CCR4-351 hydrochloride|cas:2174938-71-5|西域试剂

CCR4-351 hydrochloride,98.59%

产品编号：Bellancom-131349A| CAS NO：2174938-71-5| 分子式：C₂₄H₂₈Cl₃N₇O

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-131349A		￥11500.00	杭州北京（现货）

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CCR4-351 hydrochloride

产品介绍

CCR4-351 hydrochloride 是口服有效和选择性的 CCR4 拮抗剂。CCR4-351 hydrochloride 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 hydrochloride 具有抗肿瘤活性。

生物活性

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

体外研究

CCR4-351 (compound 38) hydrochloride shows no activity in a CYP450 induction assay.
CCR4-351 hydrochloride inhibits the migration of mouse iT_reg cells with an IC₅₀ of 39 nM, while the IC₅₀ in human iT_reg cells is 33 nM.

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

体内研究

CCR4-351 (compound 38; 50 mg/kg; PO; daily; for 40 days) hydrochloride significantly reduces the tumor growth.
CCR4-351 (0.5 mg/kg; IV) hydrochloride has low clearance (CL=10.2 mL/min/kg), medium volume of distribution (V_ss=5.2 L/kg), a T_1/2 of 6.9 h, and good bioavailability (%F = 29) of oral dosing in mouse.
CCR4-351 hydrochloride has low clearance (CL=7.3 mL/min/kg), a half-life of 12.7 hr, and is 44% bioavailable in dog. CCR4-351 hydrochloride 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.

西域 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
Dosage:	50 mg/kg
Administration:	PO; daily; for 40 days
Result:	Significantly reduced the tumor growth.

Animal Model:	Rat and mouse
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 (V_ss=5.2 L/kg), a T_1/2 of 6.9 h, and good bioavailability (%F = 29) of oral dosing in mouse.

体内研究

西域 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
Dosage:	50 mg/kg
Administration:	PO; daily; for 40 days
Result:	Significantly reduced the tumor growth.

Animal Model:	Rat and mouse
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 (V_ss=5.2 L/kg), a T_1/2 of 6.9 h, and good bioavailability (%F = 29) of oral dosing in mouse.

性状

Solid

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。