Niflumic Acid-d₅

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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[1][2].

For research use only. We do not sell to patients.

Niflumic Acid-d<sub>5</sub> Chemical Structure

Niflumic Acid-d₅ Chemical Structure

CAS No. : 1794811-58-7

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Other Forms of Niflumic Acid-d₅:

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Biological Activity
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References
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
Bone marrow cell	EC₅₀	> 20 μM Compound: Niflumic acid	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	[PMID: 27994748]
CHO	EC₅₀	30.8 μM Compound: 8	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	[PMID: 23888932]
HEK293	IC₅₀	13 μM Compound: Niflumic acid	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	[PMID: 21030469]
HEK293	IC₅₀	53 μM Compound: Niflumic acid	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	[PMID: 21030469]
HEK-293T	EC₅₀	15 μM Compound: 8	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	[PMID: 23888932]
HT-29	EC₅₀	1.15 μM Compound: Niflumic acid	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	[PMID: 24900447]
HT-29	IC₅₀	1.28 μM Compound: Niflumic acid	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	[PMID: 24900447]
THP-1	EC₅₀	> 20 μM Compound: Niflumic acid	Induction of human THP1 cell differentiation after 4 days by flow cytometry Induction of human THP1 cell differentiation after 4 days by flow cytometry	[PMID: 27994748]
U2OS	EC₅₀	40.2 μM Compound: Niflumic acid	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	[PMID: 24900447]
U-937	EC₅₀	> 20 μM Compound: Niflumic acid	Induction of human U937 cell differentiation after 4 days by flow cytometry Induction of human U937 cell differentiation after 4 days by flow cytometry	[PMID: 27994748]

In Vitro

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.

Molecular Weight

287.25

Formula

C₁₃H₄D₅F₃N₂O₂

CAS No.

1794811-58-7

Unlabeled CAS

4394-00-7

SMILES

N(C1=C(C(O)=O)C(=C(C(=N1)[2H])[2H])[2H])C2=CC(C(F)(F)F)=CC(=C2[2H])[2H]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

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- [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]