ML 00253764 hydrochloride

Cat. No. 4854 提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Melanocortin MC₄ receptor antagonist; brain penetrant

化学名： 2-[2-[2-(5-Bromo-2-methoxyphenyl)ethyl]-3-fluorophenyl]-4,5-dihydro-2-1H-imidazole hydrochloride

纯度： ≥98% (HPLC)

文献 (1)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 for ML 00253764 hydrochloride

ML 00253764 hydrochloride is a non-peptide, melanocortin MC₄ receptor antagonist (IC₅₀ values are 320, 810 and 2120 nM for MC₄, MC₃ and MC₅ receptors respectively). Decreases cAMP accumulation in HEK-293 cells expressing the MC₄ receptor. Increases food intake and reduces loss of lean body mass in tumor bearing mice. Brain penetrant.

化合物库 for ML 00253764 hydrochloride

ML 00253764 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。

技术数据 for ML 00253764 hydrochloride

分子量	413.71
公式	C₁₈H₁₈BrFN₂O.HCl
储存	Store at +4°C
纯度	≥98% (HPLC)
CAS Number	1706524-94-8
PubChem ID	90488979
InChI Key	KZUMGPQDDCBFBF-UHFFFAOYSA-N
Smiles	BrC1=CC(CCC2=C(F)C=CC=C2C3=NCCN3)=C(OC)C=C1.Cl

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for ML 00253764 hydrochloride

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
	water	4.14	10
	DMSO	41.37	100

制备储备液 for ML 00253764 hydrochloride

以下数据基于产品分子量 413.71。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

浓度/溶剂体积/质量	1 mg	5 mg	10 mg
1 mM	2.42 mL	12.09 mL	24.17 mL
5 mM	0.48 mL	2.42 mL	4.83 mL
10 mM	0.24 mL	1.21 mL	2.42 mL
50 mM	0.05 mL	0.24 mL	0.48 mL

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产品说明书 for ML 00253764 hydrochloride

分析证书/产品说明书

化学品安全技术说明书

参考文献 for ML 00253764 hydrochloride

参考文献是支持产品生物活性的出版物。

Nicholson et al (2006) Peripheral administration of a melanocortin 4-receptor inverse agonist prevents loss of lean body mass in tumor-bearing mice. J.Pharmacol.Exp.Ther. 317 771 PMID: 16436498

Vos et al (2004) Identification of 2-[2-[2-(5-bromo-2- methoxyphenyl)-ethyl]-3-fluorophenyl]-4,5-dihydro-1H-imidazole (ML00253764), a small molecule melanocortin 4 receptor antagonist that effectively reduces tumor-induced weight loss in a mouse model. J.Med.Chem. 47 1602 PMID: 15027849

Tucci et al (2005) Potent and orally active non-peptide antagonists of the human melanocortin-4 receptor based on a series of trans-2-disubstituted cyclohexylpiperazines. Bioorg.Med.Chem.Lett. 15 4389 PMID: 16098742

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