BRD3308 - CAS:1550053-02-5

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BRD3308

目录号 : KM11682 CAS No. : 1550053-02-5 纯度 : 98%

Data Sheet 产品使用指南

BRD3308 是一种高选择性的 HDAC3 抑制剂，IC₅₀ 为 54 nM。BRD3308 对 HDAC3 的选择性是 HDAC1 (IC₅₀ 为 1.26 μM) 或 HDAC2 (IC₅₀ 为 1.34 μM) 的 23 倍。BRD3308 抑制由炎性细胞因子或糖脂毒性应激诱导的胰腺 β 细胞凋亡，并增加功能性胰岛素释放。BRD3308 还可激活 HIV-1 转录并破坏 HIV-1 潜伏期。

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生物活性

BRD3308 is a highly selective HDAC3 inhibitor with an IC₅₀ of 54 nM. BRD3308 is 23-fold selectivity for HDAC3 over HDAC1 (IC₅₀ of 1.26 μM) or HDAC2 (IC₅₀ of 1.34 μM). BRD3308 suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines or glucolipotoxic stress, and increases functional insulin release. BRD3308 activates HIV-1 transcription and disrupts HIV-1 latency.

体外研究

BRD3308 (5-30 µM; 6-24 hours) treatment increases HIV-1 expression in the 2D10 cell line.
BRD3308 (15 µM; overnight) is able to induce outgrowth of HIV-1 from latently infected cells ex vivo in resting CD4+ T cells. BRD3308 inhibits HDAC1, HDAC2 and HDAC3 with K_i values of 5.1 μM, 6.3 μM and 29 nM, respectively.

RT-PCR

Cell Line:	2D10 cells
Concentration:	5 µM, 10 µM, 15 µM, or 30 µM
Incubation Time:	6 hours, 12 hours, 18 hours, or 24 hours
Result:	An increase in HIV-1 expression was observed.

体内研究

BRD3308 (5 mg/kg; intraperitoneal injection; every second day; male Zucker Diabetic Fatty rats) treatment reduces hyperglycaemia and increases insulin secretion in a rat model of type 2 diabetes. At the end of the hyperglycaemic clamp, circulating insulin levels are significantly higher in BRD3308-treated rats. Pancreatic insulin staining and contents are also significantly higher. BRD3308 preserves the functional β-cell mass against glucolipotoxicity in vivo.

Animal Model:	Male Zucker Diabetic Fatty (Obese) rats (6-week-old)
Dosage:	5 mg/kg
Administration:	Intraperitoneal injection; every second day
Result:	Reduced hyperglycaemia and increased insulin secretion in a rat model of type 2 diabetes.

分子式

C₁₅H₁₄FN₃O₂

分子量

287.29

CAS号

1550053-02-5

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 : 250 mg/mL (870.20 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.4808 mL	17.4040 mL	34.8080 mL
5 mM	0.6962 mL	3.4808 mL	6.9616 mL
10 mM	0.3481 mL	1.7404 mL	3.4808 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 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (7.24 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (7.24 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。
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (7.24 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (7.24 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。