An NK1 receptor antagonist (IC50 = 1.6 nM in CHO cells expressing the human receptor); selective for NK1 over NK2 and NK3 receptors (IC50s = >5

L-732,138 – 50 mg

Brand:
Cayman
CAS:
148451-96-1
Storage:
-20
UN-No:
Non-Hazardous - /

L-732,138 is a neurokinin-1 (NK1) receptor antagonist (IC50 = 1.6 nM in CHO cells expressing the human receptor).{57090} It is selective for NK1 over NK2 and NK3 receptors (IC50s = >5,000 nM for both). L-732,138 inhibits the growth of COLO 858, MEL HO, and COLO 679 melanoma cells (IC50s = 44.6, 76.3, and 64.2 μM, respectively), as well as induces apoptosis in these cell lines.{57091} It inhibits plasma extravasation induced by substance P (Item No. 24035) in guinea pigs (ID50 = 8 mg/kg, i.p.).{57090} L-732,138 attenuates mechanical allodynia and cold hyperalgesia in a rat model of neuropathic pain induce by chronic constriction injury of the sciatic nerve.{57092}  

 

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Description

An NK1 receptor antagonist (IC50 = 1.6 nM in CHO cells expressing the human receptor); selective for NK1 over NK2 and NK3 receptors (IC50s = >5,000 nM for both); inhibits the growth of COLO 858, MEL HO, and COLO 679 melanoma cells (IC50s = 44.6, 76.3, and 64.2 μM, respectively), as well as induces apoptosis in these cell lines; inhibits plasma extravasation induced by substance P in guinea pigs (ID50 = 8 mg/kg, i.p.); attenuates mechanical allodynia and cold hyperalgesia in a rat model of neuropathic pain induce by chronic constriction injury of the sciatic nerve

Formal name: N-acetyl-L-tryptophan [3,5-bis(trifluoromethyl)phenyl]methyl ester

Synonyms: 

Molecular weight: 472.4

CAS: 148451-96-1

Purity: ≥98%

Formulation: A crystalline solid

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