2. GPCR/G Protein Immunology/Inflammation
  3. CCR
  4. INCB 3284 dimesylate

INCB 3284 dimesylate 是一种有效的，选择性的人 CCR2 拮抗剂，能够抑制单核细胞趋化蛋白 1 与 hCCR2 结合，IC50 值为 3.7 nM。INCB 3284 dimesylate 可用于急性肝功能衰竭的研究。

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INCB 3284 dimesylate Chemical Structure

INCB 3284 dimesylate Chemical Structure

CAS No. : 887401-93-6

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INCB 3284 dimesylate 的其他形式现货产品:

Other Forms of INCB 3284 dimesylate:

INCB 3284 dimesylate 相关抗体

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CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

INCB 3284 dimesylate is a potent, selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2, with an IC50 of 3.7 nM. INCB 3284 dimesylate can be used in the research of acute liver failure.

IC50 & Target[1]

MCP-1-hCCR2

3.7 nM (IC50)

体外研究
(In Vitro)

INCB 3284 dimesylate is a pentent, selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2, with an IC50 of 3.7 nM. INCB 3284 also causes an IC50 of 4.7 nM in antagonism of chemotaxis activity, an IC50 of 84 μM in inhibition of the hERG potassium current. However, INCB 3284 has no effec on CCR1, CCR3, CCR5, CXCR3, and CXCR5, or additional GPCRs at a concentration of 1 μM. Moreover, INCB 3284 potently inhibits CCR2-mediated signaling events such as intracellular calcium mobilization and ERK phosphorylation with IC50 values of 6 and 2.6 nM, respectively[1].

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

INCB 3284 dimesylate 相关抗体:
体内研究
(In Vivo)

INCB 3284 (1 mg/kg/day, ip) reduces liver damage, and decreases microglia activation in AOM-treated mice via inhibition on CCR2. INCB 3284 also significantly reduces the pERK1/2 to tERK1/2 ratio, as well as G-protein signaling pathway activity and proinflammatory cytokine production in cortex lysates from mice administed with azoxymethane[2].

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

712.76

Formula

C28H39F3N4O10S2
CAS 号
性状

油状物

颜色

Colorless to light 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 : ≥ 83.3 mg/mL (116.87 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" 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 1.4030 mL 7.0150 mL 14.0300 mL
5 mM 0.2806 mL 1.4030 mL 2.8060 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
Animal Administration
[2]

Mice[2]
Male C57Bl/6 mice (20 to 25 g) are given free access to water and rodent chow and are housed in constant temperature, humidity, and 12 h light-dark cycling. Acute liver failure is induced via a single intraperitoneal (ip) injection of 100 mg/kg of azoxymethane (AOM). In parallel, systemic inhibition of CCR2 and CCR4 activity is accomplished via pretreatment with INCB 3284 (1 mg/kg/day ip) or C021 (1 mg/kg/day ip) for 3 days prior to injection of AOM. Following injection, mice are placed on heating pads adjusted to 37°C and monitored frequently for signs of neurological decline. To reduce the impacts of hypoglycemia and dehydration, cage floors are supplied with hydrogel and rodent chow and after 12 h, and every subsequent 4 h, mice are injected subcutaneously with 5% dextrose in 250 μL of saline. If mice undergo a 20% or greater weight loss they are removed from the study[2].

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

INCB 3284 dimesylate 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 1.4030 mL 7.0150 mL 14.0300 mL 35.0749 mL
5 mM 0.2806 mL 1.4030 mL 2.8060 mL 7.0150 mL
10 mM 0.1403 mL 0.7015 mL 1.4030 mL 3.5075 mL
15 mM 0.0935 mL 0.4677 mL 0.9353 mL 2.3383 mL
20 mM 0.0701 mL 0.3507 mL 0.7015 mL 1.7537 mL
25 mM 0.0561 mL 0.2806 mL 0.5612 mL 1.4030 mL
30 mM 0.0468 mL 0.2338 mL 0.4677 mL 1.1692 mL
40 mM 0.0351 mL 0.1754 mL 0.3507 mL 0.8769 mL
50 mM 0.0281 mL 0.1403 mL 0.2806 mL 0.7015 mL
60 mM 0.0234 mL 0.1169 mL 0.2338 mL 0.5846 mL
80 mM 0.0175 mL 0.0877 mL 0.1754 mL 0.4384 mL
100 mM 0.0140 mL 0.0701 mL 0.1403 mL 0.3507 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:

INCB 3284 dimesylate887401-93-6CCRCC chemokine receptorInhibitorinhibitorinhibit

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