148451-96-1
148451-96-1
Chemical Structure
L-732138
- CAS No.: 148451-96-1
- Formula:C22H18F6N2O3
- Molecular Weight:472.38
IUPAC Name: 3,5-bis(trifluoromethyl)benzyl acetyl-L-tryptophanate
InChIKey: BYYQYXVAWXAYQC-IBGZPJMESA-N
SMILES: O=C(OCC1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1)[C@H](CC2=CNC3=CC=CC=C23)NC(C)=O
Biological Activity: L-732138 is a selective, potent and competitive neurokinin-1 (NK-1) receptor antagonist with an IC50 of 2.3 nM. L-732138 has 200-fold more potent in cloned human NK-1 receptors than cloned rat NK-1 receptors, and has > 1000-fold more potent than human NK-2 and NK-3 receptors. L-732138 can reduce hyperalgesia and has antitumor action[1][2].
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L-732138 | 99.9% | L-732138 is a selective, potent and competitive neurokinin-1 (NK-1) receptor antagonist with an IC50 of 2.3 nM. L-732138 has 200-fold more potent in cloned human NK-1 receptors than cloned rat NK-1 receptors, and has > 1000-fold more potent than human NK-2 and NK-3 receptors. L-732138 can reduce hyperalgesia and has antitumor action. | ||||||||||||||||||||
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L-732138 (Standard) | ≥98% | L-732138 (Standard) is the analytical standard of L-732138 (HY-101249). This product is intended for research and analytical applications. L-732138 is a selective, potent and competitive neurokinin-1 (NK-1) receptor antagonist with an IC50 of 2.3 nM. L-732138 has 200-fold more potent in cloned human NK-1 receptors than cloned rat NK-1 receptors, and has > 1000-fold more potent than human NK-2 and NK-3 receptors. L-732138 can reduce hyperalgesia and has antitumor action. | ||||||||||||||||||||
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References
- [1]. Muñoz M, et al. The NK-1 Receptor Antagonist L-732,138 Induces Apoptosis and Counteracts Substance P-Related Mitogenesis in Human Melanoma Cell Lines. Cancers (Basel). 2010 Apr 20;2(2):611-23. [Content Brief]
- [2]. Cascieri MA, 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 Mar 4;269(9):6587-91. [Content Brief]
