NVP CXCR2 20
NVP CXCR2 20 is a selective CXCR2 inhibitor with analgesic and antinociceptive activities. NVP CXCR2 20 selectively blocks CXCR2 signaling and attenuates mechanical and thermal hypersensitivity in rat chronic constriction injury (CCI) models. NVP CXCR2 20 inhibits CXCL3-induced hypersensitivity in naive mice and reduces elevated CXCL3 protein levels in the spinal cord and dorsal root ganglia (DRG) of CCI-exposed rats. NVP CXCR2 20 can be used for the research of neuropathic pain and chronic obstructive pulmonary disease (COPD).
For research use only. We do not sell to patients.
- CAS No.: 1029521-30-9
- Formula: C15H11F2N3OS
- Molecular Weight:319.33
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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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CXCR2 4.9 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
0.04 μM
Compound: 20
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Displacement of [125I]-GRO-alpha from human recombinant CXCR2 receptor expressed in CHO cell membranes
Displacement of [125I]-GRO-alpha from human recombinant CXCR2 receptor expressed in CHO cell membranes
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[PMID: 24974342] |
| CHO | IC50 |
0.14 μM
Compound: 20
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Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
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[PMID: 24974342] |
NVP CXCR2 20 (100 nM; 30 min pre-incubation, 24 h with LPS) reduces LPS-induced CXCL1, CXCL2, and CXCL3 protein expression in primary rat microglial cell cultures and astroglial cell cultures[1].
NVP CXCR2 20 (0.0005–10 μM) binds to human recombinant CXCR2 in CHO membranes with an IC50 of 0.04 μM and acts as a functional CXCR2 antagonist with an [35S]-GTPγS IC50 of 0.14 μM; it shows a cLogP of 3.9 and a functional ligand-lipophilicity efficiency (LLE) of 3.0[3].
NVP CXCR2 20 (10 μM) is selective for CXCR2, with no significant inhibitory activity (IC50 > 10 μM) against a panel of 49 other GPCRs[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
NVP CXCR2 20 (10 μg/5 μL; intrathecal; single dose on day 7 post-CCI, 4 hours prior to opioid co-administration) produces analgesic effects[1].
NVP CXCR2 20 (60 μg/5 μL; intrathecal; single dose, 2 hours prior to intrathecal CXCL3) prevents CXCL3-induced mechanical and thermal hypersensitivity in naive mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar rats (male, adult, 250-300 g, chronic constriction injury of the sciatic nerve with intrathecal catheter implantation 7 days prior)[1]
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Dosage:10 μg/5 μL (repeated administration); 20 μg/5 μL (single administration); 30 μg/5 μL (single administration)
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Administration:intrathecal; single dose (single treatment); 16 h and 1 h post-CCI, then once daily for 7 days (repeated treatment)
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Result:Produced significant analgesic effects on mechanical and thermal hypersensitivity at 2, 4, and 6 h after single administration (20 and 30 μg/5 μL).
Reduced mechanical hypersensitivity and thermal hypersensitivity after repeated dosing (10 μg/5 μL).
Normalized elevated CXCL3 protein in spinal cord and DRG to naive levels.
Did not affect CCI-induced spinal IBA1 (microglia) or GFAP (astroglia) upregulation.
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Animal Model:Wistar rats (male, adult, 250-300 g, chronic constriction injury of the sciatic nerve with intrathecal catheter implantation 7 days prior)[1]
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Dosage:10 μg/5 μL
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Administration:intrathecal; single dose (day 7 post-CCI, 4 hours prior to opioid co-administration)
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Result:Produced analgesic effects similar to single doses of morphine or buprenorphine in the von Frey and cold plate tests.
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Animal Model:Albino Swiss mice (20-22 g)[1]
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Dosage:60 μg/5 μL
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Administration:intrathecal; single dose, 2 hours prior to intrathecal CXCL3
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Result:Completely prevented the mechanical and thermal hypersensitivity induced by CXCL3 in naive mice at all tested time points (1.5, 5, and 24 hours post-CXCL3 administration).
Chemical Information
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CAS No. 1029521-30-9
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Molecular Weight 319.33
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Formula C15H11F2N3OS
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SMILES
N#CC=1C(=O)N=C(SCC=2C=CC=C(F)C2F)NC1C3CC3
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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]. Piotrowska A, et al. Pharmacological Blockade of Spinal CXCL3/CXCR2 Signaling by NVP CXCR2 20, a Selective CXCR2 Antagonist, Reduces Neuropathic Pain Following Peripheral Nerve Injury. Front Immunol. 2019;10:2198. Published 2019 Sep 26. [Content Brief]
[3]. Porter DW, et al. The discovery of potent, orally bioavailable pyrimidine-5-carbonitrile-6-alkyl CXCR2 receptor antagonists. Bioorg Med Chem Lett. 2014;24(15):3285-3290. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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