化合物 T14831

生物活性靶点体外研究体内研究化合物 T14831 试剂级价格

化合物 T14831

CAS号:83314-01-6
英文名:BRYOSTATIN 1
中文名:化合物 T14831
CBNumber:CB9454936
分子式:C47H68O17
分子量:905.03
MOL File:83314-01-6.mol

化合物 T14831化学性质

熔点 :230-235°
比旋光度 :D25 +34.1° (c = 0.044 in methanol)
沸点 :716.44°C (rough estimate)
密度 :1.1245 (rough estimate)
折射率 :1.5940 (estimate)
储存条件 :-20°C
溶解度 :DMSO: soluble
酸度系数(pKa) :11.10±0.70(Predicted)
形态 :solid
颜色 :white
旋光性 (optical activity) :+34.125 (methanol)

安全信息

危险品标志 :Xn
危险类别码 :68
安全说明 :22-24/25-36/37
WGK Germany :3
RTECS号 :EH9455000
海关编码 :2932990090
毒性 :LD50 in mice, rats (mg/kg): 0.038, 0.068 i.v. (Prendiville)

化合物 T14831性质、用途与生产工艺

生物活性 Bryostatin 1 是一种天然的大环内酯类化合物，从苔藓虫 Bugula neritina 中分离出来，也是一种有效的中枢神经系统 (CNS) 渗透性的 PKC 调节剂。Bryostatin 1 以 Ki 值为 8.07 nM 和 0.45 nM 分别结合到分离的 Munc13-1 的 C1 域和全长的 Munc13-1 蛋白。Bryostatin 1 具有抗癌，抗炎，神经保护，抗 HIV-1 感染的特性。
靶点

PKC
HIV-1

体外研究

Bryostatin 1 (1 µM; 5 minutes; HT22 cells) treatment successfully recruits Munc13-1 from the cytosol to the plasma membrane. Effects of Bryostatin 1 on the other Munc13 family members, ubMunc13-2 and bMunc13-2, resembled those of Munc13-1 for translocation .
The increased level of expression of Munc13-1 following a 24 h incubation with Bryostatin 1 in both HT22 and primary mouse hippocampal cells is observed.
Bryostatin 1 can also affect the immune system by modulating dendritic cells (DCs) via toll-like receptor 4 (TLR4) through the MyD88-independent pathway, which favors an anti-inflammatory environment by inducing a type 2 phenotype that promotes the differentiation of CD4 ⁺ T-helper (Th) lymphocytes into Th2 versus Th1 effector cells.

Western Blot Analysis

Cell Line:	HT22 cells
Concentration:	1 µM
Incubation Time:	5 minutes
Result:	Caused Munc13-1 to transfer to the membrane fraction.

体内研究

Bryostatin 1 (30 μg/kg; intraperitoneal injection; 3 d per week; for 2 weeks; C57BL/6J mice) treatment abolishes the onset of EAE.

Animal Model:	Female C57BL/6J mice (8-12-week-old) with MOG _35-55
Dosage:	30 μg/kg
Administration:	Intraperitoneal injection; 3 d per week; for 2 weeks
Result:	Abolished the onset of experimental autoimmune encephalomyelitis (EAE).