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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- CAS No.: 398507-81-8
- 화학식: C27H25Cl2F6N3O3
- 분자량:624.40
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보관:
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
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
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
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 398507-81-8
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분자량 624.40
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[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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