BRD5529|cas:1358488-78-4|西域试剂

BRD5529,98.02%

产品编号：Bellancom-115497| CAS NO：1358488-78-4| 分子式：C₂₅H₃₁N₅O₄| 分子量：465.54

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-115497	￥1100.00	杭州北京（现货）
Bellancom-115497	￥1800.00	杭州北京（现货）
Bellancom-115497	￥3600.00	杭州北京（现货）
Bellancom-115497	￥5600.00	杭州北京（现货）
Bellancom-115497	￥8500.00	杭州北京（现货）

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BRD5529

产品介绍

BRD5529 是一种有效的剂量依赖性 CARD9-TRIM62 蛋白-蛋白相互作用 (PPI) 抑制剂，IC₅₀ 值为 8.6 μM。BRD5529 在体外对 CARD9 泛素化具有有效和完全的抑制作用，还具有良好的溶解性。BRD5529 可用于克罗恩病（CD）和溃疡性结肠炎（UC）等炎症性肠病（IBD）的研究。

生物活性

BRD5529 is an effective dose-dependent CARD9-TRIM62 protein–protein interaction (PPI) inhibitor with an IC₅₀ value of 8.6 μM. BRD5529 has potency and complete inhibition of CARD9 ubiquitinylation in vitro, also has favorable solubility. BRD5529 can be used for the research of inflammatory bowel disease (IBD) such as Crohn’s disease (CD) and ulcerative colitis (UC).

体外研究

BRD5529 has effective dose-dependent CARD9-TRIM62 inhibitory activity with an IC₅₀ value of 8.6 μM.
BRD5529 directly binds CARD9, but not TRIM62, and disrupt its ubiquitinylation in vitro.
BRD5529 (40 μM) produces dose-dependent inhibition of TRIM62-mediated CARD9 ubiquitinylation in vitro.
BRD5529 (200 μM, 0-50 min; 200μM, 2-4 h) inhibits CARD9-dependent signaling in innate immune cells.

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

Western Blot Analysis

Cell Line:	HEK293F cells
Concentration:	40 μM
Incubation Time:
Result:	Inhibited CARD9 ubiquitinylation reaction in vitro.

体内研究
(In Vivo)

BRD5529 (i.p.; 0.1 or 1.0 mg/kg; daily, for 2 weeks) displays no inherent safety concerns in initial general safety and toxicology assessments.

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

Animal Model:	Pneumocystis pneumonia (PCP) model
Dosage:	0.1 or 1.0 mg/kg
Administration:	intraperitoneally (IP), daily, for 2 weeks
Result:	Resulted no significant changes in daily or final weight gain and proinflammatory cytokines showed no major differences. Showed no significant change of lung, liver, and kidney in pathology scoring.

体内研究

BRD5529 (i.p.; 0.1 or 1.0 mg/kg; daily, for 2 weeks) displays no inherent safety concerns in initial general safety and toxicology assessments.

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

Animal Model:	Pneumocystis pneumonia (PCP) model
Dosage:	0.1 or 1.0 mg/kg
Administration:	intraperitoneally (IP), daily, for 2 weeks
Result:	Resulted no significant changes in daily or final weight gain and proinflammatory cytokines showed no major differences. Showed no significant change of lung, liver, and kidney in pathology scoring.

体内研究

BRD5529 (i.p.; 0.1 or 1.0 mg/kg; daily, for 2 weeks) displays no inherent safety concerns in initial general safety and toxicology assessments.

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

Animal Model:	Pneumocystis pneumonia (PCP) model
Dosage:	0.1 or 1.0 mg/kg
Administration:	intraperitoneally (IP), daily, for 2 weeks
Result:	Resulted no significant changes in daily or final weight gain and proinflammatory cytokines showed no major differences. Showed no significant change of lung, liver, and kidney in pathology scoring.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (268.51 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1480 mL	10.7402 mL	21.4804 mL
5 mM	0.4296 mL	2.1480 mL	4.2961 mL
10 mM	0.2148 mL	1.0740 mL	2.1480 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： 0.5% CMC-Na/saline water
Solubility: 20 mg/mL (42.96 mM); Suspended solution; Need ultrasonic
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.47 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.47 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
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.47 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.47 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
4.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.47 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.47 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。