear edema model established in male Kunming mice (20-25 g)[1]
Dosage: 10, 25 and 50 mg/kg
Administration: Intravenous injection (i.v.), single dose
Result: Significantly inhibited ear edema in the medium and high dose groups.
Animal Model: Experimental choroidal neovascularization (CNV) model established in rhesus monkeys[5]
Dosage: 0.64 mg, 40 μL
Administration: Intravitreally injection, 4 times a week or 2 times every 2 weeks for 2 weeks
Result: Significantly reduced the incidence of CNV and had a significant therapeutic effect on established CNV.
No significant difference in the effects between weekly and biweekly administration.
Clinical Trial
应用

ELISA, FACS, Functional assay

偶联物

Unconjugated

复溶方法

The product can be reconstituted/diluted with sterile PBS or saline.

分子量

117.45 kDa

CAS 号
性状

液体

颜色

Colorless to light yellow

中文名称

康柏西普单抗

运输条件

Shipping with dry ice.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

Format
  • [FLT1 (fms-related tyrosine kinase 1, vascular endothelial growth factor receptor 1, VEGFR-1, VEGFR, FLT, FRT, vascular permeability factor receptor)-KDR (kinase insert domain receptor, vascular endothelial growth factor receptor 2, VEGFR2, VEGF-R2, FLK1, CD309)]2-IGHG1 Fc (Fragment constant)
Biological Activity
  • Immobilized VEGF165 Protein, Human can bind Conbercept. The EC50 for this effect is 4.31 ng/mL.
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.

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产品名称:
Conbercept
目录号:
HY-P99830
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