SM-276001

Research use only, not for human use.

SM-276001 is a potent selective agonist of TLR7,and is an orally active interferon (IFN) inducer.

SM-276001 is a potent selective agonist of TLR7,and is an orally active interferon (IFN) inducer.(In Vitro):HEK-293 cells were engineered to report NF-κB activation following agonism of human TLR7, TLR8, and TLR9. SM-276001, a well-characterized human TLR7/8 dual agonist, dose-dependently activated NF-κB through human TLR7 .(In Vivo):Oral administration of 0.1 mg/kg SM-276001 in mice shows potent IFN-inducing activity . Twice weekly oral administration of SM-276001 at a dose of 3 mg/kg significantly reduced disease burden in mice bearing either Renca or CT26 tumors.

SM-276001 (1 nM-10 μM) dose-dependently activates NF-κB through human TLR7.

SM-276001 demonstrates potent IFN-inducing activity at a dose of 0.1 mg/kg by oral administration in mice. Oral administration of SM-276001, leads to the induction of an inflammatory cytokine and chemokine milieu and to the activation of a diverse population of immune effector cells including T and B lymphocytes, NK and NKT cells. SM-276001 (3 mg/kgPO biweekly) significantly inhibits tumor growth in the Renca renal cell cancer and CT26 colorectal models. SM-276001 (orally; 0.1, 1 or 10 mg/kg) leads to the activation of a diverse population of spleen-resident immune effector cells in Balb/c and C57BL/6J mice. When administered at 1 mg/kg or greater, the plasma concentration of SM-276001 exceeds the MEC of 30 nM. Animal Model:C57BL/6 and B6C3F1 mice bearing Renca or CT26 tumorsDosage:3 mg/kg Administration:Oral administration twice weekly for 25 days Result:Significantly reduced disease burden in mice bearing either Renca or CT26 tumors.

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Immunology/Inflammation

TLR

COX-1| COX-2

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473930-22-2

327.392

C16H21N7O

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (381.82 mM)

CCCCNc1nc(N)c2[nH]c(=O)n(Cc3ccc(C)nc3)c2n1

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(-20℃)

With Ice Pack

≥ 2 years