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

Vidupiprant (Synonyms: AMG 853)

Cat. No.: HY-14973 Purity: 98.08%
Handling Instructions

Vidupiprant (AMG 853) is a phenylacetic acid derivative. Vidupiprant is a potent and orally active CRTH2 (DP2) and prostanoid D receptor (DP or DP1) dual antagonist with IC50s of 3 nM and 4 nM in buffer, and 8 nM and 35 nM in human plasma, respectively. Vidupiprant has the potential for asthma treatment.

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

Vidupiprant Chemical Structure

Vidupiprant Chemical Structure

CAS No. : 1169483-24-2

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Based on 1 publication(s) in Google Scholar

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Description

Vidupiprant (AMG 853) is a phenylacetic acid derivative. Vidupiprant is a potent and orally active CRTH2 (DP2) and prostanoid D receptor (DP or DP1) dual antagonist with IC50s of 3 nM and 4 nM in buffer, and 8 nM and 35 nM in human plasma, respectively. Vidupiprant has the potential for asthma treatment[1].

IC50 & Target

Prostaglandin Receptor[1]

In Vitro

Vidupiprant (AMG 853, Compound 2) inhibits the prostaglandin D2 (PGD2)-induced down-modulation of CRTH2 on CD16 negative granulocytes (eosinophils) in human whole blood with a Kb of 0.2 nM. Vidupiprant also inhibits PGD2-induced cAMP response in platelets in 80% human whole blood with a Kb of 4.7 nM, which is significantly improved, as compared to the Kb of 148 nM of AMG 009. In addition, Vidupiprant demonstrates similar antagonist activity in an aequorin assay using CRTH2-transfected HEK 293 cells and an eosinophil shape change assay, as compared to the CRTH2 receptor down-modulation human whole blood assay[1].

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

In Vivo

The significant improvement of DP potency of Vidupiprant (AMG 853, Compound 2) over AMG 009 is also demonstrated in vivo in a guinea pig model of PGD2-induced airway constriction. In this model, airway resistance is measured in response to PGD2 challenge. The in vitro guinea pig DP potency is evaluated in guinea pig whole blood cAMP assay.Vidupiprant has a Kb of 5 nM, while the Kb of AMG 009 is 82 nM[1].

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

Clinical Trial
Molecular Weight

609.49

Formula

C₂₈H₂₇Cl₂FN₂O₆S

CAS No.
SMILES

O=C(O)CC1=CC(Cl)=C(OC2=CC=C(C(NC(C)(C)C)=O)C=C2NS(=O)(C3=CC=C(C4CC4)C=C3Cl)=O)C=C1F

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 (164.07 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6407 mL 8.2036 mL 16.4072 mL
5 mM 0.3281 mL 1.6407 mL 3.2814 mL
10 mM 0.1641 mL 0.8204 mL 1.6407 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.10 mM); Clear solution

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

VidupiprantAMG 853AMG853AMG-853Prostaglandin ReceptorCRTH2DPPGD2cAMPasthmaphenylaceticacidorallyAMG 009Inhibitorinhibitorinhibit

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Vidupiprant
Cat. No.:
HY-14973
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