Org41841

• 常用名: Org41841
• 英文名: Org41841
• CAS号: 301847-37-0
• 分子量: 402.534
• 密度: 1.3±0.1 g/cm3
• 沸点: N/A
• 分子式: C₁₉H₂₂N₄O₂S₂
• 熔点: N/A
• 闪点: N/A

Org41841用途

ORG41841 是促黄体激素/绒毛膜促性腺激素受体 (LHCGR) 和促甲状腺激素受体 (TSHR) 的部分激动剂,其 EC50 值分别为 0.2 和 7.7 μM。

Org41841名称

• 中文名: Org41841
• 英文名: Org41841

Org41841生物活性

• 描述: ORG41841 是促黄体激素/绒毛膜促性腺激素受体 (LHCGR) 和促甲状腺激素受体 (TSHR) 的部分激动剂,其 EC50 值分别为 0.2 和 7.7 μM。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> TSH受体
  研究领域 >> 内分泌
• 靶点实验:

  EC50: 0.2 μM (LHCGR), 7.7 μM (TSHR)[1]

• 体外研究: 功能测定表明,Org41841是促黄体激素/绒毛膜促性腺激素受体(LHCGR)和促甲状腺激素受体(TSHR)的部分激动剂,EC50分别为0.2和7.7μM。用Org41841处理L570F显示改善的EC50为800nM。 M9对Org41841有反应,改善的EC50为2700 nM,并且对甲状腺刺激素(TSH)刺激促甲状腺激素受体(TSHR)所观察到的99％最大值的信号传导效率大大提高[1]。
• 激酶实验: 将转染的细胞培养48小时，然后在含有1mM 3-异丁基-1-甲基黄嘌呤和牛甲状腺刺激素（TSH）（0至1.8μM）或人LH（0.1）的无血清Dulbecco改良Eagle培养基中孵育1小时。在加湿的5％CO2培养箱中加入1000 ng）或Org41841（0至100μM）。在吸出培养基后，使用cAMP Biotrak Enzymeimmunoassay System的裂解缓冲液1裂解细胞。确定细胞裂解物的cAMP含量并分析数据[1]。
• 参考文献:

  [1]. Holger Jaschke, et al. A low molecular weight agonist signals by binding to the transmembrane domain of thyroid-stimulating hormone receptor (TSHR) and luteinizing hormone/chorionic gonadotropin receptor(LHCGR). J Biol Chem. 2006 Apr 14;281(15):9841-4.

Org41841物理化学性质

• 密度: 1.3±0.1 g/cm3
• 分子式: C₁₉H₂₂N₄O₂S₂
• 分子量: 402.534
• 精确质量: 402.118408
• LogP: 4.34
• InChIKey: DVSFSADBOJYPGF-UHFFFAOYSA-N
• SMILES: COc1cccc(-c2nc(SC)nc3sc(C(=O)NC(C)(C)C)c(N)c23)c1
• 折射率: 1.670
• 储存条件: 2-8℃

Org41841靶点实验

查看更多实验

实验名称：Primary cell-based high-throughput screening assay for identification of compounds th... 来源：Johns Hopkins Ion Channel Center 靶标：regulator of G-protein signaling 4 isoform 2 [Homo sapiens] External Id：JHICC_RGS_Act_HTS

实验名称：Luminescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：mu-type opioid receptor isoform MOR-1 [Homo sapiens] External Id：OPRM1-OPRD1_AG_LUMI_1536_1X%ACT PRUN

实验名称：QFRET-based biochemical primary high throughput screening assay to identify exosite i... 来源：The Scripps Research Institute Molecular Screening Center 靶标：disintegrin and metalloproteinase domain-containing protein 17 preproprotein [Homo sapiens] External Id：ADAM17_INH_QFRET_1536_1X%INH PRUN

实验名称：Fluorescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_AG_FLUO8_1536_1X%ACT PRUN

实验名称：uHTS identification of small molecule activators of the adaptive arm of the Unfolded ... 来源：Burnham Center for Chemical Genomics 靶标：N/A External Id：BCCG-A405-UPR-XBP1-PrimaryAgonist-Assay

实验名称：Fluorescence polarization to screen for inhibitor that competite the binding of FadD2... 来源：Broad Institute 靶标：FATTY-ACID-CoA LIGASE FADD28 (FATTY-ACID-CoA SYNTHETASE) External Id：2147-01_Inhibitor_SinglePoint_HTS_Activity

实验名称：Bursicon-induced LGR2 mediated cAMP production in LGR-2/CRE6x-Luciferase co-transfect... 来源：Broad Institute 靶标：N/A External Id：Bursicon-induced LGR2 mediated cAMP production in LGR-2/CRE6x-Luciferase co-transfected HEK293 cells Inhibition - 7011-01_Antagonist_SinglePoint_HTS_Activity

实验名称：Fluorescence-based cell-based primary high throughput screening assay to identify pos... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_PAM_FLUO8_1536_1X%ACT PRUN

实验名称：Primary qHTS for Identification of Calcium Integrin Binding Protein 1 (CIB1) Competit... 来源：NCGC External Id：CIB1-p1-p2

实验名称：Fluorescence polarization-based biochemical high throughput primary assay to identify... 来源：The Scripps Research Institute Molecular Screening Center 靶标：RecName: Full=Sialate O-acetylesterase; AltName: Full=H-Lse; AltName: Full=Sialic acid-specific 9-O-acetylesterase; Flags: Precursor [Homo sapiens] External Id：SIAE_INH_FP_1536_1X%INH PRUN

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Org41841英文别名

• 5-amino-N-tert-butyl-4-(3-methoxyphenyl)-2-(methylsulfanyl)thieno[2,3-d]pyrimidine-6-carboxamide
• 5-amino-N-tert-butyl-4-(3-methoxyphenyl)-2-(methylthio)-6-thieno[2,3-d]pyrimidinecarboxamide
• 5-Amino-4-(3-methoxyphenyl)-N-(2-methyl-2-propanyl)-2-(methylsulfanyl)thieno[2,3-d]pyrimidine-6-carboxamide