ML224(NCGC00242364; ANTAG3) 是一种选择性 TSHR 反向激动剂；抑制 TSH 刺激的 cAMP 产生，IC50 = 2.3 μM。
| Cas No. | 1338824-21-7 |
| 别名 | NCGC00242364; ANTAG3 |
| Canonical SMILES | COC(C(COC1=C(C)C=C(NC(C)=O)C=C1C)=C2)=CC=C2C(NC3=C4C=CC=C3)N(C4=O)CC5=CC=CO5 |
| 分子式 | C31H31N3O5 |
| 分子量 | 525.59 |
| 溶解度 | ≥ 17.05mg/mL in DMSO |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | ML224(NCGC00242364; ANTAG3) is a selective TSHR inverse agonist; inhibits TSH-stimulated cAMP production with an IC50 = 2.3 μM.IC50 value: 2.3 uM [1]Target: TSHR agonistin vitro: ANTAG3 was selective for TSHR inhibition; half-maximal inhibitory doses were 2.1 μM for TSHR and greater than 30 μM for LH and FSH receptors [2]. in vivo: In mice treated with TRH, ANTAG3 lowered serum free T4 by 44% and lowered mRNAs for sodium-iodide cotransporter and thyroperoxidase by 75% and 83%, respectively. In mice given M22, ANTAG3 lowered serum free T4 by 38% and lowered mRNAs for sodium-iodide cotransporter and thyroperoxidase by 73% and 40%, respectively [2]. References:
[1]. Huang W, et al. Identification of Thyroid Stimulating Hormone Receptor Inverse Agonists. Probe Reports from the NIH Molecular Libraries Program
[2]. Neumann S, et al. A selective TSH receptor antagonist inhibits stimulation of thyroid function in female mice. Endocrinology. 2014 Jan;155(1):310-4. |
