1. Immunology/Inflammation
  2. Complement System
  3. SAR-443809

SAR-443809 是靶向补体因子 Bb (factor Bb) 的选择性补体旁路 (complement system) 抑制剂,也是单克隆抗体。SAR-443809 通过选择性结合活化形式因子 Bb 阻断 C3 与因子 B 的裂解,对人 factor Bb 的 KD 为 7.3 nM。SAR-443809 抑制补体旁路途径扩增环与 C3 活化,减少 C3b 沉积,阻断血管内与血管外溶血相关通路激活。SAR-443809 可用于补体旁路途径异常介导的血液与肾脏病症的研究。

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SAR-443809

SAR-443809 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SAR-443809 is a selective alternative complement system inhibitor and monoclonal antibody targeting complement factor Bb. SAR-443809 blocks the cleavage of C3 and factor B by selectively binding to the activated form of factor Bb, with a KD of 7.3 nM for human factor Bb. SAR-443809 inhibits the amplification loop of the alternative complement pathway and C3 activation, reduces C3b deposition, and blocks the activation of pathways associated with intravascular and extravascular hemolysis. SAR-443809 can be used for the research of hematological and renal disorders mediated by abnormal alternative complement pathway[1].

反应种属

Human

体外研究
(In Vitro)

SAR-443809 (Human FB: 6-500 nM; human FBb: 0.4-30 nM; SAR443809 Fab: 3.7-300 nM; 25°C during assay) 与人 Bb 因子 (KD = 7.3 nM) 和食蟹猴 Bb 因子 (KD = 61 nM) 高亲和力结合,且其 Fab 片段与活化的补体旁路途径 C3 转化酶 (C3bBb) 高亲和力结合 (KD = 0.5 nM)[1]
SAR-443809 可通过阻断 C3 和 B 因子的裂解,强效且选择性地抑制人补体旁路途径 (IC50 = 8.47 μg/mL) 与食蟹猴补体旁路途径 (IC50 = 15.72 μg/mL),且不会抑制经典途径或凝集素途径[1]
SAR-443809 (37°C 作用 50 分钟) 可抑制旁路途径介导的兔红细胞溶血,其 IC50 为 28.45 μg/mL[1]
SAR-443809 (37°C 处理 50 分钟) 可抑制旁路途径介导的 C3b 在兔红细胞上的沉积,其表观 IC50 为 33.8 μg/mL[1]
SAR-443809 (100 μg/mL; 30 minutes at 37°C) 可抑制 H 因子缺失的人血清中不受调控的液相 C3 裂解,通过补体旁路途径的自发激活阻止 C3 的消耗[1]
SAR-443809 可选择性结合人因子 Bb (EC50 = 30.9 ng/mL),且对其他受试血浆丝氨酸蛋白酶无特异性结合,其中包括大多数补体系统酶[1]

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

体内研究
(In Vivo)

SAR-443809 (15 mg/kg;静脉注射/皮下注射;单次给药) 在雌性食蟹猴中可实现补体旁路途径活性的持续性 (≥ 288 hours) 90% 抑制[1]

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

Animal Model: Cynomolgus monkeys (female)[1]
Dosage: 15 mg/kg (i.v.); 15 mg/kg (s.c.)
Administration: i.v.; single dose
s.c.; single dose
Result: Achieved 90% inhibition of alternative pathway complement activity at 24 hours post-dose, sustained for at least 288 hours (i.v.).
Reached 90% inhibition of alternative pathway complement activity between 24-48 hours post-dose, sustained for at least 288 hours (s.c.).
Showed no classical pathway inhibition.
基因 ID

629  [NCBI]

Accession

AAH04143.1

靶点

Complement Factor B/CFB

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.

组分

Please refer to the lot-specific COA for specific buffer information.

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:
SAR-443809
目录号:
HY-P992456
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