CCR8 antagonist 2

发表于2023年11月24日由上海金畔生物科技有限公司

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。

CCR8 antagonist 2

CCR8 antagonist 2 是一种有效的 CCR8 拮抗剂。CCR8 (C-C Motif 趋化因子受体 8) 主要在 Treg 细胞和 Th2 细胞上表达，但不在 Th1 细胞上表达。CCR8 antagonist 2 抑制 CCR8 活性，可用于治疗由 CCR8 介导的疾病，如癌症和/或神经性疼痛 (摘自专利 WO2022000443A1，化合物 220)。

CCR8 antagonist 2 Chemical Structure

CAS No. : 2756350-98-6

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生物活性	CCR8 antagonist 2 is a potent antagonist of CCR8. CCR8 (C-C Motif Chemokine Receptor 8) is predominantly expressed on Treg cells and Th2 cells, but not on Th1 cells. CCR8 antagonist 2 inhibits CCR8 activity, which may be used in the treatment of diseases mediated by CCR8, such as cancer, and/or neuropathic pain (extracted from patent WO2022000443A1, compound 220)^[1].
分子量	464.02
Formula	C₂₃H₃₀ClN₃O₃S
CAS 号	2756350-98-6
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Guohuang FAN, et al. Methods and compositions for targeting tregs using ccr8 inhibitors.

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CCR8 antagonist 2

发表于2023年11月24日由上海金畔生物科技有限公司

CCR8 antagonist 2

CCR8 antagonist 2 Chemical Structure

CAS No. : 2756350-98-6

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100 mg		询价
250 mg		询价
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生物活性	CCR8 antagonist 2 is a potent antagonist of CCR8. CCR8 (C-C Motif Chemokine Receptor 8) is predominantly expressed on Treg cells and Th2 cells, but not on Th1 cells. CCR8 antagonist 2 inhibits CCR8 activity, which may be used in the treatment of diseases mediated by CCR8, such as cancer, and/or neuropathic pain (extracted from patent WO2022000443A1, compound 220)^[1].
分子量	464.02
Formula	C₂₃H₃₀ClN₃O₃S
CAS 号	2756350-98-6
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Guohuang FAN, et al. Methods and compositions for targeting tregs using ccr8 inhibitors.

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CCR8 antagonist 2

发表于2023年11月24日由上海金畔生物科技有限公司

CCR8 antagonist 2

CCR8 antagonist 2 Chemical Structure

CAS No. : 2756350-98-6

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100 mg		询价
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生物活性	CCR8 antagonist 2 is a potent antagonist of CCR8. CCR8 (C-C Motif Chemokine Receptor 8) is predominantly expressed on Treg cells and Th2 cells, but not on Th1 cells. CCR8 antagonist 2 inhibits CCR8 activity, which may be used in the treatment of diseases mediated by CCR8, such as cancer, and/or neuropathic pain (extracted from patent WO2022000443A1, compound 220)^[1].
分子量	464.02
Formula	C₂₃H₃₀ClN₃O₃S
CAS 号	2756350-98-6
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Guohuang FAN, et al. Methods and compositions for targeting tregs using ccr8 inhibitors.

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CCR4 antagonist 3 hydrochloride

发表于2023年11月5日由上海金畔生物科技有限公司

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 Chemical Structure

CAS No. : 2174938-71-5

规格	价格	是否有货
5 mg	￥11500	In-stock
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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 iT_reg cells with an IC₅₀ of 39 nM, while the IC₅₀ in human iT_reg 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 (V_ss=5.2 L/kg), a T_1/2 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 (V_ss=5.2 L/kg), a T_1/2 of 6.9 h, and good bioavailability (%F = 29) of oral dosing in mouse.

Formula

C₂₄H₂₇C_l2N₇O.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.

