Cat. No.: HY-156649

Vorbipiprant

(Synonyms: CR6086)

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Vorbipiprant (CR6086) is an orally active EP4 receptor antagonist with high selectivity for the human EP4 receptor (K_i: 16.6 nM). Vorbipiprant has immunomodulatory, anti-inflammatory, antitumor, and anti-angiogenic activities. Vorbipiprant can inhibit the expression of multiple pro-inflammatory cytokines and the activation of immune cells, and convert "cold" tumors unresponsive to immune checkpoint inhibitors into "hot" tumors. Vorbipiprant is used in the research of diseases such as rheumatoid arthritis and colon cancer.

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Pureté: 98.89%
CAS No.: 1417742-86-9
Formule: C₂₆H₂₇F₃N₂O₃
Masse moléculaire:472.50

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Vorbipiprant Chemical Structure

CAS No.: 1417742-86-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]^[2]

human EP4-R

16.6 nM (Ki)

IL-6

70 nM (IC₅₀)

IL-23

608 nM (IC₅₀)

IL-17

MMP-9

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In Vitro

Vorbipiprant (0.01-30 μM; 3-24 h) dose-dependently reduces LPS (HY-D1056) and PGE₂-induced IL-6 and VEGF gene expression in human THP-1-derived macrophages, with IC₅₀ values of 70 and 25 nM, respectively^[1].
Vorbipiprant (0.01-30 μM; 24 h) dose-dependently decreases PGE₂-stimulated IL-23 release in human dendritic cells, with an IC₅₀ of 608 nM^[1].
Vorbipiprant (0.03-10 μM; 48 h) dose-dependently inhibits PGE₂-induced IL-17 release in human Th17 cells, with complete inhibition at 1 μM^[1].

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

In Vivo

Vorbipiprant (30-60 mg/kg; oral administration; 10 days) improves arthritis in mouse models, and its efficacy is further enhanced when combined with Methotrexate (HY-14519)^[1].
Vorbipiprant (30 mg/kg; oral administration; 14 days) exhibits antitumor activity in a mouse colon cancer model when used in combination with an anti-PD-1 monoclonal antibody^[2].
Pharmacokinetic Analysis in Rats^[1]

Dose (mg/kg) and Route	1 and p.o.	3 and p.o.	10 and p.o.	15 and p.o.	30 and p.o.
C_max (ng/mL)	1250	3230	14500	11900	34500
t_max (h)	0.25	0.25	0.5	0.5	1
AUC (ng·h/mL)	2170	13700	58000	61600	206000

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

Animal Model:

Male DBA/1 mice aged 6-7 weeks old treated bovine collagen type II (HY-NP158)^[1]
Dosage:

30 and 60 mg/kg
Administration:

Oral administration; 10 days
Result:

Significantly improved clinical score, paw swelling, and histology (cartilage/bone damage, synovial hyperplasia).
Reduced Th1/Th17 cells and macrophages in joints, normalized IL-6 serum levels.
Showed synergistic effects with methotrexate, reducing disease activity below baseline levels.

Animal Model:

Female BALB/c mice treated CT26 colon carcinoma cells and anti-PD-1 mAb^[2]
Dosage:

30 mg/kg
Administration:

Oral administration; 14 days
Result:

Significantly decreased tumor growth.
Increased gene expression of key factors for lymphocyte recruitment and activation (e.g., CCL4, CCL5, CXCL10, CD8α, H2-Eb1s, INFγ, TNFα, PD-L1).
Enhanced general and T cell infiltrate in tumors.
Reduced gene expression of MMP-9.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1417742-86-9
Appearance Solid
Masse moléculaire 472.50
Formule C₂₆H₂₇F₃N₂O₃
Color White to off-white
SMILES

O=C(C1=CC=C(C2(CC2)NC(C3N(CCC4(C3)CC4)CC5=CC=C(C(F)(F)F)C=C5)=O)C=C1)O
Synonyms

CR6086
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

In Vitro:

DMSO : 200 mg/mL (423.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1164 mL

10.5820 mL

21.1640 mL

5 mM

0.4233 mL

2.1164 mL

4.2328 mL

10 mM

0.2116 mL

1.0582 mL

2.1164 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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: ≥ 5 mg/mL (10.58 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 5 mg/mL (10.58 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (10.58 mM); Clear solution

This protocol yields a clear solution of ≥ 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (280 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Caselli G, et al. Pharmacological characterisation of CR6086, a potent prostaglandin E2 receptor 4 antagonist, as a new potential disease-modifying anti-rheumatic drug. Arthritis Res Ther. 2018 Mar 1;20(1):39. [Content Brief]

[2]. Caselli G, et al. Combination of the EP4 antagonist CR6086 and anti-PD-1 monoclonal antibody inhibits tumor growth in a microsatellite stable colorectal cancer in mice. Cancer Research, 2020, 80(16_Supplement): 2208-2208.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.1164 mL	10.5820 mL	21.1640 mL	52.9101 mL
	5 mM	0.4233 mL	2.1164 mL	4.2328 mL	10.5820 mL
	10 mM	0.2116 mL	1.0582 mL	2.1164 mL	5.2910 mL
	15 mM	0.1411 mL	0.7055 mL	1.4109 mL	3.5273 mL
	20 mM	0.1058 mL	0.5291 mL	1.0582 mL	2.6455 mL
	25 mM	0.0847 mL	0.4233 mL	0.8466 mL	2.1164 mL
	30 mM	0.0705 mL	0.3527 mL	0.7055 mL	1.7637 mL
	40 mM	0.0529 mL	0.2646 mL	0.5291 mL	1.3228 mL
	50 mM	0.0423 mL	0.2116 mL	0.4233 mL	1.0582 mL
	60 mM	0.0353 mL	0.1764 mL	0.3527 mL	0.8818 mL
	80 mM	0.0265 mL	0.1323 mL	0.2646 mL	0.6614 mL
	100 mM	0.0212 mL	0.1058 mL	0.2116 mL	0.5291 mL

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Vorbipiprant

Voir tous les produits spécifiques à Isoform Prostaglandin Receptor

Voir tous les produits spécifiques à Isoform Interleukin Related

Voir tous les produits spécifiques à Isoform MMP

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Vorbipiprant Related Classifications

HY-156649 Related Classifications