生物活性：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].
细胞效力(Cellular Effect)
Bone marrow cellCHOHEK293HEK-293THT-29THP-1U2OSU-937
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]
体外研究(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].
瑞禧生物 has not independently confirmed the accuracy of these methods. They are for reference only.
Niflumic Acid-d5 相关抗体:
Anoctamin 1 Antibody
CLIC4 Antibody (YA2517)
CLIC1 Antibody (YA2807)
分子量：287.25
Formula：C13H4D5F3N2O2
CAS 号：1794811-58-7
非标记 CAS：4394-00-7
中文名称：尼氟灭酸 d5
运输条件：Room temperature in continental US; may vary elsewhere.
储存方式：Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
Data Sheet (527 KB)
产品使用指南 (1538 KB)
参考文献
[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]