2. GPCR/G Protein
  3. Prostaglandin Receptor
  4. Timapiprant sodium

Timapiprant sodium  (Synonyms: OC000459 sodium)

Cat. No.: HY-15342A Purity: 99.55%
COA Handling Instructions

Molarity Calculator

Timapiprant sodium (OC000459 sodium) is a potent, selective, and orally active D prostanoid receptor 2 (DP2, also known as CRTH2) antagonist. Timapiprant sodium (OC000459 sodium) potently displaces [3H] PGD2 from human recombinant DP2 (Ki=13 nM), rat recombinant DP2 (Ki=3 nM), and human native DP2 (Ki=4 nM). Timapiprant sodium (OC000459 sodium) inhibits mast cell activation of Th2 lymphocytes and eosinophils.

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

Timapiprant sodium Chemical Structure

Timapiprant sodium Chemical Structure

CAS No. : 950688-14-9

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 66 In-stock
Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Solid
5 mg USD 60 In-stock
10 mg USD 96 In-stock
25 mg USD 192 In-stock
50 mg USD 307 In-stock
100 mg USD 490 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

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

Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Timapiprant sodium:

Timapiprant sodium Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Timapiprant sodium (OC000459 sodium) is a potent, selective, and orally active D prostanoid receptor 2 (DP2, also known as CRTH2) antagonist. Timapiprant sodium (OC000459 sodium) potently displaces [3H] PGD2 from human recombinant DP2 (Ki=13 nM), rat recombinant DP2 (Ki=3 nM), and human native DP2 (Ki=4 nM). Timapiprant sodium (OC000459 sodium) inhibits mast cell activation of Th2 lymphocytes and eosinophils[1].

IC50 & Target

Ki: 0.013 μM (human recombinant DP2); 0.003 μM (rat recombinant DP2) and 0.004 μM (human native DP2)[1]
In Vitro

Timapiprant sodium (OC000459 sodium) (0.0001 μM-10 μM; 5 hours) inhibits chemotaxis (IC50=0.028 μM) of human Th2 lymphocytes and cytokine production (IC50=0.019 μM) by human Th2 lymphocytes[1].
Timapiprant sodium (OC000459 sodium) (1 μM) inhibits the activation of Th2 cells and eosinophils in response to supernatants from IgE/anti-IgE-activated human mast cells[1].
Timapiprant sodium (OC000459 sodium) (1 nM-1000 nM; 16 hours) inhibits the anti-apoptotic effect of PGD2 on Th2 cells with an IC50 of 0.035 uM[1].

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

Timapiprant sodium Related Antibodies

Apoptosis Analysis[1]

Cell Line: Th2 Cells
Concentration: 0.0001 μM-10 μM
Incubation Time: 16 hours
Result: Inhibited the antiapoptotic effect of PGD2.
In Vivo

Timapiprant sodium (OC000459 sodium) (gavage; 2 mg/kg, 10 mg/kg) inhibits blood eosinophilia induced by 13,14-dihydro-15-keto-PGD2 (DK-PGD2) in Rat (ED50=0.04 mg/kg)[1].
Timapiprant sodium (OC000459 sodium) (gavage; 0.01 mg/kg, 0.1 mg/kg, 1.0 mg/kg) inhibits airway eosinophilia in response to an aerosol of DK-PGD2 in guinea pigs (ED50=0.01 mg/kg)[1].

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

370.35

Formula

C21H16FN2NaO2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(O[Na])CN1C2=CC=C(F)C=C2C(CC3=NC4=C(C=CC=C4)C=C3)=C1C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (270.01 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 2.7001 mL 13.5007 mL 27.0015 mL
5 mM 0.5400 mL 2.7001 mL 5.4003 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 (stored under nitrogen). 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: ≥ 2.08 mg/mL (5.62 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.62 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

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: 99.61%

COA (247 KB) HNMR (207 KB) LCMS (121 KB)

Handling Instructions (2659 KB)
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 (stored under nitrogen). 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 2.7001 mL 13.5007 mL 27.0015 mL 67.5037 mL
5 mM 0.5400 mL 2.7001 mL 5.4003 mL 13.5007 mL
10 mM 0.2700 mL 1.3501 mL 2.7001 mL 6.7504 mL
15 mM 0.1800 mL 0.9000 mL 1.8001 mL 4.5002 mL
20 mM 0.1350 mL 0.6750 mL 1.3501 mL 3.3752 mL
25 mM 0.1080 mL 0.5400 mL 1.0801 mL 2.7001 mL
30 mM 0.0900 mL 0.4500 mL 0.9000 mL 2.2501 mL
40 mM 0.0675 mL 0.3375 mL 0.6750 mL 1.6876 mL
50 mM 0.0540 mL 0.2700 mL 0.5400 mL 1.3501 mL
60 mM 0.0450 mL 0.2250 mL 0.4500 mL 1.1251 mL
80 mM 0.0338 mL 0.1688 mL 0.3375 mL 0.8438 mL
100 mM 0.0270 mL 0.1350 mL 0.2700 mL 0.6750 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Timapiprant sodium 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:

Timapiprant950688-14-9OC000459OC 000459OC-000459Prostaglandin ReceptorInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Timapiprant sodium
Cat. No.:
HY-15342A
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.