SDZ NKT 343
SDZ NKT 343 is a selective, orally active NK1 receptor antagonist with an IC50 of 0.62 nM against human NK1 receptor. SDZ NKT 343 has good analgesic activity.
For research use only. We do not sell to patients.
- CAS No.: 180046-99-5
- Formula: C33H33N5O5
- Molecular Weight:579.65
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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hNK1 0.62 nM (IC50) |
hNK2 0.52 μM (Ki) |
hNK3 3.4 μM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| COS-7 | IC50 |
82.4 μM
Compound: 5k
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In vitro binding affinity towards Tachykinin receptor 1 by measuring its ability to displace [3H]SP (0.6 nM) binding to membranes from Cos-7 cells transiently transfected with the hNK-1R
In vitro binding affinity towards Tachykinin receptor 1 by measuring its ability to displace [3H]SP (0.6 nM) binding to membranes from Cos-7 cells transiently transfected with the hNK-1R
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[PMID: 9703462] |
SDZ NKT 343 shows a markedly lower affinity at rat NK1 receptors in whole forebrain membranes (IC50=451+139 nM)[1].
SDZ NKT 343 shows weak affinity to human NK2 and NK3 receptors in transfected Cos-7 cells (Ki of 0.52+0.04 μM and 3.4+1.2 μM respectively)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 180046-99-5
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Molecular Weight 579.65
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Formula C33H33N5O5
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SMILES
O=C(NC([C@H]1N(C(NC2=CC=CC=C2[N+]([O-])=O)=O)CCC1)=O)[C@H](CC3=CC=C4C=CC=CC4=C3)N(C)CC5=CC=CC=C5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Walpole CS, et al. Comparative, general pharmacology of SDZ NKT 343, a novel, selective NK1 receptor antagonist. Br J Pharmacol. 1998 May;124(1):83-92. [Content Brief]
[2]. Walpole C, et al. 2-Nitrophenylcarbamoyl-(S)-prolyl-(S)-3-(2-naphthyl)alanyl-N-benzyl-N - methylamide (SDZ NKT 343), a potent human NK1 tachykinin receptor antagonist with good oral analgesic activity in chronic pain models. J Med Chem. 1998 Aug 13;41(17) [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SDZ NKT 343 Related Classifications
HY-108480 Related Classifications
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