1. GPCR/G Protein
    Immunology/Inflammation
  2. CXCR
  3. ACT-660602

ACT-660602 

Cat. No.: HY-151096
Handling Instructions

ACT-660602 is an orally active antagonist of chemokine receptor (CXCR3) with an IC50 value of 204 nM. ACT-660602 inhibits T-cell migration and shows efficacy in acute lung ingury model. ACT-660602 can be used for autoimmune diseases research.

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

ACT-660602 Chemical Structure

ACT-660602 Chemical Structure

CAS No. : 1646267-59-5

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Description

ACT-660602 is an orally active antagonist of chemokine receptor (CXCR3) with an IC50 value of 204 nM. ACT-660602 inhibits T-cell migration and shows efficacy in acute lung ingury model. ACT-660602 can be used for autoimmune diseases research[1][2].

IC50 & Target

CXCR3

204 nM (IC50)

In Vitro

ACT-660602 shows selectivity to CXCR3 over hERG, with IC50s of 18 μM (hERG)[1].
ACT-660602 (112 nM; 6 h) inhibits cell migration and improves the metabolic stability[1].
ACT-660602 (5, 20, 100 or 500 nM) displays an non-competitive binding mode to CXCL10 and CXCL11 in different concentration, with more stable IC50s[1].

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

Cell Migration Assay [1]

Cell Line: CD3/CD28-activated primary human T cells
Concentration: 112 nM
Incubation Time: 45 min
Result: Inhibited cell migration.
In Vivo

ACT-660602 (1 μM; 6 h) intrinsic metabolic clearance (CLint) in human, rat, mouse liver microsomes (HLM, RLM, MLM)[1].
ACT-660602 (30 mg/kg; p.o.; once daily) displays anti-inflammatory activity and exerts efficacy in the mouse model of acute lung ingury[1].
Range for Pharmacokinetics of ACT-660602[1]

Animal Route Dose (range) (mg/kg) Cmax (range) (ng/mL) Tmax (range) (h) AUC (range) (ng•h/mL) F (%) CL (range) (mL/min/kg) Vss (range) (L/kg) T1/2 (range) (h)
Dog p.o. 2 1380 1 20000 8 1.3 1.7 14.5
i.v. 0.5 1300-1450 0.5-2.0 10400-32000 / 0.6-3.0 1.6-1.7 6.3-
Rat p.o. 2 1520 0.5 14000 80 1.9 1.1 7.1
i.v. 0.5 1250-1860 0.5-1.0 11600-15641 / 1.9-1.9 0.9-1.3 5.7-8.8

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

Animal Model: LPS-induced lung inflammation model (72 h post LPS challenge)[1]
Dosage: 30 mg/kg
Administration: Oral gavage; once daily
Result: Significantly reduced recruitment of the CXCR3+ CD8+ T cell in the bronchoalveolar lavage compartment.
Molecular Weight

534.48

Formula

C20H20F6N8OS

CAS No.
SMILES

FC(C1=NC=C(C2=C(N3C[[email protected]@H](C)N(C(CN4N=C(C)N=C4C)=O)CC3)SC(C(F)(F)F)=N2)C=N1)(F)F

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
References
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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.

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ACT-660602
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HY-151096
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