1. GPCR/G Protein
    Neuronal Signaling
  2. Neurokinin Receptor
  3. L-733060 hydrochloride

L-733060 hydrochloride 

Cat. No.: HY-14406A
Handling Instructions

L-733060 hydrochloride is a potent tachykinin NK1 receptor antagonist. L-733060 hydrochloride inhibits neurogenic plasma extravasation at doses that do not cause adverse cardiovascular effects in rodents and also acts as an antitumoral agent.

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

L-733060 hydrochloride Chemical Structure

L-733060 hydrochloride Chemical Structure

CAS No. : 148687-76-7

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Description

L-733060 hydrochloride is a potent tachykinin NK1 receptor antagonist. L-733060 hydrochloride inhibits neurogenic plasma extravasation at doses that do not cause adverse cardiovascular effects in rodents and also acts as an antitumoral agent[1][2].

IC50 & Target[1]

NK1

 

In Vitro

L-733060 (30-300 nM) inhibits the [Ca2+]i mobilisation caused by substance P (100 nM) in a concentration-dependent manner in human tachykinin NK1 receptor-transfected CHO cells[1].
L-733060 (2.5-20 μM; 48 and or 96 h) results in a concentration-dependent cytotoxicity in COLO 858 cells[2].
L-733060 (10-30 μM; 24 and 48 h) inhibits MEL H0 cells proliferation with IC50s of 27.5 μM and 18.9 μM at 24 h and 48 h, respectively[2].
L-733060 (20-50 μM; and or 72 h) inhibits COLO 679 cells growth with IC50s of 33.8 μM and 31.5 μM at 30 h and 72 h, respectively[2].

Cell Proliferation Assay[2]

Cell Line: COLO 858 cells
Concentration: 2.5, 5, 10, 20 μM
Incubation Time: 0, 48, 96 h
Result: Inhibited cells growth with IC50s of 8.7 μM and 7.1 μM at 48 h and 96 h, respectively.
In Vivo

L-733060 (10-1000 μg/kg; i.v.) inhibits electrically stimulated plasma extravasation in dura mater of rats[1].
L-733060 (300-3000 μg/kg; i.v.) has no significant hypotensive or bradycardic effects are observed at doses of <3000 μg/kg in conscious or anaesthetised rats[1].

Animal Model: Male Sprague-Dawley rats (200 g) with electrical stimulation of the trigeminal ganglion[1]
Dosage: 10, 100, 1000 mg/kg
Administration: I.v. injection
Result: Produced a significant dose-related inhibition of plasma extravasation with an ID50 of 212±19 μg/kg.
Molecular Weight

439.82

Formula

C₂₀H₂₀ClF₆NO

CAS No.

148687-76-7

SMILES

FC(F)(C1=CC(C(F)(F)F)=CC(CO[[email protected]@H]2[[email protected]@](C3=CC=CC=C3)([H])NCCC2)=C1)F.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

L-733060L733060L 733060Neurokinin ReceptorNK receptortachykininNKneurogenicplasmaextravasationcardiovascularantitumoralneuroprotectionInhibitorinhibitorinhibit

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Product Name:
L-733060 hydrochloride
Cat. No.:
HY-14406A
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