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Cat. No.: HY-135773

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CRTh2 antagonist 3

CRTh2 antagonist 3 is a potent chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2) antagonist. CRTh2 antagonist 3 enhances the activity of PDK1 toward a short peptide substrate, with an EC₅₀ of 2 μM and a K_d of 8.4 μM. CRTh2 antagonist 3 has the potential for cardiovascular inflammation.

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

CAS No.: 312928-72-6
Formula: C₁₉H₂₀N₂O₃S
Molecular Weight:356.44

Storage:

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

Data Sheet (269 KB)

CRTh2 antagonist 3 Chemical Structure

CAS No.: 312928-72-6

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Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

CRTh2 antagonist 3 is a potent chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2) antagonist^[1]. CRTh2 antagonist 3 enhances the activity of PDK1 toward a short peptide substrate, with an EC₅₀ of 2 μM and a K_d of 8.4 μM. CRTh2 antagonist 3 has the potential for cardiovascular inflammation^[2].

IC₅₀ & Target

CRTh2^[1]
EC50: 2 μM (PDK1)^[2]
Ki: 8.4 μM (PDK1)^[2]

All Prostaglandin Receptor Isoforms :

In Vitro

CRTh2 antagonist 3 (compound 4) is a small-molecule allosteric modulator of the protein kinase PDK1 from structure-based docking. CRTh2 antagonist 3 is 5-fold more potent than its parent compound^[2].

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

Chemical Information

CAS No. 312928-72-6
Molecular Weight 356.44
Formula C₁₉H₂₀N₂O₃S
SMILES

O=C(O)CN1C2=CC=CC=C2N=C1SCCOC3=C(C)C=CC=C3C
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (269 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)
Handling Instructions (2659 KB)

References

[1]. Heinz Fretz, et al. 2-sulfanyl-benzoimidazol-1-yi-acetic acid derivatives as CRTH2 antagonists. US8273740B2.

[2]. Rettenmaier TJ, et al. Small-Molecule Allosteric Modulators of the Protein Kinase PDK1 from Structure-Based Docking. J Med Chem. 2015 Oct 22;58(20):8285-8291. [Content Brief]

Calculators

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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.

Keywords

100 mg

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