ML224 NCGC00242364; ANTAG3|cas:1338824-21-7|西域试剂

ML224 NCGC00242364; ANTAG3,99.71%

产品编号：Bellancom-12381| CAS NO：1338824-21-7| 分子式：C₃₁H₃₁N₃O₅| 分子量：525.59

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货号	价格	库存与货期
Bellancom-12381	￥1200.00	杭州北京（现货）
Bellancom-12381	￥2400.00	杭州北京（现货）
Bellancom-12381	￥3600.00	杭州北京（现货）
Bellancom-12381	￥11000.00	杭州北京（现货）
Bellancom-12381	￥18000.00	杭州北京（现货）

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ML224 NCGC00242364; ANTAG3

产品介绍

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 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.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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
(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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (190.26 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
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。