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L-732138

Catalog No. T8235   CAS 148451-96-1

L-732138 is a potent and competitive antagonist of neurokinin-1 (NK-1) receptor(IC50 : 2.3 nM)

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L-732138 Chemical Structure
L-732138, CAS 148451-96-1
Pack Size Availability Price/USD Quantity
1 mg In stock $ 31.00
2 mg In stock $ 44.00
5 mg In stock $ 72.00
10 mg In stock $ 122.00
25 mg In stock $ 228.00
50 mg In stock $ 397.00
100 mg In stock $ 589.00
1 mL * 10 mM (in DMSO) In stock $ 79.00
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Purity: 100%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description L-732138 is a potent and competitive antagonist of neurokinin-1 (NK-1) receptor(IC50 : 2.3 nM)
Targets&IC50 NK1:2.3 nM
In vitro L-732,138 against three human melanoma cell lines (COLO 858, MEL HO, COLO 679).?L-732,138 elicits cell growth inhibition in a concentration dependent manner in the melanoma cells studied.?Moreover, L-732,138 blocks SP mitogen stimulation.?The specific antitumor action of L-732,138 occurred through the NK-1 receptor and melanoma cell death was by apoptosis[1].
In vivo L-732138?Abolished the vagally-induced plasma leakage in tracheobronchial tissues, and dose-dependently inhibited the LPS enhanced vagally-induced plasma exudation in traceobronchial tissues[2].
Cell Research Cell Line:COLO 858, MEL HO and COLO 679 cells. Concentration:0 μM, 20 μM, 40 μM, 60 μM, 80 μM, 100 μM. Incubation Time:First doubling time[1].
Animal Research Animal Model:Male Dunkin-Hartley guinea-pigs (350-500 g) injected with lipopolysaccharide (LPS)[3].Dosage:10-4 mol/kg ,10-3 mol/kg and 10-2 mol/kg. Administration:Intravenous injection; for 15 minutes[2]
Molecular Weight 472.38
Formula C22H18F6N2O3
CAS No. 148451-96-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 4.72 mg/mL (10 mM)

TargetMolReferences and Literature

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. 2. 2 .Kuo HP, et al. Lipopolysaccharide enhances neurogenic plasma exudation in guinea-pig airways. Br J Pharmacol. 1998 Oct;125(4):711-6.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Inhibitor Library GPCR Compound Library NO PAINS Compound Library Neuronal Signaling Compound Library Bioactive Compounds Library Max Bioactive Compound Library Anti-Cancer Compound Library

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Eledoisin Aprepitant Vofopitant dihydrochloride Rolapitant hydrochloride Neurokinin A(4-10) TFA(97559-35-8 free base) Vapreotide acetate Eledoisin Related Peptide 2TFA MEN 10207 acetate

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Keywords

L-732138 148451-96-1 GPCR/G Protein Neuroscience Neurokinin receptor cytotoxicity vagally-induced NK receptor Neurokinin Receptor Inhibitor ntravenously lipopolysaccharide plasma Tachykinin receptor stimulation L 732138 mitogen peralgesia inhibit Antitumorhy L732138 apoptotic inhibitor

 

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