Cart
sales@molnova.com
L-732138
CAS No. 148451-96-1
L-732138( —— )
Catalog No. M21568 CAS No. 148451-96-1
L-732138 is a potent and competitive antagonist of neurokinin-1 (NK-1) receptor(IC50 : 2.3 nM).
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 45 | In Stock |
|
| 5MG | 41 | In Stock |
|
| 10MG | 69 | In Stock |
|
| 25MG | 130 | In Stock |
|
| 50MG | 188 | In Stock |
|
| 100MG | 281 | In Stock |
|
| 200MG | 407 | In Stock |
|
| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
-
Product NameL-732138
-
NoteResearch use only, not for human use.
-
Brief DescriptionL-732138 is a potent and competitive antagonist of neurokinin-1 (NK-1) receptor(IC50 : 2.3 nM).
-
DescriptionL-732138 is a potent and competitive antagonist of neurokinin-1 (NK-1) receptor(IC50 : 2.3 nM).
-
In VitroL-732138 (0 -100 μM; first doubling time; COLO 858, MEL HO and COLO 679 cells) treatment results in a concentration-dependent cytotoxicity. L-732138 inhibits cell growth with IC50 of 44.6 μM for COLO 858 cells, 76.3 μM for MEL HO cells and 64.2 μM for COLO 679 cells. L-732138 blocks substance P (SP) mitogen stimulation.L-732,138 treatment results in a large number of apoptotic cells were found in COLO 858, MEL HO and COLO 679 melanoma cell lines. In DAPI-stained cultures, at IC50 concentration of 43.6% apoptotic cells for the three melanoma cell lines, whereas at IC100 concentration of 51.4 % apoptotic cells. Cell Proliferation Assay 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 Result:Resulted in a concentration-dependent cytotoxicity.
-
In VivoL-732138 (10-4-10-2 mol/kg; intravenous injection; for 15 minutes; male Dunkin-Hartley guinea-pigs) treatment abolishes vagally-induced plasma exudation and significantly inhibits the enhancement by LPS. The LPS-enhanced vagally-induced plasma exudation is not completely inhibited by either L-732138 or SOD pretreatment alone, but is blocked by the combination of both pretreatments. Animal Model:Male Dunkin-Hartley guinea-pigs (350-500 g) injected withlipopolysaccharide (LPS) Dosage:10-4 mol/kg , 10-3 mol/kg and 10-2 mol/kg Administration:Intravenous injection; for 15 minutes Result:Abolished the vagally-induced plasma leakage in tracheobronchial tissues, and dose-dependently inhibited the LPS enhanced vagally-induced plasma exudation in traceobronchial tissues.
-
Synonyms——
-
PathwayGPCR/G Protein
-
TargetNeurokinin Receptor
-
RecptorNK-1
-
Research Area——
-
Indication——
Chemical Information
-
CAS Number148451-96-1
-
Formula Weight472.38
-
Molecular FormulaC22H18F6N2O3
-
Purity>98% (HPLC)
-
SolubilityIn Vitro:?DMSO : 250 mg/mL (529.23 mM)
-
SMILESCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OCc1cc(cc(c1)C(F)(F)F)C(F)(F)F
-
Chemical Name[35-Bis(trifluoromethyl)phenyl]methyl (2S)-2-acetamido-3-(1H-indol-3-yl)propanoate
Shipping & Storage Information
-
Storage(-20℃)
-
ShippingWith Ice Pack
-
Stability≥ 2 years
Reference
1.Mu?oz M et al. The NK-1 Receptor Antagonist L-732138 Induces Apoptosis and Counteracts Substance P-Related Mitogenesis in Human Melanoma Cell Lines. Cancers (Basel). 2010 Apr 20;2(2):611-23.
molnova catalog
related products
-
[Sar9,Met(O2)11]-Sub...
Sar9, Met (O2)11-Substance P is a neurokinin-1 receptor agonist. It is an analog of the naturally occurring human neuropeptide Substance P, which can be found throughout the body, including in the airways of humans and many other species.
-
[Lys5,MeLeu9,Nle10]-...
Highy selective and potent NK2 receptor agonist (IC50 = 6.1 nM). Induces contraction of the rat fundus and bladder (EC50 values are 117 and 10 nM respectively).
-
Neurokinin B
Neurokinin B (NKB) belongs in the family of tachykinin peptides. Neurokinin B is implicated in a variety of human functions and pathways such as the secretion of gonadotropin-releasing hormone.
