DNK-333
DNK-333 is a potent and balanced dual NK1 and NK2 receptor antagonist with IC50 values of 4.8 nM and 5.5 nM, respectively. DNK-333 blocks the Neurokinin A (NKA) (HY-P0197)-induced bronchoconstriction in asthma.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 398507-81-8
- Formel: C27H25Cl2F6N3O3
- Molecular Weight:624.40
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
NK1R 9.2 (pkB) |
NK2R 7.43 (pkB) |
hNK1 4.8 nM (IC50) |
hNK2 5.5 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
5.5 nM
Compound: 9 (DNK333)
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In vitro binding affinity for Tachykinin receptor 2 of human-CHO cells using 125 I-NKA radioligand
In vitro binding affinity for Tachykinin receptor 2 of human-CHO cells using 125 I-NKA radioligand
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[PMID: 11714615] |
In Vitro
DNK-333 exhibits potent and reversible NK1 and NK2 receptor antagonist activities in this assay, with pKb values of 9.2 and 7.43, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 398507-81-8
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Molecular Weight 624.40
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Formel C27H25Cl2F6N3O3
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SMILES
O=C(N([C@H](CC1=CC(Cl)=C(Cl)C=C1)/C=C/C(N[C@H]2C(NCCCC2)=O)=O)C)C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Swarna VM, et al. Design and synthesis of 3,5-disubstituted benzamide analogues of DNK333 as dual NK1/NK2 receptor probes. Bioorg Med Chem Lett. 2007 Feb 15;17(4):890-4. [Content Brief]
[2]. Schelfhout V, et al. The triple neurokinin-receptor antagonist CS-003 inhibits neurokinin A-induced bronchoconstriction in patients with asthma. Pulm Pharmacol Ther. 2006;19(6):413-8. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
DNK-333 Related Classifications
HY-128537 Related Classifications
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