L-732,138CAS: 148451-96-1
MF: C22H18F6N2O3
MW: 472.39
A selective competitive antagonist of the tachykinin NK1 receptors.

L-732,138 (CAS 148451-96-1)

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Synonym: 3,5-bis(trifluoromethyl)benzyl N-acetyltryptophan
Application: A selective competitive antagonist of the tachykinin NK1 receptors
CAS Number: 148451-96-1
Purity: 98%
Molecular Weight: 472.39
Molecular Formula: C22H18F6N2O3
* Refer to Certificate of Analysis for lot specific data (including water content).
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L-732,138 is a selective nonpeptide tachykinin NK-1R (NK1) antagonist with 1000 fold more potency towards the NK-1R receptor over NK-2R (NK2) and NK-3R (NK3) receptors with an IC50= 2.3 nM. In addition, this compound shows a 200 fold selectivity towards human NK-1R receptors compared to rat NK-1R receptors. Studies suggest that L-732,138 reduces H3 induced skin vascular permeability. L-732,138 has been shown to competitively inhibit the binding of [125I]L-703,606 to the NK-1R receptor. Furthermore, it is known that if histidine 265 or histidine 197 are replaced with alanine on NK-1R receptors the affinity of L-732,138 is reduced.


References

1. MacLeod, A.M., et al. 1993. J. Med. Chem. 36: 2044-2045. PMID: 8393115
2. Cascieri, M.A., et al. 1994. J. Biol. Chem. 269: 6587-6591. PMID: 7509807
3. MacLeod, A.M., et al. 1994. J. Med. Chem. 37: 1269-1274. PMID: 7513763
4. Muñoz, M., et al. 2007. Invest. Ophthalmol. Vis. Sci. 48: 2775-2781. PMID: 17525212

Physical State :
Solid
Solubility :
Soluble in ethanol (100 mM), ethyl acetate (50 mg/ml), water (partly), and DMSO (100 mM).
Storage :
Store at room temperature
Melting Point :
147-148° C (lit.)
Boiling Point :
554.07° C at 760 mmHg (Predicted)
Density :
1.40 g/cm3 (Predicted)
Refractive Index :
n20D 1.54 (Predicted)
IC50 :
NK-1R: IC50 = 1.48 nM (human); Neurokinin 2 receptor: IC50 = 0.40 µM (rat); NK-2R: IC50 >5 µM (human); NK-3R: IC50 >5 µM (human)
Ki Data :
NK-1R: Ki= 0.73 nM (human); Neurokinin 2 receptor: Ki= 134 nM (rat); Neurokinin 1 receptor: Ki= 0.13 µM (rat)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
132837
MDL Number :
MFCD00237267
SMILES :
CC(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)OCC3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F

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Certificate of Analysis

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