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PD 404182

Names

[ CAS No. ]:
72596-74-8

[ Name ]:
PD 404182

[Synonym ]:
3,4-dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine
PD 404,182
6H-6-Imino-(2,3,4,5-tetrahydropyrimido)[1,2-c]-[1,3]benzothiazine
Lopac-P-2742

Biological Activity

[Description]:

PD 404182 is a potent and competitive inhibitor of human dimethylarginine dimethylaminohydrolase 1 (DDAH1), with an IC50 of 9 μM. PD 404182 exhibits antiangiogenic and antiviral activity in vitro[1][2].

[Related Catalog]:

Signaling Pathways >> Others >> Others
Research Areas >> Inflammation/Immunology

[Target]

IC50: 9 μM (DDAH1)[1]


[In Vitro]

PD 404182 (20 μM) increases asymmetric dimethylarginine (ADMA) approximately 70% in ECs[1]. PD 404182 (50-100 μM; 18 hours) attenuates endothelial tube formation in virto and does not perturb cell membrane integrity or induces cytotoxicity[1]. PD 404182 inhibits HIV-1 in seminal plasma, with an IC50 of 1 μM[2]. PD 404182 (300 μM;30 minutes) exhibits low toxicity toward several human cell lines , freshly activated PBMCs, primary CD4+ T lymphocytes, macrophages, and dendritic cells, and lactobacilli found in the normal vaginal flora[2]. Cell Viability Assay[1] Cell Line: Human dermal microvascular endothelial cells (ECs) Concentration: 10-300 μM Incubation Time: 24 hours Result: Did not induce cytotoxicity.

[References]

[1]. Ghebremariam YT, et, al. A novel and potent inhibitor of dimethylarginine dimethylaminohydrolase: a modulator of cardiovascular nitric oxide. J Pharmacol Exp Ther. 2014 Jan; 348(1): 69-76.

[2]. Chamoun-Emanuelli AM, et, al. Evaluation of PD 404,182 as an anti-HIV and anti-herpes simplex virus microbicide. Antimicrob Agents Chemother. 2014; 58(2): 687-97.

Chemical & Physical Properties

[ Molecular Formula ]:
C11H11N3S

[ Molecular Weight ]:
217.29000

[ Exact Mass ]:
217.06700

[ PSA ]:
69.38000

[ LogP ]:
1.02200

MSDS

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H315-H319-H335

[ Precautionary Statements ]:
P261-P305 + P351 + P338

[ Personal Protective Equipment ]:
dust mask type N95 (US);Eyeshields;Gloves

[ RIDADR ]:
NONH for all modes of transport

Synthetic Route

Precursor & DownStream


Related Compounds