Shanghai Nianxing Industrial Co., Ltd
China
Product Name: Furamidine-D8
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Purity: 95.0%
Stocking Period: 10 Day
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336786-81-3

336786-81-3 structure

Name: Furamidine-d8
Chemical Name: Furamidine-d8
CAS Number: 336786-81-3
Molecular Formula: C₁₈H₈D₈N₄O
Molecular Weight: 312.40
Catalog: Signaling Pathways Epigenetics Histone Methyltransferase
Create Date: 2021-11-03 09:23:29
Modify Date: 2024-01-09 09:45:43
Furamidine-d8 (DB75-d8) is the deuterium labeled Furamidine. Furamidine (DB75) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine is also an antiparasite agent[1][2][3].

Name	Furamidine-d8

Description	Furamidine-d8 (DB75-d8) is the deuterium labeled Furamidine. Furamidine (DB75) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine is also an antiparasite agent[1][2][3].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE) Research Areas >> Infection Signaling Pathways >> Epigenetics >> Histone Methyltransferase Research Areas >> Inflammation/Immunology
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].
References	[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. Yan L, et al. Diamidine compounds for selective inhibition of protein arginine methyltransferase 1. J Med Chem. 2014 Mar 27;57(6):2611-22. [3]. Antony S, et al. Novel high-throughput electrochemiluminescent assay for identification of human tyrosyl-DNA phosphodiesterase (Tdp1) inhibitors and characterization of furamidine (NSC 305831) as an inhibitor of Tdp1. Nucleic Acids Res. 2007;35(13):4474-84. [4]. Keil A, et al. The Topoisomerase I Inhibitor Irinotecan and the Tyrosyl-DNA Phosphodiesterase 1 Inhibitor Furamidine Synergistically Suppress Murine Lupus Nephritis. Arthritis Rheumatol. 2015 Jul;67(7):1858-67.

Molecular Formula	C₁₈H₈D₈N₄O
Molecular Weight	312.40

Hazard Codes	Xi

336786-81-3	55368-40-6
73819-26-8	1265295-16-6
1624587-87-6	1794760-48-7
1538624-35-9	1092804-88-0
35434-71-0	2037-26-5