Diprovocim-1是一种TLR1/TLR2激动剂，在THP-1细胞和小鼠巨噬细胞中的EC50值分别为0.11nM和1.3nM。
Cas No.:2170867-89-5
Sample solution is provided at 25 µL, 10mM.
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Diprovocim-1 is a TLR1/TLR2 agonist, with EC50 values of 0.11nM and 1.3nM in THP-1 cells and mouse macrophages, respectively[1]. Diprovocim-1 induces the formation of TLR2/TLR1 heterodimers as well as TLR2 homodimers in vitro[2]. Diprovocim-1 has been widely used as an adjuvant in combination with anti-PD-L1 therapy to eliminate melanoma in mice[3].
In vitro, Diprovocim-1 treatment (10nM) for 4h significantly enhanced the levels of tumor necrosis factor (TNF) in mouse peritoneal macrophages [4].
In vivo, a single intraperitoneal injection of Diprovocim-1 (10mg/kg) and ovalbumin (OVA) (5mg/kg) for 14 days significantly increased the levels of OVA-specific circulating antibodies of different subtypes in serum of C57BL/6J mice[5]. Diprovocim-1 (10mg/kg) administered intraperitoneally to C57BL/6 mice at 18h and 2h before 12Gy total body irradiation (TBI) significantly ameliorated radiation-induced intestinal injury, reduced leukocyte loss, and alleviated body weight loss[6].
References:
[1] Morin M D, Wang Y, Jones B T, et al. Diprovocims: a new and exceptionally potent class of toll-like receptor agonists[J]. Journal of the American Chemical Society, 2018, 140(43): 14440-14454.
[2] Su L, Wang Y, Wang J, et al. Structural basis of TLR2/TLR1 activation by the synthetic agonist diprovocim[J]. Journal of medicinal chemistry, 2019, 62(6): 2938-2949.
[3] Hu H G, Li Y M. Emerging adjuvants for cancer immunotherapy[J]. Frontiers in Chemistry, 2020, 8: 601.
[4] 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 mice[J]. Proceedings of the National Academy of Sciences, 2018, 115(37): E8698-E8706.
[5] Yang M H, Russell J L, Mifune Y, et al. Next-generation diprovocims with potent human and murine TLR1/TLR2 agonist activity that activate the innate and adaptive immune response[J]. Journal of medicinal chemistry, 2022, 65(13): 9230-9252.
[6] Fang D, Zhao H, Pei L, et al. Diprovocim protects against the radiation-induced damage via the TLR2 signaling pathway[J]. Molecular Medicine, 2025, 31(1): 139.
Diprovocim-1是一种TLR1/TLR2激动剂，在THP-1细胞和小鼠巨噬细胞中的EC50值分别为0.11nM和1.3nM[1]。Diprovocim-1可在体外诱导TLR2/TLR1异源二聚体及TLR2同源二聚体的形成[2]。Diprovocim-1已广泛作为佐剂与抗PD-L1疗法联用，在小鼠模型中实现黑色素瘤的清除[3]。
在体外，使用10nM的Diprovocim-1处理小鼠腹腔巨噬细胞4小时，能显著提升肿瘤坏死因子(TNF)水平[4]。
在体内，单次腹腔注射Diprovocim-1(10mg/kg)与卵清蛋白(OVA)(5mg/kg)14天后，可显著提高C57BL/6J小鼠血清中OVA特异性循环抗体各亚型的水平[5]。在全身辐射(TBI)前18小时和2小时对C57BL/6小鼠腹腔注射Diprovocim-1(10mg/kg)，能显著改善辐射诱导的肠道损伤，减少白细胞损失，并缓解体重下降[6]。
| Cell experiment [1]: | |
Cell lines | Mouse peritoneal macrophages |
Preparation Method | Mouse peritoneal macrophages were cultured in DMEM medium containing 10% v/v fetal bovine serum (1% v/v penicillin and streptomycin) at 37°C in 95% air /5% CO2. Cells were seeded in 96-well plates at a density of 1×105 cells per well and stimulated with Diprovocim-1 (0.01, 0.1, 1, 10, and 100nM) for 4 hours. Levels of TNF in cells were measured. |
Reaction Conditions | 0.01, 0.1, 1, 10, and 100nM; 4h |
Applications | Diprovocim-1 treatment significantly enhanced the levels of TNF of mouse peritoneal macrophages in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Female C57BL/6J mice |
Preparation Method | Female 8-week-old C57BL/6J mice (approximately 20g) were intravenously injected with vehicle (DMSO:Tween 80:saline = 1:1:8) on day 0. Saline = 1:1:1.8) (n=8), vehicle mixed with OVA (5mg/kg) (n=8), or OVA (5mg/kg) was further mixed with Diprovocim-1 (10mg/kg) (n=8) per mouse. On day 14, the titers of OVA-specific IgG, IgG1, or IgG2b in the serum of the mice were measured. |
Dosage form | 10mg/kg for once; i.p. |
Applications | Diprovocim-1 treatment enhanced the levels of OVA-specific IgG, IgG1, or IgG2b in the mice. |
References: | |
| Cas No. | 2170867-89-5 | SDF | |
| Canonical SMILES | O=C(C1=CC=C(C=C1)C(N2C[C@@H](C(N[C@@H]3[C@](C4=CC=CC=C4)([H])C3)=O)[C@H](C(N[C@@H]5[C@](C6=CC=CC=C6)([H])C5)=O)C2)=O)N7C[C@@H](C(N[C@@H]8[C@](C9=CC=CC=C9)([H])C8)=O)[C@H](C(N[C@@H]%10[C@](C%11=CC=CC=C%11)([H])C%10)=O)C7 | ||
| 分子式 | C56H56N6O6 | 分子量 | 909.1 |
| 溶解度 | DMSO : 33.33 mg/mL (36.66 mM; ultrasonic and warming and heat to 60°C); H2O : < 0.1 mg/mL (insoluble) | 储存条件 | -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.1 mL | 5.4999 mL | 10.9999 mL |
| 5 mM | 220 μL | 1.1 mL | 2.2 mL |
| 10 mM | 110 μL | 550 μL | 1.1 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.50% Appearance: A solid
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