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CCR7 Ligand 1(Synonyms: CCR7-Cmp2105)

发表于2023年10月28日由上海金畔生物科技有限公司

CCR7 Ligand 1 (Synonyms: CCR7-Cmp2105) 纯度: 99.64%

CCR7 Ligand 1 (CCR7-Cmp2105) 是人 CC 趋化因子受体 7 (CCR7) 的变构配体，也是有效的 CCR7 拮抗剂，K_d 值为 3 nM。CCR7 Ligand 1 是一种噻二唑-二氧化物配体，可抑制蛋白与 CCL19 激活反应结合，IC₅₀ 为 7.3 μM。

CCR7 Ligand 1 Chemical Structure

CAS No. : 681514-83-0

规格	价格	是否有货
5 mg	￥5950	In-stock
10 mg	￥9500	In-stock
50 mg	￥29500	In-stock
100 mg		询价
200 mg		询价

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CCR7 Ligand 1 相关产品

•相关化合物库:

Bioactive Compound Library Plus
GPCR/G Protein Compound Library
Immunology/Inflammation Compound Library
Anti-Cancer Compound Library
Small Molecule Immuno-Oncology Compound Library
Targeted Diversity Library

生物活性

CCR7 Ligand 1 (CCR7-Cmp2105) is an allosteric Ligand and antagonist for human CC chemokine receptor 7 (CCR7) with a K_d of 3 nM. CCR7 Ligand 1, thiadiazole-dioxide ligan, suppresses arrestin binding in response to activation by CCL19 with an IC₅₀ of 7.3 μM^[1].

IC₅₀ & Target^[1]

Human CCR7

3 nM (Kd)

体外研究
(In Vitro)

CCR7 Ligand 1 (CCR7-Cmp2105) binds to a pocket at the intracellular part of CCR7 between the ends of TM1, TM2, TM3, and TM6 and the loop between TM7 and H8^[1].
CCR7 Ligand 1 allosterically inhibits binding of the native chemokine CCL19 ligand in scintillation proximity assays (bottom) with an IC50 of 35 nM^[1].
CCR7 Ligand 1 (20, 40, 60, 80, 100 μM) has dose-dependent thermo-stabilizing effect on CCR7^[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.

分子量

475.56

Formula

C₂₂H₂₉N₅O₅S

CAS 号

681514-83-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据

In Vitro:

DMSO : 100 mg/mL (210.28 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1028 mL	10.5139 mL	21.0278 mL
5 mM	0.4206 mL	2.1028 mL	4.2056 mL
10 mM	0.2103 mL	1.0514 mL	2.1028 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 (stored under nitrogen)。-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。

参考文献

[1]. Jaeger K, et al. Structural Basis for Allosteric Ligand Recognition in the Human CC Chemokine Receptor 7. Cell. 2019 Aug 22;178(5):1222-1230.e10.

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CCR4 antagonist 3

发表于2023年8月28日由上海金畔生物科技有限公司

CCR4 antagonist 3

CCR4 antagonist 3 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 Chemical Structure

CAS No. : 2174938-70-4

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100 mg		询价
250 mg		询价
500 mg		询价

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CCR4 antagonist 3 的其他形式现货产品:

CCR4 antagonist 3 hydrochloride

生物活性

CCR4 antagonist 3 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^[1]

CCR4

体外研究
(In Vitro)

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Shanghai Jinpan Biotech Co Ltd 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 (V_ss=5.2 L/kg), a T_1/2 of 6.9 h, and good bioavailability (%F = 29) of oral dosing in mouse.

分子量

500.42

Formula

C₂₄H₂₇Cl₂N₇O

CAS 号

2174938-70-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

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.

