L-733060
Based on 2 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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 148700-85-0
- 分子式: C20H19F6NO
- 分子量:403.36
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 L-733060
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生物活性
製品説明
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NK1R |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.87 nM
Compound: 1
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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
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10.1016/0960-894X(95)00009-I |
| CHO | IC50 |
0.87 nM
Compound: 4
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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
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[PMID: 8627597] |
| CHO | IC50 |
1 nM
Compound: (+/-)2 (2S, 3S)
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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
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10.1016/S0960-894X(01)80280-8 |
| CHO | IC50 |
1 nM
Compound: 2
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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
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[PMID: 9873445] |
| CHO | IC50 |
1 nM
Compound: 2
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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
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10.1016/0960-894X(95)00220-N |
| CHO | IC50 |
1 nM
Compound: 4
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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.
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[PMID: 9804702] |
| CHO | IC50 |
1 nM
Compound: L-733060
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Binding affinity for human NK1 receptor expressed in CHO cells
Binding affinity for human NK1 receptor expressed in CHO cells
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10.1016/S0960-894X(01)80585-0 |
化学情報
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CAS 番号 148700-85-0
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分子量 403.36
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分子式 C20H19F6NO
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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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (2)
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Journal Impact Factor
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Most Recent
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Nat Commun
2025 Mar 31;16(1):3093. PMID: 40164597 -
Acta Pharmacol Sin
Enhanced substance P-NK1R signaling in the parabrachial-parasubthalamic pathway promotes hyperalgesia and affective aversion in neuropathic pain. [Abstract]2026 Aug 4. PMID: 42552466
純度とドキュメンテーション
参考文献
[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]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
L-733060 関連分類
HY-14406 関連分類
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