ACT-660602|cas:1646267-59-5|西域试剂

ACT-660602,99.86%

产品编号：Bellancom-151096| CAS NO：1646267-59-5| 分子式：C₂₀H₂₀F₆N₈OS| 分子量：534.48

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货号	价格	库存与货期
Bellancom-151096	￥4500.00	杭州北京（现货）
Bellancom-151096	￥7000.00	杭州北京（现货）
Bellancom-151096	￥14800.00	杭州北京（现货）

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ACT-660602

产品介绍

ACT-660602 是一种具有口服活性的趋化因子受体 CXCR3 拮抗剂， IC₅₀ 为 204 nM。ACT-660602 抑制 T 细胞迁移，并在体内急性肺损伤模型中表现出显著作用。ACT-660602 可用于自身免疫性疾病的研究。

生物活性

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.

体外研究

ACT-660602 shows selectivity to CXCR3 over hERG, with IC₅₀s of 18 μM (hERG).
ACT-660602 (112 nM; 6 h) inhibits cell migration and improves the metabolic stability.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Migration Assay

Cell Line:	CD3/CD28-activated primary human T cells
Concentration:	112 nM
Incubation Time:	45 min
Result:	Inhibited cell migration.

体内研究
(In Vivo)

ACT-660602 (1 μM; 6 h) intrinsic metabolic clearance (CLint) in human, rat, mouse liver microsomes (HLM, RLM, MLM).
ACT-660602 (30 mg/kg; p.o.; once daily) displays anti-inflammatory activity and exerts efficacy in the mouse model of acute lung ingury.
Range for Pharmacokinetics of ACT-660602

Animal	Route	Dose (range) (mg/kg)	C_max (range) (ng/mL)	T_max (range) (h)	AUC (range) (ng•h/mL)	F (%)	CL (range) (mL/min/kg)	V_ss (range) (L/kg)	T_1/2 (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

西域 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)
Dosage:	30 mg/kg
Administration:	Oral gavage; once daily
Result:	Significantly reduced recruitment of the CXCR3+ CD8+ T cell in the bronchoalveolar lavage compartment.

体内研究

Animal	Route	Dose (range) (mg/kg)	C_max (range) (ng/mL)	T_max (range) (h)	AUC (range) (ng•h/mL)	F (%)	CL (range) (mL/min/kg)	V_ss (range) (L/kg)	T_1/2 (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

西域 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)
Dosage:	30 mg/kg
Administration:	Oral gavage; once daily
Result:	Significantly reduced recruitment of the CXCR3+ CD8+ T cell in the bronchoalveolar lavage compartment.

体内研究

Animal	Route	Dose (range) (mg/kg)	C_max (range) (ng/mL)	T_max (range) (h)	AUC (range) (ng•h/mL)	F (%)	CL (range) (mL/min/kg)	V_ss (range) (L/kg)	T_1/2 (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

西域 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)
Dosage:	30 mg/kg
Administration:	Oral gavage; once daily
Result:	Significantly reduced recruitment of the CXCR3+ CD8+ T cell in the bronchoalveolar lavage compartment.

性状

Solid

溶解性数据

In Vitro:

DMSO : 110 mg/mL (205.81 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	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
10 mM	0.1871 mL	0.9355 mL	1.8710 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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)

参考文献