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CCR4 antagonist 2

发表于2023年7月18日由上海金畔生物科技有限公司

CCR4 antagonist 2

CCR4 antagonist 2 (Compound 31) 是一种新的有效，口服生物可利用的趋化因子受体 4 (CCR4) 的小分子拮抗剂，其抑制T_reg 贩运进入肿瘤微环境而不影响健康组织中 T_reg 的数量。 CCR4 antagonist 2 (Compound 31) 抑制 Ca²⁺ flux 和 CTX 的 IC₅₀ 值分别为 40 nM 和 70 nM。

CCR4 antagonist 2 Chemical Structure

CAS No. : 2206788-99-8

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100 mg		询价
250 mg		询价
500 mg		询价

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生物活性	CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits T_reg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues. CCR4 antagonist 2 (Compound 31) exhibits IC₅₀ values of Ca²⁺flux and (chemotaxis) CTX are 40 nM and 70 nM, respectively^[1].
IC₅₀ & Target	IC50: 40 nM (Ca²⁺flux); 70 nM (CTX) (CCR4 antagonist 2)^[1]
分子量	511.45
Formula	C₂₆H₂₈Cl₂N₆O
CAS 号	2206788-99-8
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Jackson JJ, et al. Discovery of a Potent and Selective CCR4 Antagonist That Inhibits Treg Trafficking into the Tumor Microenvironment. J Med Chem. 2019 Jul 11;62(13):6190-6213.

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CCR6 inhibitor 1

发表于2023年6月2日由上海金畔生物科技有限公司

CCR6 inhibitor 1 纯度: 99.87%

CCR6 inhibitor 1 是一种有效、选择性的 CCR6 抑制剂，对猴子和人 CCR6 的 IC₅₀ 值分别为 0.45 和 6 nM，对其选择性远高于人 CCR1 (IC₅₀，> 30000 nM) 和 CCR7 (IC₅₀，9400 nM)。CCR6 inhibitor 1 显著抑制 ERK 磷酸化。可用于自身免疫病和癌症的研究。

CCR6 inhibitor 1 Chemical Structure

CAS No. : 2437547-04-9

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥4995	In-stock
5 mg	￥4500	In-stock
10 mg	￥7500	In-stock
50 mg	￥19500	In-stock
100 mg	￥33000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

CCR6 inhibitor 1 相关产品

•相关化合物库:

Bioactive Compound Library Plus
GPCR/G Protein Compound Library
Immunology/Inflammation Compound Library
Anti-Cancer Compound Library
Small Molecule Immuno-Oncology Compound Library
Endocrinology Compound Library
Targeted Diversity Library

生物活性

CCR6 inhibitor 1 is a potent and selective CCR6 inhibitor, with IC₅₀s of 0.45 and 6 nM for monkey and human CCR6, much more selective at CCR6 over human CCR1 (IC₅₀, > 30000 nM), and CCR7 (IC₅₀, 9400 nM). CCR6 inhibitor 1 markedly blocks ERK phosphorylation. CCR6 inhibitor 1 is used in the research of autoimmune diseases and cancer^[1].

IC₅₀ & Target^[1]

Moneky CCR6

0.45 nM (IC₅₀)

Human CCR6

6 nM (IC₅₀)

Human CCR7

9400 nM (IC₅₀)

体外研究
(In Vitro)

CCR6 inhibitor 1 (Compound 35) inhibits L20-induced human B cell migration^[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.

分子量

504.52

Formula

C₂₄H₂₃F₃N₄O₃S

CAS 号

2437547-04-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 125 mg/mL (247.76 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9821 mL	9.9104 mL	19.8208 mL
5 mM	0.3964 mL	1.9821 mL	3.9642 mL
10 mM	0.1982 mL	0.9910 mL	1.9821 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。-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。

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：

1.

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

Solubility: ≥ 2.08 mg/mL (4.12 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.12 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 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% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (4.12 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.12 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (4.12 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.12 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 20.8 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]. Tawaraishi T, et al. Identification of a novel series of potent and selective CCR6 inhibitors as biological probes. Bioorg Med Chem Lett. 2018 Oct 1;28(18):3067-3072.

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标签归档：ccr

CCR8 antagonist 2

CCR8 antagonist 2

CCR8 antagonist 2

CCR4 antagonist 3 hydrochloride

CCR4 antagonist 3 hydrochloride 相关产品

•相关化合物库:

CCR7 Ligand 1(Synonyms: CCR7-Cmp2105)

CCR7 Ligand 1 相关产品

•相关化合物库:

CCR4 antagonist 3

CCR4 antagonist 2

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