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Gardiquimod

Names

[ CAS No. ]:
1020412-43-4

[ Name ]:
Gardiquimod

[Synonym ]:
Gardiquimod
gardiquimod

Biological Activity

[Description]:

Gardiquimod, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod specifically activates TLR7 when used at concentrations below 10 μM[1][2].

[Related Catalog]:

Signaling Pathways >> Immunology/Inflammation >> Toll-like Receptor (TLR)
Research Areas >> Cancer
Signaling Pathways >> Anti-infection >> HIV
Research Areas >> Infection

[Target]

TLR7

TLR8

HIV-1


[In Vitro]

Gardiquimod (6-60 μM ) significantly inhibits cDNA synthesis by HIV-1 reverse transcriptase[1].

[In Vivo]

Dendritic cells (DCs) in combination with Gardiquimod (1 mg/kg per mouse; i.p.; daily for 7 days) improves the anti-tumor effects of NK cells[2]. Animal Model: Male athymic nude mice (Balb-nu/nu, 5 weeks old) (bearing human HepG2 liver carcinoma xenografts)[2] Dosage: 1 mg/kg per mouse Administration: i.p.; daily for 7 days Result: Significantly suppressed the growth of human HepG2 liver carcinoma xenografts.

[References]

[1]. Buitendijk M, et al. Gardiquimod: a Toll-like receptor-7 agonist that inhibits HIV type 1 infection of human macrophages and activated T cells. AIDS Res Hum Retroviruses. 2013 Jun;29(6):907-18.

[2]. Zhou Z, et al. TLR7/8 agonists promote NK-DC cross-talk to enhance NK cell anti-tumor effects in hepatocellular carcinoma. Cancer Lett. 2015 Dec 28;369(2):298-306.

Chemical & Physical Properties

[ Molecular Formula ]:
C17H23N5O

[ Molecular Weight ]:
313.39700

[ Exact Mass ]:
313.19000

[ PSA ]:
88.99000

[ LogP ]:
3.01920

[ Storage condition ]:
20°C

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H315-H319-H335

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

[ Hazard Codes ]:
Xi

[ RIDADR ]:
NONH for all modes of transport

Related Compounds