CPHPC
(Synonyms: Ro 63-8695|GSK2315698) 目录号 : GC14828
An inhibitor of the protein-protein interaction between SAP and amyloid fibrils
Cas No.:224624-80-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
CPHPC is used with anti-SAP antibodies to eliminate amyloid deposits.
The amyloid deposits causing disease in systemic amyloidosis contain the normal plasma protein, serum amyloid P (SAP) component. SAP is the target of a novel immunotherapy approach being developed to eliminate amyloid deposits.
In vitro: Previous study found that the multi-point binding of CPHPC between pairs of pentameric SAP molecules increased the avidity of the interaction, and this was reflected in an apparent affinity constant of 10 nM. Moreover, the X-ray crystal structure of the SAP–CPHPC complex confirmed that it was a decamer composed of two pentameric SAP molecules reversibly crosslinked by five CPHPC molecules [1].
In vivo: Mice were received CPHPC at 1 mg/ml in their drinking water for the rest of the experiment. Circulating human SAP was depleted but significant amounts of SAP remained in the amyloid deposits. Five days after starting on CPHPC, one group received a single intraperitoneal injection of 50 mg of the IgG fraction of sheep anti-human SAP antiserum, containing 7 mg of anti-SAP antibody. A control group received 50 mg of unrelated sheep IgG. The third group received no treatment and thus controlled for spontaneous regression of AA amyloid. Results showed that there was dramatically less amyloid after treatment with CPHPC plus anti-SAP antibody than in the other two groups but there was no difference between CPHPC alone and no treatment [2].
Clinical trial: In a first, exploratory, open label proof of principle study, it was found that CPHPC produced sustained, >95% depletion of circulating SAP in all patients. There were no significant adverse effects of either SAP depletion or CPHPC itself. No accumulation of amyloid was demonstrable by SAP scintigraphy in any patient on the drug. In hereditary fibrinogen amyloidosis, proteinuria was reduced in four of five patients receiving CPHPC [3].
References:
[1] M. B. Pepys, J. Herbert, W. L. Hutchinson, et al. Targeted pharmacological depletion of serum amyloid P component for treatment of human amyloidosis. Nature 417, 254-259 (2002).
[2] K. Bodin, S. Ellmerich, M. C. Kahan, et al. Antibodies to human serum amyloid P component eliminate visceral amyloid deposits. Nature 468, 93-97 (2010).
[3] Gillmore JD et al. ustained pharmacological depletion of serum amyloid P
component in patients with systemic amyloidosis. Br J Haematol. 2010 Mar;148(5):760-7.
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9377 mL | 14.6886 mL | 29.3772 mL |
| 5 mM | 0.5875 mL | 2.9377 mL | 5.8754 mL |
| 10 mM | 0.2938 mL | 1.4689 mL | 2.9377 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。