NVP-QAV680 - CAS 872365-16-7
Catalog number: 872365-16-7
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
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Molecular Weight:
CRTh2 antagonist
NVP-QAV680 is a potent and selective CRTh2 receptor antagonist with Ki of 36 nM by 3H-PGD2 filtration binding assay.
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1.Discovery and characterization of NVP-QAV680, a potent and selective CRTh2 receptor antagonist suitable for clinical testing in allergic diseases.
Sandham DA1, Arnold N, Aschauer H, Bala K, Barker L, Brown L, Brown Z, Budd D, Cox B, Docx C, Dubois G, Duggan N, England K, Everatt B, Furegati M, Hall E, Kalthoff F, King A, Leblanc CJ, Manini J, Meingassner J, Profit R, Schmidt A, Simmons J, Sohal B, S Bioorg Med Chem. 2013 Nov 1;21(21):6582-91. doi: 10.1016/j.bmc.2013.08.025. Epub 2013 Aug 22.
Optimization of a 7-azaindole-3-acetic acid CRTh2 receptor antagonist chemotype derived from high throughput screening furnished a highly selective compound NVP-QAV680 with low nM functional potency for inhibition of CRTh2 driven human eosinophil and Th2 lymphocyte activation in vitro. The molecule exhibited good oral bioavailability in the rat, combined with efficacy in rodent CRTh2-dependent mechanistic and allergic disease models and was suitable for clinical development.
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CAS 872365-16-7 NVP-QAV680

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