| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Targets |
CP-105696 targets the leukotriene B4 (LTB4) receptor (LTB4R). LTB4 is a potent chemoattractant and pro-inflammatory lipid mediator. The compound is a selective and structurally unique LTB4 receptor antagonist. It inhibits LTB4 binding to both high-affinity and low-affinity receptors on neutrophils.
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| ln Vitro |
CP-105696 is an extremely selective and structurally unique LTB4 receptor antagonist. With an IC50 value of 8.42±0.26 nM, CP-105696 inhibits the binding of [3H]LTB4 (0.3 nM) to the high-affinity LTB4 receptor on human neutrophils in vitro. When [3H]LTB4 binds to these high-affinity receptors, CP-105696 binds to the receptors noncompetitively, as revealed by Scatchard analysis. With an IC50 value of 5.0±2.0 nM, CP-105696 inhibits human neutrophil chemotaxis mediated by LTB4 (5 nM) in a non-competitive manner. By using Scatchard analysis, it is possible to determine that CP-105696 functions as a competitive antagonist for [3H]LTB4 binding to low-affinity receptors on neutrophils and that it competitively inhibits LTB4-mediated inhibition of human neutrophil CD11b was increased (pA2= 8.03±0.19). At 10 μM, CP-105696 does not prevent CD11b overexpression or human neutrophil chemotaxis that is mediated by G protein-coupled chemokine receptors other than C5a, IL-8, or PAF. CP-105696, with an IC50 value of 940±70 nM, inhibits LTB4 (5 nM)-mediated Ca2+ mobilization in isolated human monocytes[1].
In vitro, CP-105696 is an extremely selective LTB4 receptor antagonist with an IC50 of 8.42±0.26 nM for inhibiting [3H]LTB4 binding to the high-affinity receptor on human neutrophils. It inhibits human neutrophil chemotaxis mediated by LTB4 with an IC50 of 5.0±2.0 nM. It inhibits LTB4-mediated Ca2+ mobilization in isolated human monocytes with an IC50 of 940±70 nM. |
| ln Vivo |
B10.BR (H2k) allografts transplanted into C57Bl/6 (H2b) recipients were considerably protected as compared with control grafts at a dose of 50 mg/kg/day (28 days) Reflected by mean survival time (27 ± 20 days) [n = 10] vs. 12 ± 6 days [n = 14]; P = 0.0146). Using the induction regimen (days -1 to 3), CP-105696 at 100 mg/kg/day significantly increased allograft survival (33±23 days [n=9]; P=0.0026) , but not 10 mg of CP-105696/kg/day (18±16 days [n=8]; P=0.1433). Syngeneic grafts survived indefinitely (n=11). Immunohistological assessment of allograft rejection revealed a mononuclear cell infiltrate comprised predominantly of CD3+ and CD11b+ (Mac-1+) cells, which is rarely found in syngeneic grafts. Allografts from mice treated with 50 or 100 mg/kg/day CP-105696 revealed preferential reduction in β2-integrin (Mac-1) expression on monocytes/macrophages, consistent with allogeneic This was verified by the density of CD11b staining relative to allograft controls [2].
In vivo, CP-105696 at 50 mg/kg/day significantly protected B10.BR (H2k) allografts transplanted into C57Bl/6 (H2b) recipients, with a mean survival time of 27±20 days vs. 12±6 days for controls. At 100 mg/kg/day, it significantly increased allograft survival (33±23 days). It reduced β2-integrin expression on monocytes/macrophages in allografts. |
| Enzyme Assay |
The in vitro receptor binding assay for CP-105696 involves measuring its inhibition of [3H]LTB4 binding to LTB4 receptors on human neutrophils. The IC50 of 8.42±0.26 nM is determined. Scatchard analysis reveals non-competitive binding to high-affinity receptors and competitive binding to low-affinity receptors.
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| Cell Assay |
In vitro cell-based assays for CP-105696 involve treating human neutrophils or monocytes with the compound and measuring LTB4-induced chemotaxis, CD11b expression, or Ca2+ mobilization. The compound’s effects on these LTB4-mediated responses are quantified.
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| Animal Protocol |
In vivo animal studies for CP-105696 involve transplantation models in mice. B10.BR (H2k) allografts are transplanted into C57Bl/6 (H2b) recipients, and CP-105696 is administered orally. Allograft survival is monitored, and immunohistological assessment of rejection is performed.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of CP-105696 are not detailed in the provided literature. The compound is orally active.
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| Toxicity/Toxicokinetics |
No specific toxicity data for CP-105696 are available in the provided literature. The compound is for research use only.
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| References |
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| Additional Infomation |
CP-105696 is a potent, selective LTB4 receptor antagonist. It has an IC50 of 8.42 nM. It is orally active. It is for research use only. Its CAS number is 158081-99-3.
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| Molecular Formula |
C28H28O4
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| Molecular Weight |
428.51952
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| Exact Mass |
428.198
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| CAS # |
158081-99-3
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| PubChem CID |
9867257
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| Appearance |
White to light yellow solid powder
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| LogP |
5.5
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
32
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| Complexity |
627
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| Defined Atom Stereocenter Count |
2
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| 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
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| InChi Key |
KMNLXCBYBKHKSK-BKMJKUGQSA-N
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| InChi Code |
InChI=1S/C28H28O4/c29-26-22(16-19-8-10-21(11-9-19)20-6-2-1-3-7-20)18-32-25-17-23(12-13-24(25)26)28(27(30)31)14-4-5-15-28/h1-3,6-13,17,22,26,29H,4-5,14-16,18H2,(H,30,31)/t22-,26+/m0/s1
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| Chemical Name |
1-[(3S,4R)-4-hydroxy-3-[(4-phenylphenyl)methyl]-3,4-dihydro-2H-chromen-7-yl]cyclopentane-1-carboxylic acid
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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 |
| 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 : ~100 mg/mL (~233.36 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.83 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.83 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.83 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3336 mL | 11.6681 mL | 23.3361 mL | |
| 5 mM | 0.4667 mL | 2.3336 mL | 4.6672 mL | |
| 10 mM | 0.2334 mL | 1.1668 mL | 2.3336 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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