CID-1067700 - CAS:314042-01-8

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CID-1067700 (Synonyms:ML282)

目录号 : KM8862 CAS No. : 314042-01-8 纯度 : 98%

Data Sheet 产品使用指南

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。

规格	价格	是否有货
5mg		In-stock
10mg		In-stock
50mg	询价	In-stock
100mg	询价	In-stock

加入购物车大包装询价

Other Forms of Rapamycin:

Kgp-IN-1 hydrochloride In-stock
Ginkgolide A In-stock
Ginkgetin In-stock
VKGILS-NH2 In-stock
7,3',4'-Tri-O-methylluteolin In-stock

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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.

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 mice. CID-1067700 also targets B cells and specifically impairs the CSR machinery in vivo.

分子式

C₁₈H₁₈N₂O₄S₂

分子量

390.48

CAS号

314042-01-8

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 : 75 mg/mL (192.07 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。