| 生物活性: |
靶点:TRH-R 通路:Endocrinology & Hormones 背景说明:Taltirelin是一种促甲状腺激素释放激素受体 (TRH-R) 激动剂。 生物活性:Taltirelin (TA0910) is a superagonist at thyrotropin-releasing hormone receptor (TRH-R) with an IC50 of 910 nM and EC50 of 36 nM for stimulating an increase in cytosolic Ca2+ concentration (Ca2+ release)[1]. IC50:IC50: 910 nM (Thyrotropin-releasing hormone receptor)[1] In Vitro:Taltirelin (TAL) exhibited lower binding affinities than TRH and lower signaling potency via the inositol-1,4,5-trisphosphate/calcium pathway than TRH. However, TAL exhibited higher intrinsic efficacy than TRH in stimulating inositol-1,4,5-trisphosphate second messenger generation. TAL is a superagonist at TRH-R.[1] 数据来源文献:[1]. Thirunarayanan N, et al. Taltirelin is a superagonist at the human thyrotropin-releasing hormone receptor. Front Endocrinol (Lausanne). 2012 Oct 9;3:120.
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| 其它标识: |
SMILES:CN1C(=O)C[C@H](NC1=O)C(=O)N[C@@H](CC2=CN=CN2)C(=O)N3CCC[C@H]3C(=O)N InChIKey:LQZAIAZUDWIVPM-SRVKXCTJSA-N InChI:InChI=1S/C17H23N7O5/c1-23-13(25)6-10(22-17(23)29)15(27)21-11(5-9-7-19-8-20-9)16(28)24-4-2-3-12(24)14(18)26/h7-8,10-12H,2-6H2,1H3,(H2,18,26)(H,19,20)(H,21,27)(H,22,29)/t10-,11-,12-/m0/s1 PubChem CID:114750
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| 基本信息: |
CAS:103300-74-9 中文名称:他替瑞林 英文名称:Taltirelin 分子式:C17H23N7O5 分子量:405.41 规格:5mg 溶解性:Soluble in DMSO(Need ultrasonic) 纯度:≥98% 外观(性状):Solid 储存条件:Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
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| 靶点: |
TRH-R |