J-113863|cas:353791-85-2|西域试剂

J-113863,97.30%

产品编号：Bellancom-103360| CAS NO：353791-85-2| 分子式：C₃₀H₃₇Cl₂IN₂O₂| 分子量：655.44

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货号	价格	库存与货期
Bellancom-103360	￥1600.00	杭州北京（现货）
Bellancom-103360	￥2100.00	杭州北京（现货）
Bellancom-103360	￥6800.00	杭州北京（现货）
Bellancom-103360	￥10500.00	杭州北京（现货）

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J-113863

产品介绍

J-113863 是一种有效的选择性的 CCR1 拮抗剂，对人和小鼠 CCR1 受体的 IC₅₀ 值分别为 0.9 nM 和 5.8 nM。J-113863 是人 CCR3 的强效拮抗剂 (IC₅₀ 为 0.58 nM)，还是小鼠 CCR3 的弱效拮抗剂 (IC₅₀ 为 460 nM)。J-113863 对 CCR2，CCR4 和 CCR5 以及 LTB4 或 TNF-α 受体没有活性。抗炎作用。

生物活性

J-113863 is a potent and selective CCR1 antagonist with IC₅₀ values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively. J-113863 is also a potent antagonist of the human CCR3 (IC₅₀ of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC₅₀ of 460 nM). J-113863 is inactive against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect.

体外研究

Modified Vaccinia virus Ankara (MVA) but not MVA and vaccinia virus (VACV) infected MH-S cells increase the expression of the CXCR2 acting chemokine CXCL2. MH-S cells constitutively produce CCL2 and CCR1 acting chemokines CCL3, CCL5 and CCL9. Consequently, supernatants of mock treated and virus infected MH-S cells induce chemotaxis of murine promyelocyte MPRO cells and human monocytic THP-1 cells at the same level. However, supernatants of MVA infected MH-S cells significantly increase chemotaxis of the CCR2 deficient human monocytic cell line U-937. Chemotaxis of all above cell types is inhibited by J-113863.

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

体内研究

J-113863 (3-10 mg/kg; intraperitoneal injection; once daily; for 11 days; DBA-1 male mice) treatment improves paw inflammation and joint damage, and dramatically decreases cell infiltration into joints in arthritic mice.

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

Animal Model:	DBA-1 male mice (10-12 weeks) induced with Collagen
Dosage:	3 mg/kg, 10 mg/kg
Administration:	Intraperitoneal injection; once daily; for 11 days
Result:	Improved paw inflammation and joint damage, and dramatically decreased cell infiltration into joints.

体内研究

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

Animal Model:	DBA-1 male mice (10-12 weeks) induced with Collagen
Dosage:	3 mg/kg, 10 mg/kg
Administration:	Intraperitoneal injection; once daily; for 11 days
Result:	Improved paw inflammation and joint damage, and dramatically decreased cell infiltration into joints.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (76.28 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5257 mL	7.6285 mL	15.2569 mL
5 mM	0.3051 mL	1.5257 mL	3.0514 mL
10 mM	0.1526 mL	0.7628 mL	1.5257 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 (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。

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: ≥ 2.5 mg/mL (3.81 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (3.81 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (3.81 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (3.81 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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