2. GPCR/G Protein
  3. Prostaglandin Receptor
  4. Laropiprant

Laropiprant  (Synonyms: MK-0524)

Cat. No.: HY-50175 Purity: 99.93%
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Laropiprant is a potent and selective DP receptor antagonist with Ki values of 0.57 nM and 2.95 nM for DP receptor and TP Receptor, respectively.

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

Laropiprant Chemical Structure

Laropiprant Chemical Structure

CAS No. : 571170-77-9

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Other Forms of Laropiprant:

Laropiprant Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Laropiprant is a potent and selective DP receptor antagonist with Ki values of 0.57 nM and 2.95 nM for DP receptor and TP Receptor, respectively[1][2][3].

IC50 & Target[1]

DP

0.57 nM (Ki)

TP Receptor

2.95 nM (Ki)

In Vitro

Laropiprant (0.01-1000 μM; 10 mins; HEK293 cells) is an inverse agonist of DP1 cAMP signaling and reduces DP1 cAMP signaling below basal levels[1].
Laropiprant (1 μM; 0-24 h; HEK293 cells) is a pharmacochaperone in promoting DP1 cell surface expression[1].

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

Laropiprant Related Antibodies
In Vivo

Laropiprant (0-100 mg/kg; p.o. and i.v.; male Sprague-Dawley rats) exhibits good pharmacokinetic profiles[3].

Pharmacokinetic Analysis in Male Sprague-Dawley rats[3]

Route Dose (mg/kg) AUC0-∞ (μM·hr) Clp (mL/min/kg) Vdss (L/kg) T1/2 (hr)
PO 1 22.7 1.9 0.7 7.4
PO 5 96.0 2.1 0.9 7.6
Route Dose (mg/kg) AUC0-∞ (μM·hr) Cmax (μM) Tmax (hr) F(%)
IV 5 52.6 15.6 1.2 /

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

435.90

Formula

C21H19ClFNO4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=CC(F)=CC2=C1N(C3=C2CC[C@@H]3CC(O)=O)CC4=CC=C(Cl)C=C4)(C)=O
Shipping

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

DMSO : ≥ 100 mg/mL (229.41 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2941 mL 11.4705 mL 22.9410 mL
5 mM 0.4588 mL 2.2941 mL 4.5882 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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 (5.74 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 (5.74 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
References
Cell Assay
[2]

Vena8Fluoro+ Biochips are coated with collagen (200 µg/mL) at 4°C overnight and thereafter blocked with bovine serum albumin (10 µg/mL) for 30 minutes at room temperature followed by washing steps. Whole blood collected in sodium citrate is incubated with 3, 3-dihexyloxacarbocyanine iodide (1 µM) in the dark for 10 minutes. PGD2 (30 nM), BW245c (3 nM) are added 10 min before the start of perfusion, and the DP antagonist BWA868c or Laropiprant (1 µM) are added 10 min before the agonists. In another set of experiments whole blood is treated with niacin (3 mM), acetylsalicylic acid (1 mM) or Laropiprant (1 µM and 10 µM) for 30 min. CaCl2 at a final concentration of 1 mM is added 2 minutes before the perfusion over the collagen-coated chip. Perfusion is carried out at a shear rate of 30 dynes cm2. Thrombus formation is recorded. Computerized image analysis is performed by DucoCell analysis software, where the area covered by the thrombus is calculated. Data are expressed as percent of area covered in a control sample[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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2941 mL 11.4705 mL 22.9410 mL 57.3526 mL
5 mM 0.4588 mL 2.2941 mL 4.5882 mL 11.4705 mL
10 mM 0.2294 mL 1.1471 mL 2.2941 mL 5.7353 mL
15 mM 0.1529 mL 0.7647 mL 1.5294 mL 3.8235 mL
20 mM 0.1147 mL 0.5735 mL 1.1471 mL 2.8676 mL
25 mM 0.0918 mL 0.4588 mL 0.9176 mL 2.2941 mL
30 mM 0.0765 mL 0.3824 mL 0.7647 mL 1.9118 mL
40 mM 0.0574 mL 0.2868 mL 0.5735 mL 1.4338 mL
50 mM 0.0459 mL 0.2294 mL 0.4588 mL 1.1471 mL
60 mM 0.0382 mL 0.1912 mL 0.3824 mL 0.9559 mL
80 mM 0.0287 mL 0.1434 mL 0.2868 mL 0.7169 mL
100 mM 0.0229 mL 0.1147 mL 0.2294 mL 0.5735 mL
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Laropiprant 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:

Laropiprant571170-77-9MK-0524MK0524MK 0524Prostaglandin ReceptorDP receptorpharmacokineticsmetabolismacylglucuronideInhibitorinhibitorinhibit

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