2. GPCR/G Protein
  3. Leukotriene Receptor
  4. CP-105696

CP-105696  (Synonyms: Pfizer 105696)

Cat. No.: HY-19193 Purity: 99.81%
SDS COA Handling Instructions

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CP-105696 is a potent and selective Leukotriene B4 Receptor antagonist, with an IC50 of 8.42 nM.

For research use only. We do not sell to patients.

CP-105696 Chemical Structure

CP-105696 Chemical Structure

CAS No. : 158081-99-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 110 In-stock
Solution
10 mM * 1 mL in DMSO USD 110 In-stock
Solid
5 mg USD 100 In-stock
10 mg USD 180 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

CP-105696 Related Antibodies

Top Publications Citing Use of Products

View All Leukotriene Receptor Isoform Specific Products:

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LTB4 LTC4/CysLT2 LTD4/CysLT1 LTE4

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

CP-105696 is a potent and selective Leukotriene B4 Receptor antagonist, with an IC50 of 8.42 nM.

IC50 & Target[1]

LTB4

8.42±0.26 nM (IC50)

In Vitro

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.

CP-105696 Related Antibodies
In Vivo

At a dose of 50 mg/kg/day (28 days), B10.BR (H2k) allografts transplanted into C57Bl/6 (H2b) recipients are significantly protected, as reflected by the mean survival time versus control grafts (27±20 days [n=10] vs. 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 (33±23 days [n=9]; P=0.0026), but CP-105696 at 10 mg/kg/day does not (18±16 days [n=8]; P=0.1433). Syngeneic grafts survive indefinitely (n=11). Immunohistological evaluation of allografts at rejection reveals a mononuclear cell infiltrate composed primarily 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 demonstrat a selective reduction in β2-integrin (Mac-1) expression on monocytes/macrophages, as demonstrated by CD11b staining density compared with allograft controls[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

428.52

Formula

C28H28O4
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.81%

SDS (392 KB)

COA (249 KB) HNMR (304 KB) LCMS (94 KB) OR (171 KB)

Handling Instructions (2659 KB)
References
Animal Administration
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

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
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CP-105696 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CP-105696158081-99-3Pfizer 105696CP105696CP 105696Pfizer105696Pfizer-105696Leukotriene ReceptorInhibitorinhibitorinhibit

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