1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. Timapiprant

Timapiprant (Synonyms: OC000459)

Cat. No.: HY-15342 Purity: 95.12%
Handling Instructions

Timapiprant (OC000459) is a potent and selective D prostanoid receptor 2 (DP2) antagonist with IC50 of 13 nM.

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

Timapiprant Chemical Structure

Timapiprant Chemical Structure

CAS No. : 851723-84-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 73 In-stock
Estimated Time of Arrival: December 31
5 mg USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 113 In-stock
Estimated Time of Arrival: December 31
50 mg USD 408 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

Timapiprant (OC000459) is a potent and selective D prostanoid receptor 2 (DP2) antagonist with IC50 of 13 nM.

IC50 & Target

IC50 Value: 13 nM( Ki for hrCRTH2); 3 nM( Ki for Rat rCRTH2);13 nM(Ki for human native CRTH2)

In Vitro

OC000459 is an indole-acetic acid derivative that potently displaces [3H]PGD2from human recombinant DP2 (Ki = 0.013 μM), rat recombinant DP2 (Ki = 0.003 μM), and human native DP2 (Th2 cell membranes; Ki = 0.004 μM) but does not interfere with the ligand binding properties or functional activities of other prostanoid receptors (prostaglandin E1-4 receptors, D prostanoid receptor 1, thromboxane receptor, prostacyclin receptor, and prostaglandin F receptor). OC000459 inhibited chemotaxis (IC50 = 0.028 μM) of human Th2 lymphocytes and cytokine production (IC50 = 0.019 μM) by human Th2 lymphocytes. OC000459 competitively antagonized eosinophil shape change responses induced by PGD2 in both isolated human leukocytes (pKB = 7.9) and human whole blood (pKB = 7.5) but did not inhibit responses to eotaxin, 5-oxo-eicosatetraenoic acid, or complement component C5a. OC000459 also inhibited the activation of Th2 cells and eosinophils in response to supernatants from IgE/anti-IgE-activated human mast cells. OC000459 had no significant inhibitory activity on a battery of 69 receptors and 19 enzymes including cyclooxygenase 1 (COX1) and COX2[3] .

In Vivo

OC000459 was found to be orally bioavailable in rats and effective in inhibiting blood eosinophilia induced by 13,14-dihydro-15-keto-PGD2 (DK-PGD2) in this species (ED50 = 0.04 mg/kg p.o.) and airway eosinophilia in response to an aerosol of DK-PGD2 in guinea pigs (ED50 = 0.01 mg/kg p.o.) [3].

Clinical Trial
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 : 4 mg/mL (11.48 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8705 mL 14.3526 mL 28.7051 mL
5 mM 0.5741 mL 2.8705 mL 5.7410 mL
10 mM 0.2871 mL 1.4353 mL 2.8705 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.4 mg/mL (1.15 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Molecular Weight

348.37

Formula

C₂₁H₁₇FN₂O₂

CAS No.

851723-84-7

SMILES

O=C(O)CN1C(C)=C(CC2=NC3=CC=CC=C3C=C2)C4=C1C=CC(F)=C4

Shipping

Room temperature in continental US; may vary elsewhere

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Timapiprant
Cat. No.:
HY-15342
Quantity:

Timapiprant

Cat. No.: HY-15342