产品
编 号：F524764
分子式：C26H34N4O2
分子量：434.57
分子式：C26H34N4O2
分子量：434.57
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
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5mg
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10mg
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询价
结构图
CAS No: 929300-19-6
产品详情
生物活性：
AZ084 is a potent, selective, allosteric and oral active CCR8 allosteric antagonist, with a Ki 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.
体内研究：
AZ084 (5 mg/kg；腹腔注射；每三天一次，持续 9 或 21 天) 通过下调 Treg 分化抑制免疫耐受 PMN 的形成和肿瘤细胞在肺部的转移。 AZ084 (434.57-869.14 mg/kg；静脉注射；single) 在大鼠中显示生物利用度 >70%。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:1.19Pharmacokinetic 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 Vss (L/kg)6.0
Rat HW plasma PK T1/2 (h)5.4
Rat HW plasma PK Cmax (μM)0.5
Rat HW plasma PK bioavailability (%)68.0
体外研究：
AZ084 (5 μg/mL；每天一次，持续 4 天) 抑制 Treg 的比例并减少表达 CCR8 的 T 细胞 (与 LLC-exo MPF CM 体外共培养)。AZ084 (0-10 μM) 抑制 AML、DC 和 T 细胞，IC50 分别为 1.3、4.6 和 5.7 nM。
AZ084 is a potent, selective, allosteric and oral active CCR8 allosteric antagonist, with a Ki 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.
体内研究：
AZ084 (5 mg/kg；腹腔注射；每三天一次，持续 9 或 21 天) 通过下调 Treg 分化抑制免疫耐受 PMN 的形成和肿瘤细胞在肺部的转移。 AZ084 (434.57-869.14 mg/kg；静脉注射；single) 在大鼠中显示生物利用度 >70%。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:1.19Pharmacokinetic 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 Vss (L/kg)6.0
Rat HW plasma PK T1/2 (h)5.4
Rat HW plasma PK Cmax (μM)0.5
Rat HW plasma PK bioavailability (%)68.0
体外研究：
AZ084 (5 μg/mL；每天一次，持续 4 天) 抑制 Treg 的比例并减少表达 CCR8 的 T 细胞 (与 LLC-exo MPF CM 体外共培养)。AZ084 (0-10 μM) 抑制 AML、DC 和 T 细胞，IC50 分别为 1.3、4.6 和 5.7 nM。
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