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| Targets |
CP-447697 primarily targets the C5a receptor (C5aR, CD88), a G protein-coupled receptor that mediates the inflammatory effects of the complement component C5a. C5a is a potent chemoattractant and anaphylatoxin that recruits and activates inflammatory cells. By antagonizing the C5a receptor, CP-447697 blocks C5a-mediated signaling, reducing inflammation. It has an IC50 of 31 nM for the C5a receptor.
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| ln Vitro |
In vitro, CP-447697 is a potent C5a receptor antagonist with an IC50 of 31 nM. Its activity is characterized by its ability to block C5a receptor-mediated signaling in cell-based assays. The compound's lipophilic nature may influence its pharmacokinetic properties. It can be used for the research of inflammation. Specific functional assay data are not detailed in the provided search results.
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| ln Vivo |
Specific in vivo activity data for CP-447697 is not detailed in the provided search results. As a C5a receptor antagonist, it is being investigated for its potential in treating inflammatory diseases where C5a plays a pathogenic role. By blocking C5a-mediated inflammation, it may reduce tissue damage and disease severity. Further studies are needed to characterize its in vivo efficacy and safety.
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| Enzyme Assay |
The in vitro activity of CP-447697 is assessed using radioligand binding assays and functional assays. For receptor binding, membrane preparations from cells expressing the C5a receptor are incubated with a radiolabeled C5a receptor ligand in the presence of varying concentrations of CP-447697. The displacement of the radiolabeled ligand is measured to determine the IC50. For functional assays, cells expressing the C5a receptor are treated with CP-447697 and stimulated with C5a.
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| Cell Assay |
For cellular assays, cells expressing the C5a receptor (e.g., neutrophils, macrophages) are cultured in appropriate media. Cells are treated with various concentrations of CP-447697 (typically 0.1-1000 nM) for defined periods. Calcium flux is measured using fluorescent dyes (e.g., Fluo-4). Chemotaxis is assessed using Transwell chambers. The inhibition of C5a-mediated signaling is measured. Cell viability is assessed using standard assays.
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| Animal Protocol |
In vivo, CP-447697 would be administered to animal models of inflammatory diseases. The compound is formulated in a suitable vehicle and administered at various doses via oral or intraperitoneal routes. Efficacy is assessed by measuring inflammatory markers, leukocyte infiltration, and disease severity. Pharmacokinetic studies involve measuring CP-447697 levels in plasma. Toxicological studies are performed.
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| ADME/Pharmacokinetics |
CP-447697 has a molecular weight of 554.05 g/mol and a molecular formula of C29H26ClF2N3O2S. It is a lipophilic C5a receptor antagonist. The compound should be stored as a powder at -20°C under desiccated conditions. Specific solubility and pharmacokinetic parameters are not detailed in the provided search results. It is soluble in DMSO and other organic solvents.
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| Toxicity/Toxicokinetics |
Specific toxicity data for CP-447697 is not available in the provided search results. As a C5a receptor antagonist, it may affect the immune system and potentially increase susceptibility to infections. The compound is intended for research purposes only and is not approved for human or veterinary use. Standard laboratory safety precautions should be followed when handling the compound.
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| References | |
| Additional Infomation |
CP-447697 is a lipophilic C5a receptor antagonist with an IC50 of 31 nM. It can be used for the research of inflammation. By blocking the C5a receptor, CP-447697 inhibits C5a-mediated inflammatory signaling. The compound is not approved for clinical use and is intended for research purposes only.
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| Molecular Formula |
C29H26CLF2N3O2S
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|---|---|
| Molecular Weight |
554.05
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| Exact Mass |
553.14
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| Elemental Analysis |
C, 62.87; H, 4.73; Cl, 6.40; F, 6.86; N, 7.58; O, 5.78; S, 5.79
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| CAS # |
1092847-21-6
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| PubChem CID |
44593654
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| Appearance |
White to off-white solid powder
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| LogP |
6.6
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
38
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| Complexity |
809
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1(C(NC2=CC=C(F)C=C2F)=O)CCC(N(C(C2=CSC3=CC=CC=C32)=O)CCC2=CC=C(Cl)C=C2)CC1
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| InChi Key |
UMERSEDFPNHLEN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C29H26ClF2N3O2S/c30-20-7-5-19(6-8-20)11-16-35(28(36)24-18-38-27-4-2-1-3-23(24)27)22-12-14-34(15-13-22)29(37)33-26-10-9-21(31)17-25(26)32/h1-10,17-18,22H,11-16H2,(H,33,37)
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| Chemical Name |
4-[1-benzothiophene-3-carbonyl-[2-(4-chlorophenyl)ethyl]amino]-N-(2,4-difluorophenyl)piperidine-1-carboxamide
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| Synonyms |
CP-447697; CP 447697; CP447697;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~225.61 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8049 mL | 9.0245 mL | 18.0489 mL | |
| 5 mM | 0.3610 mL | 1.8049 mL | 3.6098 mL | |
| 10 mM | 0.1805 mL | 0.9024 mL | 1.8049 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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