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L-732138

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Chemical Structure| 148451-96-1 同义名 : -
CAS号 : 148451-96-1
货号 : A801868
分子式 : C22H18F6N2O3
纯度 : 99%+
分子量 : 472.38
MDL号 : MFCD00237267
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(529.23 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Substance P is an undecapeptide that binds to the neurokinin-1 (NK-1) receptor, regulating many biological functions involved in neurogenic inflammation, pain, depression, and tumor cell migration. L-732138 is an NK-1 receptor antagonist that inhibits the binding of 125I-substance P to human NK-1 receptor expressed in Chinese hamster ovary cells with an IC50 value of 2.3 ± 0.7 nM. It shows over 1000-fold lower affinity for human NK-2 and NK-3 receptors. L-732138 also competitively inhibited the binding of [125I]-L-703,606, the quinuclidine amine antagonist, to human NK-1 receptor with an IC50 value of 3 nM[1]. The IC50 growth inhibition concentrations of L-732138 on melanoma cell lines COLO 858, MEL-H0, and COLO 679 are 44.6, 76.3, and 64.2 μM, respectively[2]. In (C57BL/6xDBA/2) F1 mice, daily intravenous injection of L-732138 (20 mg/kg) for 4 days reduced bone marrow B220+ population to 8.1% compared to 21.2% in DMSO-treated group[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.12mL

0.42mL

0.21mL

10.58mL

2.12mL

1.06mL

21.17mL

4.23mL

2.12mL
参考文献

[1]Cascieri MA, Macleod AM, Underwood D, et al. Characterization of the interaction of N-acyl-L-tryptophan benzyl ester neurokinin antagonists with the human neurokinin-1 receptor. J Biol Chem. 1994;269(9):6587-6591.

[2]Muñoz M, Rosso M, González-Ortega A, Coveñas R. The NK-1 Receptor Antagonist L-732,138 Induces Apoptosis and Counteracts Substance P-Related Mitogenesis in Human Melanoma Cell Lines. Cancers (Basel). 2010;2(2):611-623. Published 2010 Apr 20. doi:10.3390/cancers2020611

[3]Zhang Y, Lu L, Furlonger C, Wu GE, Paige CJ. Hemokinin is a hematopoietic-specific tachykinin that regulates B lymphopoiesis. Nat Immunol. 2000;1(5):392-397. doi:10.1038/80826