Nangibotide TFA (Synonyms: LR12 TFA) |
Katalog-Nr.GC63949
One-Click Copy Product Info
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Nangibotide TFA ist ein TREM-1-Rezeptor-Inhibitor, der die angeborene Immunantwort modulieren kann.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2014384-91-7
Sample solution is provided at 25 µL, 10mM.
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Nangibotide TFA is a synthetic peptide and TREM-1 receptor inhibitor[1]. TREM-1 (Triggering Receptor Expressed on Myeloid Cells-1) is an immune receptor belonging to the immunoglobulin superfamily, primarily expressed on the surface of myeloid cells such as monocytes, macrophages, and neutrophils[2]. This receptor plays a crucial role in amplifying inflammatory responses, significantly enhancing the host's inflammatory response to pathogens[3]. By targeting TREM-1, Nangibotide TFA can be used in research for conditions such as septic shock, osteoarthritis, acute lung injury, and acute liver failure[4-7].
In vitro, treatment of MC3T3-E1 cells with Nangibotide TFA (50 or 100μg/mL; 7-21 days) significantly reversed the inhibition of osteogenic differentiation, increased alkaline phosphatase activity, calcium nodule formation, and the expression of Runx2, Osterix, and COL1A1 protein[5].
In vivo, Nangibotide TFA (5mg/kg; i.p.; every 2 days for 4 weeks) significantly alleviated cartilage degeneration, improved subchondral bone microstructure, and inhibited osteoblast apoptosis in ACLT-induced osteoarthritic mice[5]. Nangibotide TFA (5mg/kg; i.v.; administered 2 hours before LPS injection) attenuated LPS-induced acute lung injury in mice by reducing pulmonary inflammation (decreasing MPO activity), lowering the lung wet/dry weight ratio, and inhibiting NLRP3 inflammasome activation (reducing NLRP3 protein expression)[6]. Nangibotide TFA (5mg/kg; i.v.; administered 1 hour after TAA injection) promoted liver repair in thioacetamide-induced acute liver failure mice by improving inflammation resolution and liver regeneration[7].
References:
[1] Cuvier V, Lorch U, Witte S, et al. A first-in-man safety and pharmacokinetics study of nangibotide, a new modulator of innate immune response through TREM-1 receptor inhibition. Br J Clin Pharmacol. 2018;84(10):2270-2279.
[2] Bouchon A, Dietrich J, Colonna M. Cutting edge: inflammatory responses can be triggered by TREM-1, a novel receptor expressed on neutrophils and monocytes. J Immunol. 2000;164(10):4991-4995.
[3] Bouchon A, Facchetti F, Weigand MA, Colonna M. TREM-1 amplifies inflammation and is a crucial mediator of septic shock. Nature. 2001;410(6832):1103-1107.
[4] François B, Wittebole X, Ferrer R, et al. Nangibotide in patients with septic shock: a Phase 2a randomized controlled clinical trial. Intensive Care Med. 2020;46(7):1425-1437.
[5] Zhong Y, Xu Y, Xue S, et al. Nangibotide attenuates osteoarthritis by inhibiting osteoblast apoptosis and TGF-β activity in subchondral bone. Inflammopharmacology. 2022;30(3):1107-1117.
[6] Liu T, Zhou Y, Li P, et al. Blocking triggering receptor expressed on myeloid cells-1 attenuates lipopolysaccharide-induced acute lung injury via inhibiting NLRP3 inflammasome activation. Sci Rep. 2016;6:39473.
[7] Wang Y, Xie X, Liu H, Liu H, Jiang H. LR12 Promotes Liver Repair by Improving the Resolution of Inflammation and Liver Regeneration in Mice with Thioacetamide- (TAA-) Induced Acute Liver Failure. Mediators Inflamm. 2021;2021:2327721.
| Cell experiment [1]: | |
Cell lines | MC3T3-E1 mouse osteoblast cell line |
Preparation Method | MC3T3-E1 mouse osteoblast cell line was used for this study. MC3T3-E1 cells were grown in α-MEM containing 10% FBS and 1% penicillin/streptomycin in a cell incubator under 5% CO2 at 37°C. Cell Counting Kit-8 (CCK-8) test was used to measure cell viability and proliferation. The cells were grown at a density of 6×103 cells/well in 96-well plates for 12h for adhesion. To determine the toxicity of Nangibotide TFA, the cells were treated with Nangibotide TFA at concentrations of 0, 25, 50, 100, and 200μg/mL for 1, 3, or 5 days. To determine whether Nangibotide TFA could restore the proliferation of MC3T3-E1 cells, 10ng/mL TNF-α was added to various concentrations of Nangibotide TFA. In addition, 10μL of CCK-8 per well was then added to the cells. After incubating at 37℃ for 2h, the cells were assessed by spectrophotometry. |
Reaction Conditions | 0, 25, 50, 100, and 200μg/mL for 1, 3, or 5 days |
Applications | Nangibotide TFA significantly enhanced osteoblast proliferation. |
| Animal experiment [2]: | |
Animal models | C57BL/6 J mice |
Preparation Method | For the acute lung injury (ALI) model, C57BL/6 J mice were randomly grouped and treated with lipopolysaccharide (LPS) (5mg/kg) intratracheal injection (i.t.) for 6h. Control animals received saline respectively. For survival study, mice were treated with a lethal dose of LPS (20mg/kg, i.t). Survival rate was monitored every 12h for 3 days after LPS injection. Mice were received saline, antagonistic TREM-1 peptide Nangibotide TFA (5mg/kg) or sequence-scrambled control peptide LRS (5mg/kg) respectively via intravenous injection (i.v) 2h before LPS administration. Lung tissue samples were collected for further analysis. |
Dosage form | 5mg/kg; i.v. ; 2h before LPS administration |
Applications | Nangibotide TFA attenuated LPS-induced acute lung injury in mice by reducing pulmonary inflammation (decreasing MPO activity), lowering the lung wet/dry weight ratio, and inhibiting NLRP3 inflammasome activation (reducing NLRP3 protein expression). |
References: | |
| Cas No. | 2014384-91-7 | SDF | |
| Überlieferungen | LR12 TFA | ||
| Formula | C56H83F3N14O24S2 | M.Wt | 1457.46 |
| Löslichkeit | DMSO : 50 mg/mL (34.31 mM; Need ultrasonic) | Storage | Store at -20°C, protect from light, stored under nitrogen |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 686.1 μL | 3.4306 mL | 6.8613 mL |
| 5 mM | 137.2 μL | 686.1 μL | 1.3723 mL |
| 10 mM | 68.6 μL | 343.1 μL | 686.1 μL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)