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Referencia número: HY-133151

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CXCR6 antagonist 1

Name: CXCR6 antagonist 1
Brand: MedChemExpress
SKU: HY-133151
Price: 590.00 USD
Availability: InStock
Rating: 5 (1 reviews)

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.

Para uso exclusivo en investigación. No vendemos a pacientes.

No. CAS: 2579689-85-1
Fòrmula: C₂₇H₃₀F₃N₃O₄S
Peso molecular:549.61

Almacenamiento:

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

Data Sheet (273 KB)

CXCR6 antagonist 1 Chemical Structure

No. CAS: 2579689-85-1

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Pureza y Documentación
Referencias
Calculators
Help & FAQs
Classifications
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Actividad biológica

Descripciòn

IC₅₀ & Target

^[1]

CXCR6

Ver todos los productos específicos de isoformas CXCR :

Cellular Effect

Cell Line	Type	Value	Description	References
SK-HEP1	IC₅₀	2.1 μM Compound: 81	Inhibition of CXCR6-mediated cell invasion in human SKHEP1 cells after 72 hrs by transwell assay Inhibition of CXCR6-mediated cell invasion in human SKHEP1 cells after 72 hrs by transwell assay	[PMID: 31882297]

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.

Parmacokinetics

Species	Dose	Route	C_max	T_1/2	AUC	CL	V_dss
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.

Related Protocols :

Chemical Information

No. CAS 2579689-85-1
Peso molecular 549.61
Fòrmula C₂₇H₃₀F₃N₃O₄S
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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (273 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Peddibhotla S, et al. Discovery of small molecule antagonists of chemokine receptor CXCR6 that arrest tumor growth in SK-HEP-1 mouse xenografts as a model of hepatocellular carcinoma. Bioorg Med Chem Lett. 2020;30(4):126899. [Content Brief]

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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.

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