LY2886721
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
LY2886721是β位淀粉样蛋白裂解酶(BACE)的口服抑制剂,IC50为20.3 nM。该产品可以用于阿尔茨海默症的治疗。
BACE,也被称为β-分泌酶1,是天冬氨酸蛋白酶,对外周神经细胞中髓鞘的形成起重要作用。
在体外, LY2886721可以抑制HEK293Swe和PDAPP神经元培养物中Aβ,IC50值分别为18.7 nM和 10.7 nM 1。LY2886721剂量依赖性减少CSF sAPPβ并增加CSF sAPPα2。
在PDAPP小鼠中,口服给药LY2886721剂量依赖性降低大脑中的Aβ、C99和sAPPβ2,与赋形剂组相比,3-30 mg/kg 剂量的LY2886721治疗3个小时后,大脑中Aβ水平降低了20%-65%。此外,MAD研究表明,LY2886721显著降低了血和脑脊液中的Aβs 1。
参考文献:
1. Vassar R. BACE1 inhibitor drugs in clinical trials for Alzheimer's disease. Alzheimer's research & therapy. 2014;6(9):89.
2. Nishitomi K, Sakaguchi G, Horikoshi Y, et al. BACE1 inhibition reduces endogenous Abeta and alters APP processing in wild-type mice. Journal of neurochemistry. 2006;99(6):1555-1563.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 390.41 |
Cas No. | 1262036-50-9 |
Formula | C18H16F2N4O2S |
Solubility | insoluble in H2O; insoluble in EtOH; ≥19.52 mg/mL in DMSO |
Chemical Name | N-[3-[(4aS,7aS)-2-amino-4,4a,5,7-tetrahydrofuro[3,4-d][1,3]thiazin-7a-yl]-4-fluorophenyl]-5-fluoropyridine-2-carboxamide |
SDF | Download SDF |
Canonical SMILES | C1C2CSC(=NC2(CO1)C3=C(C=CC(=C3)NC(=O)C4=NC=C(C=C4)F)F)N |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
动物实验 [1]: | |
动物模型 |
PDAPP小鼠 |
给药剂量 |
3、10或30 mg/kg;口服给药 |
实验结果 |
在3种剂量下,LY2886721均能显著降低海马以及皮层的Aβ1-x水平。此外,LY2886721显著降低脑实质的C99和sAPPβ水平。在10和30 mg/kg的剂量下,LY2886721显著降低皮质的C99水平,在3 mg/kg的剂量下,LY2886721的效应没有达到统计学显著性。另一方面,在3种剂量下,LY2886721均能显著降低sAPPβ水平。 |
其它注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。 |
References: [1]. May PC, Willis BA, Lowe SL, Dean RA, Monk SA, Cocke PJ, Audia JE, Boggs LN, Borders AR, Brier RA, Calligaro DO, Day TA, Ereshefsky L, Erickson JA, Gevorkyan H, Gonzales CR, James DE, Jhee SS, Komjathy SF, Li L, Lindstrom TD, Mathes BM, Martényi F, Sheehan SM, Stout SL, Timm DE, Vaught GM, Watson BM, Winneroski LL, Yang Z, Mergott DJ. The potent BACE1 inhibitor LY2886721 elicits robust central Aβ pharmacodynamic responses in mice, dogs, and humans. J Neurosci. 2015 Jan 21;35(3):1199-210. |
Description | LY2886721是β位淀粉样蛋白裂解酶(BACE)的口服小分子抑制剂,用于治疗阿尔茨海默症。 | |||||
靶点 | BACE | |||||
IC50 |
质量控制和MSDS
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