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.
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- No. CAS: 398507-81-8
- Fòrmula: C27H25Cl2F6N3O3
- Peso molecular:624.40
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
Descripciòn
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.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 398507-81-8
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Peso molecular 624.40
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DNK-333 Related Classifications
HY-128537 Related Classifications
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