2. GPCR/G Protein
    Neuronal Signaling
  3. Neurokinin Receptor
  4. L-732138

L-732138 

Cat. No.: HY-101249 Purity: 99.75%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

L-732138 Chemical Structure

L-732138 Chemical Structure

CAS No. : 148451-96-1

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Solution
10 mM * 1 mL in DMSO USD 99 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 99 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
50 mg USD 480 In-stock
Estimated Time of Arrival: December 31
100 mg USD 760 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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].

IC50 & Target[1][2]

NK1

2.3 nM (IC50)

In Vitro

L-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[1].
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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

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 Vivo

L-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[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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
Result: Abolished the vagally-induced plasma leakage in tracheobronchial tissues, and dose-dependently inhibited the LPS enhanced vagally-induced plasma exudation in traceobronchial tissues.
Molecular Weight

472.38

Appearance

Solid

Formula

C22H18F6N2O3
CAS No.
SMILES

O=C(OCC1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1)[[email protected]](CC2=CNC3=CC=CC=C23)NC(C)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (529.23 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1169 mL 10.5847 mL 21.1694 mL
5 mM 0.4234 mL 2.1169 mL 4.2339 mL
10 mM 0.2117 mL 1.0585 mL 2.1169 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 6.25 mg/mL (13.23 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 6.25 mg/mL (13.23 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.75%

COA (251 KB) LCMS (269 KB)

Handling Instructions (2659 KB)
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

L-732138148451-96-1L732138L 732138Neurokinin ReceptorNK receptorTachykinin receptorAntitumorhyperalgesiacytotoxicitymitogenstimulationapoptoticntravenouslylipopolysaccharidevagally-inducedplasmaInhibitorinhibitorinhibit

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