| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| Other Sizes |
|
| ln Vitro |
Cytotoxicity is concentration-dependent and is produced in COLO 858, MEL HO, and COLO 679 cells treated with L-732138 (0 -100 µM; initial doubling time). With an IC50 of 44.6 μM in COLO 858 cells, 76.3 μM in MEL HO cells, and 64.2 μM in COLO 679 cells, L-732138 suppresses cell growth. Substance P (SP) mitogen stimulation is blocked by L-732138 [1]. Following L-732,138 treatment, a significant number of apoptotic cells were discovered in the melanoma cell lines COLO 858, MEL HO, and COLO 679. Three melanoma cell lines had an IC50 concentration of 43.6% apoptotic cells in DAPI-stained cultures, and an IC100 concentration of 51.4% apoptotic cells [1].
|
|---|---|
| ln Vivo |
Vagus nerve-induced plasma extravasation was eliminated and LPS enhancement was markedly decreased in male Dunkin-Hartley guinea pigs treated with L-732138 (10-4-10-2 mol/kg; intravenous injection; 15 min duration). LPS-enhanced vagus nerve-induced plasma extravasation cannot be fully inhibited by L-732138 or SOD administration alone, but it can be blocked by the combination of the two pretreatments [3].
|
| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: COLO 858, MEL HO and COLO 679 Cell Tested Concentrations: 0 µM, 20 µM, 40 µM, 60 µM, 80 µM, 100 µM Incubation Duration: First Doubling Time Experimental Results: Produced Concentration - dependent cytotoxicity. |
| Animal Protocol |
Animal/Disease Models: Male Dunkin-Hartley guinea pigs (350-500 g) injected with lipopolysaccharide (LPS) [3]
Doses: 10-4 mol/kg, 10-3 mol/kg and 10-2 mol/kg Route of Administration: intravenous (iv) (iv)Injection Injection; 15 min Experimental Results: Eliminates vagus nerve-induced plasma leakage in tracheobronchial tissue and dose-dependently inhibits vagus nerve-induced plasma leakage in LPS-enhanced tracheobronchial tissue. |
| References |
|
| Molecular Formula |
C22H18F6N2O3
|
|---|---|
| Molecular Weight |
472.39
|
| Exact Mass |
472.122
|
| CAS # |
148451-96-1
|
| PubChem CID |
132837
|
| Appearance |
White to off-white solid powder
|
| Melting Point |
147-148 ℃(lit.)
|
| LogP |
5.387
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
33
|
| Complexity |
677
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
CC(=O)N[C@@H](CC1=CNC2=CC=CC=C21)C(=O)OCC3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F
|
| InChi Key |
BYYQYXVAWXAYQC-IBGZPJMESA-N
|
| InChi Code |
InChI=1S/C22H18F6N2O3/c1-12(31)30-19(8-14-10-29-18-5-3-2-4-17(14)18)20(32)33-11-13-6-15(21(23,24)25)9-16(7-13)22(26,27)28/h2-7,9-10,19,29H,8,11H2,1H3,(H,30,31)/t19-/m0/s1
|
| Chemical Name |
[3,5-bis(trifluoromethyl)phenyl]methyl (2S)-2-acetamido-3-(1H-indol-3-yl)propanoate
|
| Synonyms |
L 732138; L732138; 3,5-bis(TFM)Bz NAcTrp
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~529.23 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (13.23 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 6.25 mg/mL (13.23 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1169 mL | 10.5845 mL | 21.1689 mL | |
| 5 mM | 0.4234 mL | 2.1169 mL | 4.2338 mL | |
| 10 mM | 0.2117 mL | 1.0584 mL | 2.1169 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
