2. GPCR/G Protein
  3. Leukotriene Receptor Prostaglandin Receptor
  4. KP496

KP496 is a selective, dual antagonist for Leukotriene D4 receptor and Thromboxane A2 receptor.

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

KP496 Chemical Structure

KP496 Chemical Structure

CAS No. : 217799-03-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 1295 In-stock
Solution
10 mM * 1 mL in DMSO USD 1295 In-stock
Solid
1 mg USD 450 In-stock
5 mg USD 850 In-stock
10 mg USD 1360 In-stock
25 mg USD 2800 In-stock
50 mg USD 4500 In-stock
100 mg   Get quote  
200 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

KP496 Related Antibodies

Top Publications Citing Use of Products

View All Leukotriene Receptor Isoform Specific Products:

View All Isoforms
LTB4 LTC4/CysLT2 LTD4/CysLT1 LTE4

View All Prostaglandin Receptor Isoform Specific Products:

View All Isoforms
DP EP FP IP TXA2/TP TXB2

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

KP496 is a selective, dual antagonist for Leukotriene D4 receptor and Thromboxane A2 receptor.

IC50 & Target[1]

LTD4

 

TXA2 Receptor

 

In Vivo

KP496 significantly inhibits acute (day 7) and chronic (day 21) lung inflammation. KP496 attenuates the number of lymphocytes on day 7 and those of macrophages, neutrophils, and eosinophils on days 7 and 21. KP496 and prednisolone significantly suppress the increase of hydroxyl-L-proline content in the lung. Compare to respective vehicle control group, the inhibition ratio of KP496 and prednisolone for increase of hydroxyl-L-proline content is about 74 and 63%, respectively[1]. The KP496 (100 mg/head) group and prednisolone (10 mg/kg) group exhibit significant inhibition of numbers of infiltrating total cells, eosinophils, monocytes/macrophages, and lymphocytes compare with the control group. Infiltration of all types of cells except neutrophils is decreased in the KP496 (30m g/head) group, though not to significant extents[2].

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

692.27

Formula

C31H34ClN3O7S3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)C1=CC=CC=C1S(=O)(N(CCCCNS(=O)(C2=CC=C(Cl)C=C2)=O)CC3=CC=CC(OCC4=NC(C(C)C)=CS4)=C3)=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 (144.45 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 1.4445 mL 7.2226 mL 14.4452 mL
5 mM 0.2889 mL 1.4445 mL 2.8890 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 (3.61 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (3.61 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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: 99.79%

SDS (251 KB)

COA (248 KB) HNMR (279 KB) RP-HPLC (264 KB) MS (69 KB)

Handling Instructions (2659 KB)
References
Animal Administration
[1]

Male mice (9 weeks old, 33 to 42g are used) BLM solution (15 mg/mL) is intravenously injected into mice (0.1 mL/10 g of body weight) on day 0. Mice are sacrificed on day 7 or 21. They are exposed to an aerosol of KP496 (KP-496) solution (0.5%) for 30 min using a pressure nebulizer 1 h before and 3 h after BLM-injection on day 0. From day 1 to the day before sacrificed, mice are exposed to KP496 (0.5%) for 30 min morning and evening[1].

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 1.4445 mL 7.2226 mL 14.4452 mL 36.1131 mL
5 mM 0.2889 mL 1.4445 mL 2.8890 mL 7.2226 mL
10 mM 0.1445 mL 0.7223 mL 1.4445 mL 3.6113 mL
15 mM 0.0963 mL 0.4815 mL 0.9630 mL 2.4075 mL
20 mM 0.0722 mL 0.3611 mL 0.7223 mL 1.8057 mL
25 mM 0.0578 mL 0.2889 mL 0.5778 mL 1.4445 mL
30 mM 0.0482 mL 0.2408 mL 0.4815 mL 1.2038 mL
40 mM 0.0361 mL 0.1806 mL 0.3611 mL 0.9028 mL
50 mM 0.0289 mL 0.1445 mL 0.2889 mL 0.7223 mL
60 mM 0.0241 mL 0.1204 mL 0.2408 mL 0.6019 mL
80 mM 0.0181 mL 0.0903 mL 0.1806 mL 0.4514 mL
100 mM 0.0144 mL 0.0722 mL 0.1445 mL 0.3611 mL
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KP496 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:

KP496217799-03-6KP 496KP-496Leukotriene ReceptorProstaglandin ReceptorInhibitorinhibitorinhibit

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