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239823

CXCR3 Agonist, PS372424

Name: CXCR3 Agonist, PS372424
Brand: MM

The CXCR3 Agonist, PS372424 controls the biological activity of CXCR3. This small molecule/inhibitor is primarily used for Cell Signaling applications.

Synonym(s):

CXCR3 Agonist, PS372424, (S)-N-((S)-1-((cyclohexylmethyl)amino)-5-guanidino-1-oxopentan-2-yl)-2-(4-oxo-4-phenylbutanoyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide, Chemokine (C-X-C motif) Receptor 3 Agonist

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About This Item

Empirical Formula (Hill Notation):

C₃₃H₄₄N₆O₄ · 3H₂O

CAS Number:

914291-61-5

Molecular Weight:

642.79

UNSPSC Code:

12352200

PubChem Substance ID:

12000484

Assay:

≥97% (HPLC)

Form:

powder

Storage condition:

OK to freeze, protect from light

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Properties

Quality Segment

100

assay

≥97% (HPLC)

form

powder

manufacturer/tradename

Calbiochem^®

drug control

Új pszichoaktív anyag / New psychoactive substance (Hungary), 78/2022. (XII. 28.) BM rendelet

storage condition

OK to freeze, protect from light

color

white

solubility

DMSO: 100 mg/mL

shipped in

wet ice

storage temp.

2-8°C

SMILES string

C1CCC(CC1)CNC(=O)C(CCCN=C(N)N)NC(=O)C2CC3=CC=CC=C3CN2C(=O)CCC(=O)C4=CC=CC=C4

Description

General description

A peptidomimetic derivative containing tetrahydroisoquinoline-arginine motif that aligns with a Pro-Arg motif of CXCL10. Acts as a highly specific agonist of human CXCR3 (EC₅₀ = 1.1 mM, competitive CXCL10 binding IC₅₀ = 42 nM). Does not affect murine CXCR3. Induces a long-lasting internalization of about 87% of cell-surface CXCR3 within 30 min. Effectively stimulates T-cell migration (~ 50 nM) and blocks the migration of activated T cells towards CXCL11, CXCL12, and CCL5. Also reduces the migration of activated T cells towards rheumatoid arthritis synovial fibroblasts (RASF). Shown to induce phosphorylation of ERK with similar potency and kinetics as CXCL11. Also shown to block CXCL11 induced migration of CD45+ cells to air pouches generated on humanized mice.

Packaging

Packaged under inert gas

Physical form

Supplied as a trifluoroacetate salt.

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

O′Boyle, G., et al. 2012, PNAS.109, 4598.
Stroke, I. L., et al. 2006, Biochem Biophys Res Comm.349, 221.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c