CP-105696
Based on 5 publication(s) in Google Scholar
CP-105696 is a potent and selective Leukotriene B4 Receptor antagonist, with an IC50 of 8.42 nM.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.93%
- CAS. Nr.: 158081-99-3
- Formel: C28H28O4
- Molecular Weight:428.52
-
Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
-
Biologische Aktivität
-
Chemical Information
-
Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
-
GPCR/G Protein Compound Library
HY-L006
-
Immunology/Inflammation Compound Library
HY-L007
-
Clinical Compound Library
HY-L026
-
Membrane Protein-targeted Compound Library
HY-L149
-
Membrane Receptor-targeted Compound Library
HY-L150
-
Highly Selective Inhibitors Library
HY-L158
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Clinical Compound Library Plus
HY-L026P
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
-
Anti-Rheumatic Arthritis Compound Library
HY-L210
-
Lactylation Compound Library
HY-L249
Publications Citing Use of MedChemExpress (MCE) CP-105696
MoreAlle Leukotriene Receptor Isoform-spezifische Produkte anzeigen
More
Biologische Aktivität
|
LTB4 8.42±0.26 nM (IC50) |
CP-105696 is a structurally novel, selective and potent LTB4 receptor antagonist. In vitro, CP-105696 inhibits [3H]LTB4 (0.3 nM) binding to high-affinity LTB4 receptors on human neutrophils with an lC50 value of 8.42±0.26 nM. Scatchard analyses of [3H]LTB4 binding to these high-affinity receptors indicate that CP-105696 acts as a noncompetitive antagonist. CP-105696 inhibits human neutrophil chemotaxis mediated by LTB4 (5 nM) in a noncompetitive manner with an IC50 value of 5.0±2.0 nM. Scatchard analyses of [3H]LTB4 binding to low-affinity receptors on neutrophils indicate that CP-105696 acts as a competitive antagonist at this receptor, and inhibition of LTB4-mediated CD11b upregulation on human neutrophils is competitively inhibited by CP-105696 (pA2=8.03±0.19). CP-105696 at 10 μM does not inhibit either human neutrophil chemotaxis or CD11b upregulation mediated through alternate (i.e., C5a, lL-8, PAF) G-protein coupled chemotactic factor receptors. In isolated human monocytes, LTB4 (5 nM)-mediated Ca2+ mobilization is inhibited by CP-105696 with an lC50 value of 940±70 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS. Nr. 158081-99-3
-
Appearance Solid
-
Molecular Weight 428.52
-
Formel C28H28O4
-
Color White to light yellow
-
SMILES
O=C(C1(C2=CC=C3[C@H](O)[C@@H](CC4=CC=C(C5=CC=CC=C5)C=C4)COC3=C2)CCCC1)O
-
Synonyms
Pfizer 105696
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (5)
-
Journal Impact Factor
-
Most Recent
-
Nat Commun
Sirt6 deficiency in mast cells promotes adipose fibroinflammation in obesity through galectin-3 signaling. [Abstract]2026 Jan 6;17(1):57. PMID: 41495031 -
-
J Leukoc Biol
Caging giants: Characterizing the molecular mechanisms of neutrophil swarming against Candida albicans hyphae. [Abstract]2025 Jun 6:qiaf082. PMID: 40476443 -
-
bioRxiv
APOE Protects Against Severe Infection with Mycobacterium tuberculosis by Restraining Production of Neutrophil Extracellular Traps. [Abstract]2024 Oct 4:2024.10.04.616580. PMID: 39605723
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (233.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.83 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.83 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
Mice[2]
Allogeneic donor hearts are harvested after intravenous heparinization of donor B10.BR mice (H2k) and are preserved via retrograde perfusion with cold cardioplegia solution into the left ventricle. Recipient C57Bl/6 mice (H2b) are prepared by ligating the lumbar vessels and isolating the abdominal aorta and vena cava; donor hearts are sutured in place by microvascular anastomoses of the donor aorta and pulmonary artery to the recipient aorta and inferior vena cava, respectively. CP-105696 is evaluated in a 28-day treatment protocol (50 mg/kg/day), a high-dose (100 mg/kg/day) induction protocol (day -1 to day 3), and a low-dose (10 mg/kg/day) induction protocol (day -1 to day 3). In all study groups, drug is administered orally in a 0.5% methylcellulose vehicle. In parallel studies, treatment of C57Bl/6 (H2b) recipients bearing B10.BR (H2k) cardiac allografts given FK506 (2 mg/kg/day for 28 days), our standard control immunosuppressant, significantly prolongs allograft survival (mean survival time [MST], 40±18 days [n=9]; P=0.0002)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
-
Data Sheet (279 KB)
-
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
-
Handling Instructions (2659 KB)
Verweise
[1]. Showell HJ, et al. The in vitro and in vivo pharmacologic activity of the potent and selective leukotriene B4 receptor antagonist CP-105696. J Pharmacol Exp Ther. 1995 Apr;273(1):176-84. [Content Brief]
[2]. Weringer EJ, et al. Antagonizing leukotriene B4 receptors delays cardiac allograft rejection in mice. Transplantation. 1999 Mar 27;67(6):808-15. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3336 mL | 11.6681 mL | 23.3361 mL | 58.3403 mL |
| 5 mM | 0.4667 mL | 2.3336 mL | 4.6672 mL | 11.6681 mL | |
| 10 mM | 0.2334 mL | 1.1668 mL | 2.3336 mL | 5.8340 mL | |
| 15 mM | 0.1556 mL | 0.7779 mL | 1.5557 mL | 3.8894 mL | |
| 20 mM | 0.1167 mL | 0.5834 mL | 1.1668 mL | 2.9170 mL | |
| 25 mM | 0.0933 mL | 0.4667 mL | 0.9334 mL | 2.3336 mL | |
| 30 mM | 0.0778 mL | 0.3889 mL | 0.7779 mL | 1.9447 mL | |
| 40 mM | 0.0583 mL | 0.2917 mL | 0.5834 mL | 1.4585 mL | |
| 50 mM | 0.0467 mL | 0.2334 mL | 0.4667 mL | 1.1668 mL | |
| 60 mM | 0.0389 mL | 0.1945 mL | 0.3889 mL | 0.9723 mL | |
| 80 mM | 0.0292 mL | 0.1459 mL | 0.2917 mL | 0.7293 mL | |
| 100 mM | 0.0233 mL | 0.1167 mL | 0.2334 mL | 0.5834 mL |
Powered by Bioz