Diprovocim is a potent TLR1/TLR2 agonist. Diprovocim elicits full agonist activity in human THP-1 cells (EC 50 =110 pM). Diprovocim stimulates the release of TNF-α from mouse macrophages (EC 50 =1.3 nM). Diprovocim activates downstream MAPK and NF-κB signaling pathway. Diprovocim displays strong adjuvant activity in mice, particularly abetting cellular immune responses In Vitro Diprovocim (5 nM in THP-1 and 500 nM in mouse peritoneal macrophage; 15-120 mins) induces phosphorylation of IKKα, IKKβ, p38, JNK, and ERK, as well as degradation of IκBα in THP-1 cells and mouse peritoneal macrophages. Diprovocim (0.01-10000 nM; 4 hours) induces dose-dependent TNF production by THP-1 cells (EC 50 =110 pM) and human peripheral blood mononuclear cells (PBMC) (EC 50 =875 pM) and by mouse peritoneal macrophages (EC 50 =1.3 nM) and bone marrow-derived dendritic cells (BMDC) (EC 50 =6.7 nM). In addition to TNF, Diprovocim induced IL-6 production by mouse BMDC. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: THP-1 cells and mouse peritoneal macrophages Concentration: 5 nM in THP-1 and 500 nM in mouse peritoneal macrophages Incubation Time: 15, 30, 60, 120 mins Result: Induced phosphorylation of IKKα, IKKβ, p38, JNK, and ERK, as well as degradation of IκBα. In Vivo Diprovocim (10 mg/kg) uses as an adjuvant and mixed with ovalbumin (OVA; 100 μg) by i.m. induces similar levels of serum OVA-specific IgG after 14 days. Diprovocim (10 mg/kg; i.m.) mixed with ovalbumin (OVA; 100 μg) before inoculation with B16-OVA cells immunizes significantly slows tumor growth rate but failed to prolong survival relative to OVA alone after 7 days. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: WT or Tlr2 −/− C57BL/6J miceDosage: 10 mg/kg Administration: IM Result: Induced similar levels of serum OVA-specific IgG, which were highly elevated compared with levels induced by immunization with OVA plus vehicle by i.m. with 100 μg OVA mixed with this drug. Form:Solid IC50& Target:TLR1|TLR2|p38 MAPK|NF-κB
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Diprovocim
CAS number：2170867-89-5 molecular formula：C56H56N6O6
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| Chinese alias | 迪普罗沃辛 | ||
| English alias | - | ||
| CAS number | 2170867-89-5 | molecular formula | C56H56N6O6 |
| molecular weight | 909.08 g/mol | Exact mass | ≥98% |
| PSA | 157.000 Ų | logp | 5.300 |
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