| Chemical Properties | Back Directory | [density ]
1.37±0.1 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
DMSO: soluble | [form ]
A solid | [pka]
14.18±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Diprovocim is a potent TLR1/TLR2 agonist. Diprovocim elicits full agonist activity in human THP-1 cells (EC50=110 pM). Diprovocim stimulates the release of TNF-α from mouse macrophages (EC50=1.3 nM). Diprovocim activates downstream MAPK and NF-κB signaling pathway. Diprovocim displays strong adjuvant activity in mice, particularly abetting cellular immune responses[1][2]. | [Biological Activity]
Diprovocim-1 is an agonist of the toll-like receptor 1/2 heterodimer.1 It induces TNF-α release in THP-1 cells (EC50 = 110 pM), an effect that can be inhibited by anti-TLR1 or anti-TLR2 antibodies. Diprovocim-1 (10 mg/kg) increases the production of ovalbumin-specific IgG1 in wild-type, but not TLR2-/-, mice sensitized to ovalbumin.2 It also enhances anti-PD-L1 antibody-induced activation of cytotoxic T lymphocytes, reduction of tumor growth, and increases in survival in a B16/F10 murine melanoma model. | [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[2].
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[2].
| Animal Model: | WT or Tlr2?/? C57BL/6J mice[2] | | Dosage: | 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.
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| [IC 50]
TLR1; TLR2; p38 MAPK; NF-κB | [References]
1.Morin, M.D., Wang, Y., Jones, B.T., et al.Diprovocims: A new and exceptionally potent class of toll-like receptor agonistsJ. Am. Chem. Soc.140(43)14440-14454(2018)
2.Wang, Y., Su, L., Morin, M.D., et al.Adjuvant effect of the novel TLR1/TLR2 agonist Diprovocim synergizes with anti-PD-L1 to eliminate melanoma in miceProc. Natl. Acad. Sci. U.S.A.115(37)E8698-E8706(2018)
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| Company Name: |
ChemeGen 中国
|
| Tel: |
18818260767 |
| Website: |
https://www.chemegen.com |
| Company Name: |
Merck KGaA
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| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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