货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
S82901-5mg	≥99%	￥820.00 S82901-5mg ￥820.00 3-5天	0 货期：3-5天	-	-	-	-
S82901-10mg	≥99%	￥1600.00 S82901-10mg ￥1600.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

ML224 (NCGC00242364) is a selective TSHR antagonist with an IC50 value of 2.1 µM. ML224 can be used in the study of Graves' disease and other thyroid disorders.

靶点：

TSHR:2.1 μM (IC50);LHR:＞30 μM (IC50);FSHR:＞30 μM (IC50);TSHReceptor

体外研究：

ML224 (0.001-100 µM; 20 min) exhibits half-maximal inhibitory doses of 2.1 µM for TSHR and greater than 30 µM for LH and FSH receptors in human embryonic kidney 293 cells. Cell Viability Assay Cell Line: Human embryonic kidney 293 cells (stably expressing TSHRs, LHRs, or FSHRs) Concentration: 0.001-100 µM Incubation Time: 20 min Result: Showed the IC50 for stimulation by bovine TSH (1.8 nM) was 2.1 µM.Showed inhibition of LH and FSH stimulation was less than 15% for LH (1 nM) and less than 30% for FSH (1 nM) at 30 µM.

体内研究：

ANTAG3 (2 mg/mice; i.p. via osmotic pump; single daily for 3 days) lowers serum FT4 levels and thyroidal mRNAs for TPO and NIS in mice continuously stimulated by TRH. Animal Model: Female BALB/c mice (8 to 13-week-old; ~18.7 g). Dosage: 2 mg/mice Administration: Intraperitoneal injection via osmotic pump; single daily for 3 days Result: Lowered the levels of FT4 by 44%, and the levels of TPO and NIS mRNAs by 75% and 83%, respectively.

参考文献：

1. Neumann S, et al. A selective TSH receptor antagonist inhibits stimulation of thyroid function in female mice. Endocrinology. 2014 Jan;155(1):310-4.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.903 ml	9.513 ml	19.026 ml
5 mM	0.381 ml	1.903 ml	3.805 ml
10 mM	0.19 ml	0.951 ml	1.903 ml
50 mM	0.038 ml	0.19 ml	0.381 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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