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

Vidupiprant  (Synonyms: AMG 853)

Cat. No.: HY-14973 Purity: 98.33%
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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.

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Vidupiprant Chemical Structure

Vidupiprant Chemical Structure

CAS No. : 1169483-24-2

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Based on 1 publication(s) in Google Scholar

Vidupiprant Related Antibodies

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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]
Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
0.003 μM
Compound: 2, AMG-853
Displacement of [3H]-PGD2 from human CRTH2 receptor expressed in human HEK293 cells by scintillation counter in presence of 0.5% bovine serum albumin
Displacement of [3H]-PGD2 from human CRTH2 receptor expressed in human HEK293 cells by scintillation counter in presence of 0.5% bovine serum albumin
[PMID: 24900313]
HEK293 IC50
0.004 μM
Compound: 2, AMG-853
Displacement of [3H]-PGD2 from human Prostanoid DP receptor expressed in human HEK293 cells by scintillation counter in presence of 0.5% bovine serum albumin
Displacement of [3H]-PGD2 from human Prostanoid DP receptor expressed in human HEK293 cells by scintillation counter in presence of 0.5% bovine serum albumin
[PMID: 24900313]
HEK293 IC50
0.008 μM
Compound: 2, AMG-853
Displacement of [3H]-PGD2 from human CRTH2 receptor expressed in human HEK293 cells by scintillation counter in presence of 50% human plasma
Displacement of [3H]-PGD2 from human CRTH2 receptor expressed in human HEK293 cells by scintillation counter in presence of 50% human plasma
[PMID: 24900313]
HEK293 IC50
0.035 μM
Compound: 2, AMG-853
Displacement of [3H]-PGD2 from human Prostanoid DP receptor expressed in human HEK293 cells by scintillation counter in presence of 50% human plasma
Displacement of [3H]-PGD2 from human Prostanoid DP receptor expressed in human HEK293 cells by scintillation counter in presence of 50% human plasma
[PMID: 24900313]
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].

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

Vidupiprant Related Antibodies
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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

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; 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 1.6407 mL 8.2036 mL 16.4072 mL
5 mM 0.3281 mL 1.6407 mL 3.2814 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.10 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

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. 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 1.6407 mL 8.2036 mL 16.4072 mL 41.0179 mL
5 mM 0.3281 mL 1.6407 mL 3.2814 mL 8.2036 mL
10 mM 0.1641 mL 0.8204 mL 1.6407 mL 4.1018 mL
15 mM 0.1094 mL 0.5469 mL 1.0938 mL 2.7345 mL
20 mM 0.0820 mL 0.4102 mL 0.8204 mL 2.0509 mL
25 mM 0.0656 mL 0.3281 mL 0.6563 mL 1.6407 mL
30 mM 0.0547 mL 0.2735 mL 0.5469 mL 1.3673 mL
40 mM 0.0410 mL 0.2051 mL 0.4102 mL 1.0254 mL
50 mM 0.0328 mL 0.1641 mL 0.3281 mL 0.8204 mL
60 mM 0.0273 mL 0.1367 mL 0.2735 mL 0.6836 mL
80 mM 0.0205 mL 0.1025 mL 0.2051 mL 0.5127 mL
100 mM 0.0164 mL 0.0820 mL 0.1641 mL 0.4102 mL
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Vidupiprant 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:

Vidupiprant1169483-24-2AMG 853AMG853AMG-853Prostaglandin ReceptorCRTH2DPPGD2cAMPasthmaphenylaceticacidorallyAMG 009Inhibitorinhibitorinhibit

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