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Cat. No.: HY-14406

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L-733060

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

L-733060 is a selective neurokinin-1 (NK-1) receptor antagonist. L-733060 mainly regulates pain transmission and neural plasticity by blocking the binding of Substance P (P substance) to the NK-1 receptor. L-733060 blocks the promoting effect of Substance P on long-term potentiation (LTP) in the hippocampus. L-733060 reverses the orofacial hyperalgesia induced by experimental occlusal interference (EOI) in rats. L-733060 hydrochloride inhibits neurogenic plasma extravasation at a dose that does not cause adverse cardiovascular effects in rodents, and also acts as an anti-tumor agent. L-733060 can be used for the study of chronic orofacial pain.

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

CAS No.: 148700-85-0
Formula: C₂₀H₁₉F₆NO
Molecular Weight:403.36

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

Data Sheet (272 KB)

L-733060 Chemical Structure

CAS No.: 148700-85-0

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Publications (1)
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Bioz

Biological Activity

Description

IC₅₀ & Target^[1]^[2]

NK1R

All Neurokinin Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	0.87 nM Compound: 1	Displacement of [125I]- Substance P from human Neurokinin 1 (hNK1) receptor expressed in CHO cells Displacement of [125I]- Substance P from human Neurokinin 1 (hNK1) receptor expressed in CHO cells	10.1016/0960-894X(95)00009-I
CHO	IC₅₀	0.87 nM Compound: 4	Displacement of [125I]-labeled SP from human Tachykinin receptor 1 expressed in CHO cells Displacement of [125I]-labeled SP from human Tachykinin receptor 1 expressed in CHO cells	[PMID: 8627597]
CHO	IC₅₀	1 nM Compound: (+/-)2 (2S, 3S)	Compound was tested for the displacement of [ 1251] Substance P from hNK1 receptor in CHO cells Compound was tested for the displacement of [ 1251] Substance P from hNK1 receptor in CHO cells	10.1016/S0960-894X(01)80280-8
CHO	IC₅₀	1 nM Compound: 2	Ability to displace [125I]-substance P from hNK1 receptor in chinese hamster ovarian (CHO) cells Ability to displace [125I]-substance P from hNK1 receptor in chinese hamster ovarian (CHO) cells	[PMID: 9873445]
CHO	IC₅₀	1 nM Compound: 2	Binding affinity towards Neurokinin -1(NK-1) receptor of human by using [125I]- Tyr8 substance P as a radioligand in CHO cells Binding affinity towards Neurokinin -1(NK-1) receptor of human by using [125I]- Tyr8 substance P as a radioligand in CHO cells	10.1016/0960-894X(95)00220-N
CHO	IC₅₀	1 nM Compound: 4	Binding affinity at human tachykinin receptor 1 by measuring its ability to displace [125I]-labeled substance P from the cloned receptor expressed in CHO cells. Binding affinity at human tachykinin receptor 1 by measuring its ability to displace [125I]-labeled substance P from the cloned receptor expressed in CHO cells.	[PMID: 9804702]
CHO	IC₅₀	1 nM Compound: L-733060	Binding affinity for human NK1 receptor expressed in CHO cells Binding affinity for human NK1 receptor expressed in CHO cells	10.1016/S0960-894X(01)80585-0

Chemical Information

CAS No. 148700-85-0
Molecular Weight 403.36
Formula C₂₀H₁₉F₆NO
SMILES

FC(C1=CC(C(F)(F)F)=CC(CO[C@@H]2[C@H](C3=CC=CC=C3)NCCC2)=C1)(F)F
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Room temperature in continental US; may vary elsewhere.
Storage

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

Publications (1)

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Nat Commun

Optogenetic activation of mechanical nociceptions to enhance implant osseointegration. [Abstract]

2025 Mar 31;16(1):3093. PMID: 40164597

Purity & Documentation

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Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Langosch JM, et al. Effects of substance P and its antagonist L-733060 on long term potentiation in guinea pig hippocampal slices. Prog Neuropsychopharmacol Biol Psychiatry. 2005 Feb;29(2):315-9. [Content Brief]

[2]. Muñoz M, et, al. Antitumoral action of the neurokinin-1 receptor antagonist L-733 060 on human melanoma cell lines. Melanoma Res. 2004 Jun;14(3):183-8. [Content Brief]

[3]. SI-Yi Mo et al. Neuronal Activities in the Rostral Ventromedial Medulla Associated with Experimental Occlusal Interference-Induced Orofacial Hyperalgesia. J Neurosci. 2022 Jul 6;42(27):5314-5329. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
Chemical Information
Publications (1)
Purity & Documentation
References

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L-733060

Publications Citing Use of MedChemExpress (MCE) L-733060

All Neurokinin Receptor Isoforms