BRD3308|1550053-02-5|-陌孚医药/Medlife

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BRD3308

目录号: PL04907 纯度: ≥98%

CAS No. :1550053-02-5

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中文名称	BRD3308
英文名称	BRD3308
英文别名	BRD3308;RRJDFENBXIEAPD-UHFFFAOYSA-N;BDBM178100;BRD3308, >=98% (HPLC);4-acetamido-N-(2-amino-4-fluorophenyl)benzamide;CID 72734382;4-Acetylamino-N-(2-amino-4-fluorophenyl)-benzamide;BRD 3308;s8962;BB168411;D84119;4-Acetamido-N-(2-amino-4-fluorophenyl)benzamide
Cas No.	1550053-02-5
分子式	C₁₅H₁₄FN₃O₂
分子量	287.29
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	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。
生物活性	BRD3308 is a highly selective HDAC3 inhibitor with an IC 50 of 54 nM. BRD3308 is 23-fold selectivity for HDAC3 over HDAC1 (IC 50 of 1.26 μM) or HDAC2 (IC 50 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.
性状	Solid
IC50 & Target[1][2]	HDAC3 54 nM (IC50) HDAC3 29 nM (Ki)
体外研究(In Vitro)	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 Ki values of 5.1 μM, 6.3 μM and 29 nM, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.RT-PCR
体内研究(In Vivo)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
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
参考文献	[1]. Barton KM, et al. Selective HDAC inhibition for the disruption of latent HIV-1 infection. PLoS One. 2014 Aug 19;9(8):e102684. [2]. Lundh M, et al. Histone deacetylase 3 inhibition improves glycaemia and insulin secretion in obese diabetic rats. Diabetes Obes Metab. 2015 Jul;17(7):703-7. [3]. Wagner FF, et al. A

溶解度数据	In Vitro: DMSO : 250 mg/mL (870.20 mM; Need ultrasonic)配制储备液

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