2. GPCR/G Protein Immunology/Inflammation
  3. CXCR
  4. ACT-660602

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。

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ACT-660602 Chemical Structure

ACT-660602 Chemical Structure

CAS No. : 1646267-59-5

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥5291
In-stock
1 mg ￥2045
In-stock
5 mg ￥4500
In-stock
10 mg 现货 询价
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Customer Review

ACT-660602 相关抗体

Top Publications Citing Use of Products

查看 CXCR 亚型特异性产品:

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CXCR CXCR1 CXCR2 CXCR3 CXCR4 CXCR7 CXCR6

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1][2].

IC50 & Target

CXCR3

204 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
T-cell IC50
37 nM
Compound: 9j; ACT-660602
Inhibition of cell migration in human T cell in presence of CXCL11 as agonist by imaging method
Inhibition of cell migration in human T cell in presence of CXCL11 as agonist by imaging method
[PMID: 35947786]
体外研究
(In Vitro)

ACT-660602 shows selectivity to CXCR3 over hERG, with IC50s of 18 μM (hERG)[1].
ACT-660602 (112 nM; 6 h) inhibits cell migration and improves the metabolic stability[1].
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[1].

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

ACT-660602 相关抗体:

Cell Migration Assay [1]

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)[1].
ACT-660602 (30 mg/kg; p.o.; once daily) displays anti-inflammatory activity and exerts efficacy in the mouse model of acute lung ingury[1].
Range for Pharmacokinetics of ACT-660602[1]

Animal Route Dose (range) (mg/kg) Cmax (range) (ng/mL) Tmax (range) (h) AUC (range) (ng•h/mL) F (%) CL (range) (mL/min/kg) Vss (range) (L/kg) T1/2 (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

MCE 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)[1]
Dosage: 30 mg/kg
Administration: Oral gavage; once daily
Result: Significantly reduced recruitment of the CXCR3+ CD8+ T cell in the bronchoalveolar lavage compartment.
分子量

534.48

Formula

C20H20F6N8OS
CAS 号
性状

固体

颜色

White to off-white

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)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 110 mg/mL (205.81 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

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
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

ACT-660602 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8710 mL 9.3549 mL 18.7098 mL 46.7744 mL
5 mM 0.3742 mL 1.8710 mL 3.7420 mL 9.3549 mL
10 mM 0.1871 mL 0.9355 mL 1.8710 mL 4.6774 mL
15 mM 0.1247 mL 0.6237 mL 1.2473 mL 3.1183 mL
20 mM 0.0935 mL 0.4677 mL 0.9355 mL 2.3387 mL
25 mM 0.0748 mL 0.3742 mL 0.7484 mL 1.8710 mL
30 mM 0.0624 mL 0.3118 mL 0.6237 mL 1.5591 mL
40 mM 0.0468 mL 0.2339 mL 0.4677 mL 1.1694 mL
50 mM 0.0374 mL 0.1871 mL 0.3742 mL 0.9355 mL
60 mM 0.0312 mL 0.1559 mL 0.3118 mL 0.7796 mL
80 mM 0.0234 mL 0.1169 mL 0.2339 mL 0.5847 mL
100 mM 0.0187 mL 0.0935 mL 0.1871 mL 0.4677 mL
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:

ACT-6606021646267-59-5ACT660602ACT 660602CXCRCXC chemokine receptorsC-X-C motif chemokine receptorsautoimmune diseasesT-cellacute lung ingury modelcell migrationselectivepiperazinyltriazolylethanone derivativesnon-competitive binding modeintrinsic metabolic clearanceClintG-protein-coupled receptorGPCRInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-151096
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