1. GPCR/G Protein
  2. Endothelin Receptor
  3. Rendomab B4

Rendomab B4 是一种靶向 ETB 的单克隆抗体。Rendomab B4 优先与处于活性构象状态的 ETB 结合,且对黑色素瘤细胞上的 ETB 具有选择性。Rendomab B4 可抑制 G 蛋白依赖性磷脂酶 C (PLC) 通路,阻断 ET-3 诱导的 Gαi/o 介导的腺苷酸环化酶抑制作用,且不会影响 ERK1/2 通路的激活。Rendomab B4 适用于黑色素瘤相关研究。

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Rendomab B4

Rendomab B4 Chemical Structure

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查看 Endothelin Receptor 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Rendomab B4 is a monoclonal antibody targeting ETB. Rendomab B4 preferentially binds to ETB in the active conformational state and exhibits selectivity for ETB on melanoma cells. Rendomab B4 inhibits the G protein-dependent phospholipase C (PLC) pathway, blocks ET-3-induced Gαi/o-mediated inhibition of adenylate cyclase, and does not affect the activation of the ERK1/2 pathway. Rendomab B4 is applicable to melanoma-related research[1][2].

反应种属

Human

体外研究
(In Vitro)

Rendomab B4 (0.15-100 nM; overnight-1 h) 可特异性、高亲和力地与 CHO-ETB 细胞上表达的人内皮素 B 受体结合 (表观 Kd* = 0.15 nM),且不与啮齿类内皮素 B 受体或人内皮素 A 受体发生交叉反应[1]
Rendomab B4 (10 nM; overnight) 不会与内皮素-1 或内皮素-3 竞争结合 CHO-ETB 细胞上的人内皮素 B 受体,提示二者具有不同的结合位点[1]
Rendomab B4 (1 μg/mL; 90 min) 识别人内皮素 B 受体 N 端结构域中由两段非连续序列构成的不连续构象表位,该表位涵盖第 28-38 位和第 70-77 位残基[1]
Rendomab B4 (0.14-10 nM; overnight) 可特异性结合多种黑色素瘤细胞系上表达的人内皮素 B 受体,对 UACC-257 细胞的亲和力最高 (表观 Kd = 0.14 nM),且不结合非癌细胞系 HEK293T 或 HUVEC 上的内皮素 B 受体[1]
Rendomab B4 (150 nM; 2 h 30 min) 可强效抑制 UACC-257 黑色素瘤细胞中由内皮素-1 和内皮素-3 诱导的磷脂酶 C 活化,使活性降低约 75%[1]
Rendomab B4 (150 nM; 2 h 5 min) 不会抑制 UACC-257 黑色素瘤细胞中由内皮素-1 或内皮素-3 诱导的 ERK1/2 磷酸化,表明其对内皮素 B 受体信号通路具有偏向性抑制作用[1]
Rendomab B4 (150 nM; 22 h) 可完全抑制内皮素-1 诱导的 UACC-257 黑色素瘤细胞迁移,且不影响细胞的基础迁移[1]

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

Cell Migration Assay[1]

Cell Line: UACC-257 human melanoma cells
Concentration: 150 nM (Rendomab B4, pre-incubation); 50 nM ET-1 (stimulation)
Incubation Time: 2 h (37°C, pre-incubation); 20 h (37°C, stimulation)
Result: Completely abolished ET-1-induced UACC-257 cell migration, with migration levels matching unstimulated cells.
Had no effect on baseline cell migration in the absence of ET-1.
ET-1 increased UACC-257 cell migration by 3-fold compared to unstimulated cells.
体内研究
(In Vivo)

Rendomab-B49 (嵌合型 xiRB49)(4 mg/kg; i.p.; 2 doses) 不会抑制无胸腺裸鼠中黑色素瘤异种移植物的生长,且未观察到与治疗相关的毒性[2]

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

Animal Model: athymic nude mice (female, 10 weeks old)[2]
Dosage: 4 mg/kg
Administration: i.p.; 2 doses (Day 47 and Day 80)
Result: Showed no effect on melanoma xenograft tumor progression over 136 days.
Resulted in all mice being sacrificed on Day 108 due to significant ulceration or excessively large tumor volume, matching vehicle control outcome.
Caused no behavioral signs of toxicity or weight loss.
基因 ID

1910  [NCBI]

Accession
靶点

EDNRB/Endothelin R

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.

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
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  • 稀释计算器

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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:
Rendomab B4
目录号:
HY-P991964
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