CP-105696 NEW
| Price | $81 | $147 |
| Package | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2025-11-09 |
Product Details
| Product Name: CP-105696 | CAS No.: 158081-99-3 |
| Purity: 99.78% | Supply Ability: 10g |
| Release date: 2025/11/09 |
Product Introduction
Bioactivity
| Name | CP-105696 |
| Description | CP-105696 is a potent and selective leukotriene B4 (LTB4) receptor antagonist used to study allograft rejection. |
| In vitro | CP-105696 is a structurally novel, selective, and potent LTB4 receptor antagonist. In vitro, it inhibits [3H]LTB4 (0.3 nM) binding to high-affinity LTB4 receptors on human neutrophils with an IC50 of 8.42±0.26 nM and acts as a noncompetitive antagonist. It noncompetitively inhibits LTB4 (5 nM)-mediated human neutrophil chemotaxis with an IC50 of 5.0±2.0 nM. For low-affinity receptors on neutrophils, CP-105696 acts as a competitive antagonist according to Scatchard analyses. Additionally, it competitively inhibits LTB4-mediated CD11b upregulation on human neutrophils (pA2=8.03±0.19). At 10 μM, CP-105696 does not inhibit human neutrophil chemotaxis or CD11b upregulation mediated by other G-protein coupled receptors (e.g., C5a, IL-8, PAF). In isolated human monocytes, it inhibits LTB4 (5 nM)-mediated Ca2+ mobilization with an IC50 of 940±70 nM[2]. |
| In vivo | At a dose of 50 mg/kg/day for 28 days, B10.BR (H2k) allografts transplanted into C57Bl/6 (H2b) recipients show significant protection, with mean survival time of 27±20 days (n=10) compared to control grafts' 12±6 days (n=14); P=0.0146. Using an induction protocol (day -1 to day 3), CP-105696 at 100 mg/kg/day significantly prolongs allograft survival to 33±23 days (n=9; P=0.0026), whereas at 10 mg/kg/day, it does not (18±16 days; n=8; P=0.1433). Syngeneic grafts exhibit indefinite survival (n=11). Immunohistological evaluation of allografts at rejection reveals a mononuclear cell infiltrate primarily composed of CD3+ and CD11b+ (Mac-1+) cells, which are infrequent in syngeneic grafts. Allografts from mice treated with CP-105696 at 50 or 100 mg/kg/day show a selective reduction in β2-integrin (Mac-1) expression on monocytes/macrophages, as indicated by CD11b staining density compared with allograft controls[1]. |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 80 mg/mL (186.69 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (7.7 mM), Sonication is recommended. |
| Keywords | plusmn | LTB4 | CP-105696 | CP105696 | CP 105696 |
| Inhibitors Related | Montelukast sodium | LTB4-IN-1 | L 674573 | Olsalazine disodium | Desloratadine | CGP 35949 | Bestatin | Tebufelone | ABT-080 | LTβR-IN-1 | Darbufelone mesylate | Ticolubant |
| Related Compound Libraries | Bioactive Compound Library | Inhibitor Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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- Since: 2011-01-07
- Address: 36 Washington Street, Wellesley Hill, MA
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