CID-1067700 ML282|cas:314042-01-8|西域试剂

CID-1067700 ML282,98.06%

产品编号：Bellancom-13452| CAS NO：314042-01-8| 分子式：C₁₈H₁₈N₂O₄S₂| 分子量：390.48

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-13452	￥880.00	杭州北京（现货）
Bellancom-13452	￥1400.00	杭州北京（现货）
Bellancom-13452	￥2600.00	杭州北京（现货）
Bellancom-13452	￥5000.00	杭州北京（现货）
Bellancom-13452	￥6000.00	杭州北京（现货）

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CID-1067700 ML282

产品介绍

CID-1067700 (ML282) 是 pan GTPase 抑制剂，可竞争性抑制大脑 7 (Rab7) 中的 Ras 相关蛋白，K_i 为 13 nM。

生物活性

CID-1067700 (ML282) is a pan GTPase inhibitor, and competitively inhibits Ras-related in brain 7 (Rab7) with a K_i of 13 nM.

体外研究

CID-1067700 (ML282) is a pan GTPase inhibitor, and competitively inhibits Rab7 with a K_i of 13 nM. CID-1067700 shows inhibitory activity against nucleotide binding by Rab7, with K_ds of 100 nM and 40 nM for BODIPY-GTP and BODIPY-GDP, respectively. With increasing concentration, CID-1067700 causes strong inhibition on binding of the BODIPY-linked nucleotides, with EC₅₀ values of 11.22 ± 1.34 nM for BODIPY-GTP and 20.96 ± 1.34 nM for BODIPY-GDP and calculated K_i values of 12.89 nM and 19.70 nM respectively. CID-1067700 (10 μM) has no effect on the rate of release of bound BODIPY-linked nucleotide by wild type Rab7 under equilibrium binding conditions. CID-1067700 (0-40 μM) inhibits Rab7 activity, NF-κB activation as well as AID induction in B cells. Furthermore, CID-1067700 binds Rab7 with a high affinity (EC₅₀: 10-20 nM), and blocks Class switch DNA recombination (CSR) in B cells via targeting Rab7.

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

体内研究

CID-1067700 (ML282; 16 mg/kg, i.p.) prevents disease development in lupus-prone mice by Rab7 inhibition, and reduces IgG-IC deposition in MRL/Fas^lpr/lpr mice. CID-1067700 also targets B cells and specifically impairs the CSR machinery in vivo.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 12.5 mg/mL (32.01 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5610 mL	12.8048 mL	25.6095 mL
5 mM	0.5122 mL	2.5610 mL	5.1219 mL
10 mM	0.2561 mL	1.2805 mL	2.5610 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：

——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 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.40 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