| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| L409213-1ml |
1ml |
现货  |
|
| 英文别名 | (S)-4-(2,4-difluoro-5-(pyrimidin-5-yl)phenyl)-4-methyl-5,6-dihydro-4H-1,3-thiazin-2-amine |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | LY2811376 |
| 生化机理 | LY2811376 是首个可口服的非肽β分泌酶（BACE1）抑制剂，其 IC50 值为 239 nM-249 nM，可减少 Aβ 的分泌，EC50 值为 300 nM，对 BACE1 的选择性是 BACE2 的 10 倍，对其他天冬氨酸蛋白酶（包括 cathepsin D、胃蛋白酶或肾素）的抑制率超过 50 倍。第一阶段 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | beta 分泌酶 1 抑制剂 |
| 产品介绍 |
LY2811376是第一个口服有效的，非肽类β-secretase(BACE1)抑制剂，IC50为239 nM-249 nM，可以减少Aβ分泌，EC50为300 nM，作用于BACE1比作用于BACE2选择性高10倍，比作用于其他天冬氨酸蛋白酶（包括Cathepsin D，胃蛋白酶和肾素）抑制效果高50倍以上。Phase 1。 Information LY2811376 LY2811376 is the first orally available non-peptidic β-secretase(BACE1) inhibitor with IC50 of 239 nM-249 nM, that act to decrease Aβ secretion with EC50 of 300 nM, demonstrated to have 10-fold selectivity towards BACE1 over BACE2, and more th LY2811376 demonstrates concentration-dependent inhibition of hBACE1 with an IC50 of 239 and 249 nM against a small synthetic peptide or a larger chimeric protein substrate, respectively. LY2811376 treatment yields a concentration-dependent decrease in Aβ secretion in APP-overexpressing HEK293 cells. LY2811376 inhibits Aβ secretion with EC50 of ~100 nM in primary neuronal cultures of PDAPP transgenic mouse. In vivo Administration of LY2811376 (10, 30, and 100 mg/kg doses) results in dose-dependent, significant reductions in Aβ, as well as sAPPβ and C99, the proximal cleavage products of APP proteolysis by BACE1 in APPV717F mouse model of Aβ pathology. After treatment with LY2811376 (5 mg/kg), reductions in Aβ1-x are observed in plasma, with a maximal 85% reduction observed from 4 to 12 h after dosing in beagle dogs. cell lines：MV-4-11, MOLM-13, and OCI-AML-3 cell lines Concentrations：~ 100 μM Incubation Time：48–72 hours Powder Purity:≥99% |
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | C[C@]1(CCSC(=N1)N)C2=C(C=C(C(=C2)C3=CN=CN=C3)F)F |
| 分子量 | 320.36 |
| Reaxy-Rn | 45675369 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=45675369&ln= |
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