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

Timapiprant sodium (Synonyms: OC000459 sodium)

Cat. No.: HY-15342A Purity: 99.91%
Handling Instructions

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.

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Timapiprant sodium Chemical Structure

Timapiprant sodium Chemical Structure

CAS No. : 950688-14-9

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10 mM * 1  mL in DMSO USD 132 In-stock
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10 mg USD 190 In-stock
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Based on 1 publication(s) in Google Scholar

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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].

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].

Clinical Trial
Molecular Weight

370.35

Formula

C₂₁H₁₆FN₂NaO₂

CAS No.

950688-14-9

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)

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
10 mM 0.2700 mL 1.3501 mL 2.7001 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: ≥ 2.08 mg/mL (5.62 mM); Clear solution

  • 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

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

Purity: 99.91%

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Keywords:

TimapiprantOC000459OC 000459OC-000459Prostaglandin ReceptorInhibitorinhibitorinhibit

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Timapiprant sodium
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