Niflumic Acid-d5
Niflumic Acid-d5 is the deuterium labeled Niflumic acid. Niflumic acid, a Ca2+-activated Cl- channel blocker, is an analgesic and anti-inflammatory agent used in the treatment of rheumatoid arthritis.
For research use only. We do not sell to patients.
- CAS No.: 1794811-58-7
- Formula: C13H4D5F3N2O2
- Molecular Weight:287.25
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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 |
|---|---|---|---|---|
| Bone marrow cell | EC50 |
>20 μM
Compound: Niflumic acid
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Induction of bone marrow cell differentiation isolated from ER-HOXA9 fusion protein expressed mouse harboring GFP-lysozyme assessed as upregulation of CD11b/MAC1 after 4 days by flow cytometry
Induction of bone marrow cell differentiation isolated from ER-HOXA9 fusion protein expressed mouse harboring GFP-lysozyme assessed as upregulation of CD11b/MAC1 after 4 days by flow cytometry
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[PMID: 27994748] |
| CHO | EC50 |
30.8 μM
Compound: 8
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Agonist activity at C-terminal beta-galactosidase tagged human recombinant GPR35 expressed in CHO cells after 90 mins by beta-arrestin recruitment assay
Agonist activity at C-terminal beta-galactosidase tagged human recombinant GPR35 expressed in CHO cells after 90 mins by beta-arrestin recruitment assay
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[PMID: 23888932] |
| HEK293 | IC50 |
13 μM
Compound: Niflumic acid
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Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS method
Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS method
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[PMID: 21030469] |
| HEK293 | IC50 |
53 μM
Compound: Niflumic acid
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Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS method
Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS method
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[PMID: 21030469] |
| HEK-293T | EC50 |
15 μM
Compound: 8
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Agonist activity at human GPR35 expressed in HEK293T cells at 5 uM by EYPF-based beta-arrestin-2 luciferase reporter gene assay
Agonist activity at human GPR35 expressed in HEK293T cells at 5 uM by EYPF-based beta-arrestin-2 luciferase reporter gene assay
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[PMID: 23888932] |
| HT-29 | EC50 |
1.15 μM
Compound: Niflumic acid
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Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay
Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay
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[PMID: 24900447] |
| HT-29 | IC50 |
1.28 μM
Compound: Niflumic acid
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Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins
Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins
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[PMID: 24900447] |
| THP-1 | EC50 |
>20 μM
Compound: Niflumic acid
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Induction of human THP1 cell differentiation after 4 days by flow cytometry
Induction of human THP1 cell differentiation after 4 days by flow cytometry
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[PMID: 27994748] |
| U2OS | EC50 |
40.2 μM
Compound: Niflumic acid
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Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay
Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay
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[PMID: 24900447] |
| U-937 | EC50 |
>20 μM
Compound: Niflumic acid
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Induction of human U937 cell differentiation after 4 days by flow cytometry
Induction of human U937 cell differentiation after 4 days by flow cytometry
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[PMID: 27994748] |
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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CAS No. 1794811-58-7
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Unlabeled Cas 4394-00-7
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Molecular Weight 287.25
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Formula C13H4D5F3N2O2
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SMILES
N(C1=C(C(O)=O)C(=C(C(=N1)[2H])[2H])[2H])C2=CC(C(F)(F)F)=CC(=C2[2H])[2H]
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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]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [Content Brief]
[2]. Criddle, D.N., et al., Inhibitory action of niflumic acid on noradrenaline- and 5-hydroxytryptamine-induced pressor responses in the isolated mesenteric vascular bed of the rat. Br J Pharmacol, 1997. 120(5): p. 813-8. [Content Brief]
[3]. Jabeen, T., et al., Non-steroidal anti-inflammatory drugs as potent inhibitors of phospholipase A2: structure of the complex of phospholipase A2 with niflumic acid at 2.5 Angstroms resolution. Acta Crystallogr D Biol Crystallogr, 2005. 61(Pt 12): p. 1579-86. [Content Brief]
[4]. Picollo, A., et al., Mechanism of interaction of niflumic acid with heterologously expressed kidney CLC-K chloride channels. J Membr Biol, 2007. 216(2-3): p. 73-82. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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