ML224 (NCGC00242364) 是一种选择性的TSHR拮抗剂,其IC50值为 2.1 μM。ML224 可用于巴塞杜氏病及其他甲状腺疾病的研究。
生物活性 | ML224 (NCGC00242364) is a selectiveTSHRantagonist with anIC50value of 2.1 μM. ML224 can be used in the study of Graves' disease and other thyroid disorders. |
IC50& Target[1] | TSHR 2.1 μM (IC50) | LHR >30 μM (IC50) | FSHR >30 μM (IC50) |
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体外研究 (In Vitro) | 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[1].
Cell Viability Assay[1] 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 IC50for 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. |
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体内研究 (In Vivo) | 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[1].
Animal Model: | Female BALB/c mice (8 to 13-week-old; ~18.7 g)[1]. | 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. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 100 mg/mL(190.26 mM;Need ultrasonic) 配制储备液 1 mM | 1.9026 mL | 9.5131 mL | 19.0262 mL | 5 mM | 0.3805 mL | 1.9026 mL | 3.8052 mL | 10 mM | 0.1903 mL | 0.9513 mL | 1.9026 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (4.76 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.76 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (4.76 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.76 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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