ACT-774312

Cat. No.: HY-182637: Data Sheet Handling Instructions
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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.

ACT-774312 Chemical Structure

CAS No. : 1809863-68-0

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Biological Activity
Purity & Documentation
References
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Description

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 %

Molecular Weight

389.81

Formula

C₁₈H₁₇ClFN₅O₂

CAS No.

1809863-68-0

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.

[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.

ACT-774312 Related Classifications

Inflammation/Immunology

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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:

ACT-7743121809863-68-0ACT774312ACT 774312Prostaglandin Receptorhuman liver microsomesDP1 receptordog liver microsomesCRTH2 receptorcytochrome P450 enzymeeosinophilhERG channelrat liver microsomesPGD2pregnane X receptorInhibitorinhibitorinhibit

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