NVP-QAV680
NVP-QAV680 is a potent and selective CRTh2 receptor antagonist with low nanomolar (nM) functional potency to inhibit CRTh2-driven activation of human eosinophils and Th2 lymphocytes. NVP-QAV680 exhibits good oral bioavailability and demonstrates efficacy in CRTh2-dependent mechanisms and allergic disease models in rats.
For research use only. We do not sell to patients.
- CAS No.: 872365-16-7
- Formula: C18H18N2O4S
- Molecular Weight:358.41
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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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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.037 μM
Compound: 18
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Antagonist activity at human CRTh2 receptor expressed in CHO cells assessed as inhibition of prostaglandin D2 and forskolin-induced cAMP accumulation after 45 mins
Antagonist activity at human CRTh2 receptor expressed in CHO cells assessed as inhibition of prostaglandin D2 and forskolin-induced cAMP accumulation after 45 mins
|
[PMID: 24021582] |
| CHO-K1 | IC50 |
0.094 μM
Compound: 18
|
Antagonist activity at mouse CRTh2 receptor expressed in CHO-K1 cells assessed as inhibition of [125S]-GTP-gamma-S binding after 50 mins by liquid scintillation counting
Antagonist activity at mouse CRTh2 receptor expressed in CHO-K1 cells assessed as inhibition of [125S]-GTP-gamma-S binding after 50 mins by liquid scintillation counting
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[PMID: 24021582] |
Chemical Information
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CAS No. 872365-16-7
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Molecular Weight 358.41
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Formula C18H18N2O4S
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SMILES
O=C(O)CC1=C(C)N(CC2=CC=C(S(=O)(C)=O)C=C2)C3=NC=CC=C31
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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]. Discovery and characterization of NVP-QAV680, a potent and selective CRTh2 receptor antagonist suitable for clinical testing in allergic diseases [Content Brief]
[2]. Sandham DA, et al. Discovery and characterization of NVP-QAV680, a potent and selective CRTh2 receptor antagonist suitable for clinical testing in allergic diseases. Bioorg Med Chem. 2013 Nov 1;21(21):6582-91. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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