LP-922056
目录号: PL13094 纯度: ≥98%
CAS No. :1365060-22-5
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中文名称
LP-922056
中文别名
2-((6-氯-7-环丙基噻吩并[3,2-d]嘧啶-4-基)硫代)乙酸
英文名称
LP-922056
英文别名
2-((6-Chloro-7-cyclopropylthieno[3,2-d]pyrimidin-4-yl)thio)acetic acid;LP-922056;2-[(6-Chloro-7-cyclopropylthieno[3,2-d]pyrimidin-4-yl)thio]acetic acid;2-(6-chloro-7-cyclopropylthieno[3,2-d]pyrimidin-4-yl)sulfanylacetic acid;2-(6-chloranyl-7-cyclopropyl-thieno[3,2-d]pyrimidin-4-yl)sulfanylethanoic acid;BDBM50154397;LP 922056;M9K
Cas No.
1365060-22-5
分子式
C11H9ClN2O2S2
分子量
300.78
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
LP-922056 是一种具有口服活性,强效的 Notum Pectinacetylesterase 抑制剂,在人和小鼠细胞测定中的 EC50 分别为 21 nM,55 nM。LP-922056 显着增加小鼠和大鼠股骨中轴的骨皮质厚度。
生物活性
LP-922056 is an orally active, highly potent Notum Pectinacetylesterase inhibitor with EC 50 s of 21 nM, 55 nM in human and mouse cellular assay, respectively. LP-922056 significantly increases midshaft femur cortical bone thickness in mice and rats.
性状
Solid
IC50 & Target[1][2]
EC50: 21 nM (human Notum Pectinacetylesterase) and 55 nM (mouse Notum Pectinacetylesterase)
体外研究(In Vitro)
NOTUM can inactivate WNTs by functioning as a WNT lipase.
has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
LP-922056 (compound 44; 3-30 mg/kg; oral gavage; daily; for 25 days) causes an increase in cortical bone thickness at all doses.
LP-922056 (10 mg/kg; orally) achieves high C max (129 μM) and AUC (1533 μM?h).
LP-922056 (10?mg/kg; daily diet; for 4 weeks) increases cortical bone thickness and strength in midshaft femur, bone mass in the femoral neck and vertebral body cortical shell in Twelve-week-old male mice.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. James E Tarver Jr, et al. Stimulation of cortical bone formation with thienopyrimidine based inhibitors of Notum Pectinacetylesterase. Bioorg Med Chem Lett. 2016 Mar 15;26(6):1525-1528.
[2]. Robert Brommage, et al. NOTUM inhibition increases endocortical bone formation and bone strength. Bone Res. 2019 Jan 8;7:2.
溶解度数据
In Vitro: DMSO : 125 mg/mL (415.59 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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