计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
PF-06751979 is a potent, brain penetrant, β-site amyloid precursor protein cleaving enzyme 1 ( BACE1 ) inhibitor with an IC 50 of 7.3 nM in BACE1 binding assay.
In Vitro
PF-06751979 shows improved selectivity over BACE2 (IC 50 =194 nM) in binding (27-fold) relative to the literature examples and across multiple chemical series in BACE1 program. PF-06751979 also inhibits BACE1 and BACE2 in a fluorescent polarization (FP) assay with IC 50 s of 26.9 nM and 238 nM, respectively. PF-06751979 has excellent potency at BACE1 in binding or FP assay formats along with cellular activity looking at production of sAPPβ in H4 cells with an IC 50 of 5 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
PF-06751979 displays excellent brain penetration, potent in vivo efficacy, and broad selectivity over related aspartyl proteases including BACE2. Acute administration of PF-06751979 yields a robust dose-responsive and time-dependent reduction of cerebral spinal fluid (CSF) Aβx-40 with peak inhibition at 3 h of >77%. To determine if the reduction in brain and CSF Aβ is maintained during sustained exposure to PF-06751979, a 5 day subchronic study is executed, dosing once daily by subcutaneous (SC) administration (10 or 50 mg/kg/day). Brain and CSF samples are collected on day 5, following the last dose. PF-06751979 produces a dose-responsive and time-dependent inhibition of Aβ42 in mouse brain. At the 50 mg/kg/day dose, maximal brain lowering is 63% at 7 to 9 h. Administration of PF-06751979 (10 or 50 mg/kg/day for 5 days) produces a dose-responsive and time-dependent inhibition of Aβx-40 in mouse CSF resulting in 77% inhibition of CSF at 3 h post-final 50 mg/kg dose . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:IC50: 7.3 nM (BACE1), 194 nM (BACE2)
规格
规格或纯度
10mM in DMSO
英文名称
PF-06751979
生化机理
PF-06751979 是一种强效、脑穿透性、β 位淀粉样前体蛋白裂解酶 1（BACE1）抑制剂，在 BACE1 结合试验中的 IC 50 为 7.3 nM。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
C[C@H]1C[C@H]2CSC(=N[C@]2(CO1)C3=NC(=CS3)NC(=O)C4=NC=C(C=C4)OC(F)F)N
关联CAS
PubChem CID
MeSH Entry Terms
2-Pyridinecarboxamide, N-(2-((4aR,6S,8aR)-2-amino-4,4a,5,6-tetrahydro-6-methylpyrano(3,4-d)(1,3)thiazin-8a(8H)-yl)-4-thiazolyl)-5-(difluoromethoxy)-;N-(2-((4aR,6S,8aR)-2-Amino-6-methyl-4,4a,5,6-tetrahydropyrano(3,4-d)(1,3)thiazin-8a(8H)-yl)-1,3-thiazol-4-
分子量
455.50
技术文档
高级数据
关联靶点（人）
BACE1
Tchem
β-分泌酶1(Beta-secretase 1)
(7 活性数据)
BACE2
Tchem
β-分泌酶2(Beta-secretase 2)
(2 活性数据)
KCNH2
Tclin
钾电压门控通道亚家族 H 成员 2(Potassium voltage-gated channel subfamily H member 2)
(3 活性数据)
安全和危险性（GHS）
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
常见问题
本产品应如何储存？
请于?80 °C条件下保存。需超低温保存以维持规定的有效期。
本产品如何运输？
本产品采用干冰配冷袋冷冻运输。收货后请立即拆包，并按上述储存条件保存；处理干冰时请戴隔热手套并保持通风。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 1818339-66-0，分子式为 C18H19F2N5O3S2，分子量为 455.50 g/mol。
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