10mM in DMSO pour les flux de travail chromatographiques et analytiques sensibles nécessitant une interférence de ligne de base minimale.
Store at -80°C Expédition Dry ice packs + Cold packs. Consultez le COA spécifique au lot pour les spécifications exactes.
SDS, COA, fiche technique et fiche de spécifications disponibles au téléchargement. COA spécifique au lot accessible via la recherche par numéro de lot.
Cité dans 0 publications à comité de lecture couvrant la chromatographie, la synthèse organique et les réactions de couplage croisé.
AZ084 is a potent, selective, allosteric and oral active CCR8 allosteric antagonist, with a K i of 0.9 nM. Has potential to treat asthma AZ084 restrains the formation of the immunologically tolerant pre-metastatic niche (PMN) and tumor cells metastasis in lung by downregulating Treg differentiation. AZ084 can be used in studies of asthma and cancer
In Vitro
AZ084 (5 μg/mL; single daily for 4 days) suppresses proportion of Tregs and reduces T cells that expresses CCR8 (co-cultured in vitro with LLC-exo MPF CM). ?\nAZ084 (0-10 μM) inhibits AML, DC and T cells with IC 50 s of 1.3, 4.6 and 5.7 nM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Splenic T cells Concentration: 5 μg/mL (single daily) Incubation Time: 4 days Result: Reversed the increased proportion of Tregs among the CD4+ T cells co-cultured in vitro with LLC-exo MPF CM. Reduced T cells that expressed CCR8 (cultured in vitro with by LLC-exo MPF CM). Cell Viability AssayCell Line: AML, DC and T cells Concentration: 0-10 µM Incubation Time: Result: Showed high potency with pronounced dose-response dependent inhibition of chemotaxis with an IC 50 of 1.3 nM in AML cells.
In Vivo
AZ084 (5 mg/kg; i.p.; every third day for 9 or 21 days) restrains the formation of the immunologically tolerant PMN and tumor cells metastasis in lung by downregulating Treg differentiation . ?\nAZ084 (434.57-869.14 mg/kg; i.v.; single) shows a bioavailability >70% in rats. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: C57BL/6 J mice (subcutaneous LLC tumor model) . Dosage: 5 mg/kg Administration: Intraperitoneal injection, every third day for 9 or 21 days. Result: Inhibited Treg differentiation and tumor cell colonization of the lungs and reduced the number of CD4+Foxp3+ Tregs in the lungs of LLC-exo pre-injected mice (every third day for 9 days). Inhibited the LLC-exo-induced LLC cell seeding in lung and also significantly reduced Treg accumulation in LLC-exo stimulated mouse lungs(every third day for 21 days). Animal Model: Female Balb/C mice, male Wistar rats and female Beagle dogs. Dosage: 434.57-869.14 mg/kg (in 0.9% NaCl) Administration: Intravenous injection, single. Result: 1.19 Pharmacokinetic Parameters of AZ084 in Female Balb/C mice, male Wistar rats and female Beagle dogs. IV (434.57-869.14 mg/kg) Dog plasma protein binding (% free) 45.7 Mu plasma protein binding (% free) 55.6 Hu plasma protein binding (% free) 31.0 Rat plasma protein binding (% free) 47.0 Rat HW plasma PK CL (mL/min/kg) 15.0 Rat HW plasma PK V ss (L/kg) 6.0 Rat HW plasma PK T 1/2 (h) 5.4 Rat HW plasma PK C max (µM) 0.5 Rat HW plasma PK bioavailability (%) 68.0
IC50& Target:CCR8 0.9 nM (Ki)
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