148451-96-1
148451-96-1 structure
- Name: L-732,138
- Chemical Name: [3,5-bis(trifluoromethyl)phenyl]methyl (2S)-2-acetamido-3-(1H-indol-3-yl)propanoate
- CAS Number: 148451-96-1
- Molecular Formula: C22H18F6N2O3
- Molecular Weight: 472.38000
- Catalog: Signaling Pathways GPCR/G Protein Neurokinin Receptor
- Create Date: 2018-12-10 18:51:43
- Modify Date: 2024-01-14 10:25:51
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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].
| Name | [3,5-bis(trifluoromethyl)phenyl]methyl (2S)-2-acetamido-3-(1H-indol-3-yl)propanoate |
|---|---|
| Synonyms |
L-732,138
Carbamoylcholine chloride N-Acetyl-L-trp-3,5-bistrifluoromethylbenzyl ester L-732138 |
| 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]. |
|---|---|
| Related Catalog | |
| Target |
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]. 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]. 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. |
| References |
| Melting Point | 147-148 ℃(lit.) |
|---|---|
| Molecular Formula | C22H18F6N2O3 |
| Molecular Weight | 472.38000 |
| Exact Mass | 472.12200 |
| PSA | 71.19000 |
| LogP | 5.38700 |
| Storage condition | 2-8°C |
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
|---|---|
| RIDADR | NONH for all modes of transport |