CPHPC (Synonyms: Ro 63-8695|GSK2315698) |
Katalog-Nr.GC14828
One-Click Copy Product Info
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CPHPC ist ein Ligand fÜr die Serum-Amyloid-P-Komponente (SAP) und soll die SAP-Bindung an Amyloidfibrillen und -knÄuel hemmen und dissoziieren.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 224624-80-0
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 224624-80-0 | SDF | |
| Überlieferungen | Ro 63-8695|GSK2315698 | ||
| Chemical Name | 1,1'-(1,6-dioxo-1,6-hexanediyl)bis-D-proline | ||
| Canonical SMILES | O=C(CCCCC(N1CCC[C@@H]1C(O)=O)=O)N2[C@@H](C(O)=O)CCC2 | ||
| Formula | C16H24N2O6 | M.Wt | 340.4 |
| Löslichkeit | ≤30mg/ml in ethanol;20mg/ml in DMSO;25mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9377 mL | 14.6886 mL | 29.3772 mL |
| 5 mM | 587.5 μL | 2.9377 mL | 5.8754 mL |
| 10 mM | 293.8 μL | 1.4689 mL | 2.9377 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)