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N,N,2-三甲基-5-硝基苯磺酰胺

选择性PDE7抑制剂
规格或纯度: ≥98%
有货

库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
B137236-50mg
50mg 现货 Stock Image
B137236-200mg
200mg 期货 Stock Image
B137236-250mg
250mg 现货 Stock Image
B137236-1g
1g 现货 Stock Image

基本描述

规格或纯度 ≥98%
英文名称 N,N,2-Trimethyl-5-nitrobenzenesulfonamide
别名 BRL-50481
英文别名 BRL-50481
生化机理 BRL 50481 is a potent and selective PDE7 inhibitor (IC50 = 260 nM).Selective, competitive PDE7 inhibitor (IC 50 values are 0.15 and 12.1 μm for PDE7A and PDE7B respectively). Active in vivo and in vitro . Potentiates the anti-inflammatory effect of PDE4 inhibitor rolipram .
储存温度 2-8°C储存
运输条件 冰袋运输
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产品介绍

BRL-50481 is a selective inhibitor of phosphodiesterase 7 (PDE 7) that has acceptable selectivity for in vitro studies. Studies sμggest that BRL-50481 is used to inhibit the activity of hrPDE7A1 which is usually expressed in baculovirus-infected Spodoptera frμgiperda in a competitive manner. In osteoblasts, BRL-50481increases mineralization and bALP as a result of PDE7 silencing which upregulates several osteogenic genes. Further studies show that BRL-50481increases apoptosis in CLL cells via a mitochondrial-dependent process, and is associated with increased cAMP accumulation and down-regulation of the antiapoptotic protein survivin. BRL-50481 is a inhibitor of PDE7A.

BRL-50481 is a selective inhibitor of phosphodiesterase 7 (PDE 7) that has acceptable selectivity for in vitro studies. Studies suggest that BRL-50481 is used to inhibit the activity of hrPDE7A1 which is usually expressed in baculovirus-infected Spodoptera frugiperda in a competitive manner. In osteoblasts, BRL-50481increases mineralization and bALP as a result of PDE7 silencing which upregulates several osteogenic genes. Further studies show that BRL-50481increases apoptosis in CLL cells via a mitochondrial-dependent process, and is associated with increased cAMP accumulation and down-regulation of the antiapoptotic protein survivin. BRL-50481 is a inhibitor of PDE7A.

名称和标识符

IUPAC Name N,N,2-trimethyl-5-nitrobenzenesulfonamide
INCHI InChI=1S/C9H12N2O4S/c1-7-4-5-8(11(12)13)6-9(7)16(14,15)10(2)3/h4-6H,1-3H3
InChi Key IFIUFCJFLGCQPH-UHFFFAOYSA-N
Canonical SMILES CC1=C(C=C(C=C1)[N+](=O)[O-])S(=O)(=O)N(C)C
WGK Germany 3
PubChem CID 2921148
分子量 244.27

化学和物理性质

敏感性 对热敏感
熔点 73 °C

安全和危险性(GHS)

WGK Germany 3
个人防护装备 Eyeshields, Gloves, type N95 (US), type P1 (EN143) respirator filter

关联配体

Ligand ID 5154
名称 BRL50481
别名 BRL-50481
类别 Synthetic organic
学名 N,N,2-trimethyl-5-nitrobenzene-1-sulfonamide
生物活性评价 The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in ).
评价 Sulfadimidine (sulfamethazine) is a sulfonamide antibacterial compound. This class of compounds are competitive inhibitors of bacterial dihydropteroate synthase (DHPS), an enzyme in the pathway which generates the folic acid that is essential for bacterial growth.

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