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 |
| 2MG | 40 | Get Quote |
|
| 5MG | 65 | Get Quote |
|
| 10MG | 110 | Get Quote |
|
| 25MG | 205 | Get Quote |
|
| 50MG | 357 | Get Quote |
|
| 100MG | 530 | Get Quote |
|
| 200MG | Get Quote | Get Quote |
|
| 500MG | Get Quote | Get Quote |
|
| 1G | Get Quote | Get Quote |
|
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
-
Hemokinin 1 (human)
Endogenous substance P homolog that is a selective agonist at the tachykinin NK1 receptor (IC50 values are 1.8, 370 and 480 nM for NK1, NK3 and NK2 receptors respectively). Has proliferative and antiapoptotic actions on B-cells in vitro and is antihypertensive in vivo.
-
NIH-12848
NIH-12848 is a putative inhibitor of phosphatidylinositol 5-phosphate 4-kinase γ (PI5P4Kγ) with an IC50 of 1 μM.
-
[Sar9] Substance P
[Sar9]-Substance P is one of NK-1 receptor agonist. The action of SP on progesterone metabolism was mimicked by the rNK1-specific agonist [Sar-9,Met(O2)11]-SP.
