CAS |
No.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 |
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 |
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 |
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. |
规格 |
5mg 10mg 50mg 100mg |
单位 |
瓶 |