2. GPCR/G Protein Immunology/Inflammation
  3. CXCR
  4. CXCR6 antagonist 1

CXCR6 antagonist 1 (Compound 81) is an orally active CXCR6 antagonist. CXCR6 antagonist 1 inhibits the CXCR6 receptor signaling pathway, including β-arrestin recruitment and Forskolin (HY-15371)-induced cAMP production. CXCR6 antagonist 1 reduces tumor growth in a mouse xenograft model of hepatocellular carcinoma. CXCR6 antagonist 1 can be used in research related to hepatocellular carcinoma.

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CXCR6 antagonist 1

CXCR6 antagonist 1 Chemical Structure

CAS No. : 2579689-85-1

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CXCR6 antagonist 1 Related Antibodies

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Description

CXCR6 antagonist 1 (Compound 81) is an orally active CXCR6 antagonist. CXCR6 antagonist 1 inhibits the CXCR6 receptor signaling pathway, including β-arrestin recruitment and Forskolin (HY-15371)-induced cAMP production. CXCR6 antagonist 1 reduces tumor growth in a mouse xenograft model of hepatocellular carcinoma. CXCR6 antagonist 1 can be used in research related to hepatocellular carcinoma[1].

IC50 & Target[1]

CXCR6

 

In Vitro

CXCR6 antagonist 1 potently inhibits CXCL16-induced β-arrestin recruitment in CXCR6-expressing DiscoveRx cells, with an IC50 of 40 nM[1].
CXCR6 antagonist 1 inhibits Forskolin (HY-15371)-induced cAMP signaling pathway in CXCR6-expressing DiscoveRx cells, with an IC50 of 540 nM[1].
CXCR6 antagonist 1 (72 h) inhibits the migration of hepatocellular carcinoma cell line SK-HEP-1 in a dose-dependent manner, with an IC50 of 2.1 μM[1].

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

CXCR6 antagonist 1 Related Antibodies
Parmacokinetics
Species Dose Route Cmax T1/2 AUC CL Vdss
Mice[1] 5 mg/kg i.v. / 1.58 h / 28.4 mL/min/kg 3.32 L/kg
Mice[1] 10 mg/kg p.o. 798 ng/mL 2.82 h 2047 ng·h/mL / /
In Vivo

CXCR6 antagonist 1 (30-60 mg/kg; p.o.; daily; from day 4 to day 30) significantly reduces the tumor weight of SK-HEP-1 hepatocellular carcinoma in female NOD/SCID mice[1].

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

Animal Model: NOD/SCID (female)[1]
Dosage: 30 mg/kg; 60 mg/kg
Administration: p.o.; daily; Day 4 to Day 30
Result: Reduced mean excised tumor weight to 59 ± 9 mg (30 mg/kg dose) and 55 ± 24 mg (60 mg/kg dose), with both doses showing significant reduction relative to vehicle control (P < 0.05).
Achieved tumor growth inhibition comparable to positive control cyclophosphamide.
Caused no deaths, behavioral phenotypes, or distinct body weight differences relative to control.
Molecular Weight

549.61

Formula

C27H30F3N3O4S
CAS No.
SMILES

C(N1[C@@]2(C[C@H](NC(=O)C3=CC(OC)=C(OC)C(OC)=C3)C[C@]1(CCC2)[H])[H])C4=NC=5C(S4)=CC=CC5C(F)(F)F
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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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CXCR6 antagonist 1 Related Classifications

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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:

CXCR6 antagonist 12579689-85-1CXCRCXC chemokine receptorsC-X-C motif chemokine receptorsβ-arrestin recruitmentforskolin-induced cAMP productioncyclophosphamidehuman CXCR6 receptorDiscoveRx cellsfemale NOD/SCID micehepatocellular carcinomamouse xenograft modelCXCL16SK-HEP-1 human hepatoma cellInhibitorinhibitorinhibit

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CXCR6 antagonist 1
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