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

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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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 529 In-stock
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10 mM * 1 mL in DMSO USD 529 In-stock
Solid
1 mg USD 180 In-stock
5 mg USD 450 In-stock
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Based on 1 publication(s) in Google Scholar

ACT-660602 Related Antibodies

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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].

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

ACT-660602 Related Antibodies

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

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

SMILES

FC(C1=NC=C(C2=C(N3C[C@@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

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 110 mg/mL (205.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8710 mL 9.3549 mL 18.7098 mL
5 mM 0.3742 mL 1.8710 mL 3.7420 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8710 mL 9.3549 mL 18.7098 mL 46.7744 mL
5 mM 0.3742 mL 1.8710 mL 3.7420 mL 9.3549 mL
10 mM 0.1871 mL 0.9355 mL 1.8710 mL 4.6774 mL
15 mM 0.1247 mL 0.6237 mL 1.2473 mL 3.1183 mL
20 mM 0.0935 mL 0.4677 mL 0.9355 mL 2.3387 mL
25 mM 0.0748 mL 0.3742 mL 0.7484 mL 1.8710 mL
30 mM 0.0624 mL 0.3118 mL 0.6237 mL 1.5591 mL
40 mM 0.0468 mL 0.2339 mL 0.4677 mL 1.1694 mL
50 mM 0.0374 mL 0.1871 mL 0.3742 mL 0.9355 mL
60 mM 0.0312 mL 0.1559 mL 0.3118 mL 0.7796 mL
80 mM 0.0234 mL 0.1169 mL 0.2339 mL 0.5847 mL
100 mM 0.0187 mL 0.0935 mL 0.1871 mL 0.4677 mL
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ACT-660602 Related Classifications

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-6606021646267-59-5ACT660602ACT 660602CXCRCXC chemokine receptorsC-X-C motif chemokine receptorsautoimmune diseasesT-cellacute lung ingury modelcell migrationselectivepiperazinyltriazolylethanone derivativesnon-competitive binding modeintrinsic metabolic clearanceClintG-protein-coupled receptorGPCRInhibitorinhibitorinhibit

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