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Cat. No.: HY-182637

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ACT-774312

ACT-774312 is a potent and selective CRTH2 antagonist with an IC₅₀ of 4 nM. ACT-774312 blocks the activity and internalization of the CRTH2 receptor, and inhibits PGD₂-induced morphological changes in eosinophils. ACT-774312 can be used in the research of nasal polyps and type 2 inflammatory diseases.

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

CAS No.: 1809863-68-0
Formula: C₁₈H₁₇ClFN₅O₂
Molecular Weight:389.81

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

ACT-774312 Chemical Structure

CAS No.: 1809863-68-0

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Biological Activity
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- In Vitro
- Parmacokinetics
Chemical Information
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Biological Activity

Description

All Prostaglandin Receptor Isoforms :

In Vitro

ACT-774312 potently inhibits PGD₂-induced eosinophil morphological changes under conditions containing 50% human plasma, with an IC₅₀ of 3 nM^[1]^[2].

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

Parmacokinetics

Species	Dose	Route	AUC_0-∞	CL	V_ss	T_1/2	C_max	T_max	F
Rat^[1]	1 mg/kg	i.v.	4.05 μg·h/mL	4.1	0.45 L/kg	3.2 h	/	/	/
Rat^[1]	2 mg/kg	p.o.	8.43 μg·h/mL	/	/	/	1.29 μg/mL	0.3 h	104 %
Dog^[1]	1 mg/kg	i.v.	9.24 μg·h/mL	1.8	0.45 L/kg	5.7 h	/	/	/
Dog^[1]	2 mg/kg	p.o.	7.24 μg·h/mL	/	/	/	2.41 μg/mL	1 h	78 %

Chemical Information

CAS No. 1809863-68-0
Molecular Weight 389.81
Formula C₁₈H₁₇ClFN₅O₂
SMILES

OC(CN1C2=C(C[C@H](CC2)N(C3=NC=C(Cl)C=N3)C)C4=NC(F)=CC=C41)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Aissaoui H, et al. Design, Synthesis, and Optimization of Indole Acetic Acid Derivatives as Potent and Selective CRTH2 Receptor Antagonists: Discovery of ACT-774312. ChemMedChem. 2023;18(10):e202300007. [Content Brief]

[2]. Géhin M, et al. Pharmacokinetics, pharmacodynamics, tolerability and prediction of clinically effective dose of ACT-774312: A novel CRTH2 antagonist. Basic Clin Pharmacol Toxicol. 2019;124(6):711-721. [Content Brief]

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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.

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Biological Activity
- Description
- In Vitro
Chemical Information
Purity & Documentation
References

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ACT-774312

All Prostaglandin Receptor Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

ACT-774312 Related Classifications

HY-182637 Related Classifications