CCR4 antagonist 3 hydrochloride

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CCR4 antagonist 3 hydrochloride  纯度: 98.59%

CCR4 antagonist 3 hydrochloride 是口服有效和选择性的 CCR4 拮抗剂。CCR4 antagonist 3 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 antagonist 3 具有抗肿瘤活性。

CCR4 antagonist 3 hydrochloride

CCR4 antagonist 3 hydrochloride Chemical Structure

CAS No. : 2174938-71-5

规格 价格 是否有货 数量
5 mg ￥11500 In-stock
10 mg   询价  
50 mg   询价  

* Please select Quantity before adding items.

CCR4 antagonist 3 hydrochloride 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus

生物活性

CCR4 antagonist 3 hydrochloride is an orally active, potent and selective CCR4 antagonist. CCR4 antagonist 3, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4 antagonist 3 has antitumor activity[1].

IC50 & Target

CCR4

 

体外研究
(In Vitro)

CCR4 antagonist 3 (compound 38) shows no activity in a CYP450 induction assay[1].
CCR4 antagonist 3 inhibits the migration of mouse iTreg cells with an IC50 of 39 nM, while the IC50 in human iTreg cells is 33 nM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

CCR4 antagonist 3 (compound 38; 50 mg/kg; PO; daily; for 40 days) significantly reduces the tumor growth[1].
CCR4 antagonist 3 (0.5 mg/kg; IV) has 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[1].
CCR4 antagonist 3 has low clearance (CL=7.3 mL/min/kg), a half-life of 12.7 hr, and is 44% bioavailable in dog. CCR4 antagonist 3 has low clearance (CL=3.7 mL/min/kg), a long terminal half-life (10.7 hr), and good bioavailability (%F = 41) in cynomolgus monkey[1].

上海金畔生物科技有限公司 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.

Formula

C24H27Cl2N7O.xHCl
CAS 号

2174938-71-5
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
In Vitro: 

DMSO : 170 mg/mL (Need ultrasonic)

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 4.25 mg/mL (Infinity mM); Clear solution

    此方案可获得 ≥ 4.25 mg/mL (Infinity mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 42.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 4.25 mg/mL (Infinity mM); Clear solution

    此方案可获得 ≥ 4.25 mg/mL (Infinity mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 42.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Omar Robles, et al. Novel Piperidinyl-Azetidines as Potent and Selective CCR4 Antagonists Elicit Antitumor Response as Single Agent and in Combination with Checkpoint Inhibitors. J Med Chem. 2020 Jul 15.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务