2. GPCR/G Protein Immunology/Inflammation
  3. CCR
  4. CCR4-351

CCR4-351 是口服有效和选择性的 CCR4 拮抗剂。CCR4-351 具有新颖的哌啶基-氮杂环丁烷基序，在钙流量和 CTX 分析中的 IC50 为 22 nM 和 50 nM。CCR4-351 具有抗肿瘤活性。

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CCR4-351 Chemical Structure

CCR4-351 Chemical Structure

CAS No. : 2174938-70-4

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥25321
In-stock
1 mg ￥4600
In-stock
5 mg   询价  
10 mg   询价  

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Customer Review

Other Forms of CCR4-351:

CCR4-351 相关抗体

Top Publications Citing Use of Products

查看 CCR 亚型特异性产品:

查看所有亚型
CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CCR4-351 is an orally active, potent and selective CCR4 antagonist. CCR4-351, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4-351 has antitumor activity[1].

IC50 & Target[1]

CCR4

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CCRF-CEM IC50
50 nM
Compound: 38
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
[PMID: 32667798]
CCRF-CEM IC50
64 nM
Compound: 38
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL17-mediated chemotaxis preincubated for 30 mins followed by CCL17 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL17-mediated chemotaxis preincubated for 30 mins followed by CCL17 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
[PMID: 32667798]
体外研究
(In Vitro)

CCR4-351 (化合物 38) 在 CYP450 诱导试验中没有活性[1]。
CCR4-351抑制小鼠和人的 iTreg细胞的迁移，IC50为39 nM 和 33 nM[1]。

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

CCR4-351 相关抗体:
体内研究
(In Vivo)

CCR4-351 (化合物 38；50 mg/kg；每天口服；持续 40 天) 显著减少肿瘤生长[1]。
CCR4-351 (0.5 mg/kg；IV) 具有低清除率 (CL=10.2 mL/min/kg)，中等分布容积 (Vss=5.2 L/kg)，T1/2 为 6.9 小时，小鼠口服给药具有良好的生物利用度 (%F=29)[1]。
CCR4-351 具有低清除率 (CL=7.3 mL/min/kg)，半衰期为 12.7 小时，在狗体内的生物利用度为 44%。CCR4-351 在食蟹猴中具有低清除率 (CL=3.7 mL/min/kg)、长终末半衰期 (10.7 hr) 和良好的生物利用度 (%F=41)[1]。

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

Animal Model: Six-to eight-week-old, female C57BL/6 mice with Pan02-OVA tumor[1]
Dosage: 50 mg/kg
Administration: PO; daily; for 40 days
Result: Significantly reduced the tumor growth.
Animal Model: Rat and mouse[1]
Dosage: 0.5 mg/kg of IV; 2 mg/kg of PO
Administration: IV or PO
Result: Possessed medium clearance (CL=47.6 mL/min/kg) and was 49% bioavailable upon oral dosing in rat.
Had low clearance (CL=10.2 mL/min/kg), medium volume of distribution (Vss=5.2 L/kg), a T1/2 of 6.9 h, and good bioavailability (%F = 29) of oral dosing in mouse.
分子量

500.42

Formula

C24H27Cl2N7O
CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 190 mg/mL (379.68 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 1.9983 mL 9.9916 mL 19.9832 mL
5 mM 0.3997 mL 1.9983 mL 3.9966 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)。-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

CCR4-351 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)。-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 1.9983 mL 9.9916 mL 19.9832 mL 49.9580 mL
5 mM 0.3997 mL 1.9983 mL 3.9966 mL 9.9916 mL
10 mM 0.1998 mL 0.9992 mL 1.9983 mL 4.9958 mL
15 mM 0.1332 mL 0.6661 mL 1.3322 mL 3.3305 mL
20 mM 0.0999 mL 0.4996 mL 0.9992 mL 2.4979 mL
25 mM 0.0799 mL 0.3997 mL 0.7993 mL 1.9983 mL
30 mM 0.0666 mL 0.3331 mL 0.6661 mL 1.6653 mL
40 mM 0.0500 mL 0.2498 mL 0.4996 mL 1.2490 mL
50 mM 0.0400 mL 0.1998 mL 0.3997 mL 0.9992 mL
60 mM 0.0333 mL 0.1665 mL 0.3331 mL 0.8326 mL
80 mM 0.0250 mL 0.1249 mL 0.2498 mL 0.6245 mL
100 mM 0.0200 mL 0.0999 mL 0.1998 mL 0.4996 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:

CCR4-3512174938-70-4CCRCC chemokine receptororallypiperidinyl-azetidinemotifantitumorCYP450Inhibitorinhibitorinhibit

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产品名称：
CCR4-351
目录号：
HY-131349
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