Nangibotide TFA
Based on 8 publication(s) in Google Scholar
Nangibotide TFA (LR12 TFA) is a synthetic peptide and TREM-1 receptor inhibitor. Nangibotide TFA inhibits NF-κB and NLRP3 inflammasome activation and reduces the release of pro-inflammatory factors (such as IL-1β, IL-8). Nangibotide TFA inhibits Apoptosis. Nangibotide TFA reduces excessive inflammatory responses and protects tissues (liver, lung) from damage. Nangibotide TFA can be used in the researches for myocardial ischemia-reperfusion injury, septic shock, acute lung injury, osteoarthritis, and acute liver failure.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.36%
- Fòrmula: C56H83F3N14O24S2
- Peso molecular:1457.46
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Almacenamiento:
Sealed storage, away from moisture and light, under nitrogen.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Nangibotide TFA
More- J Pharm Anal. 2026 Jan 6.
- J Headache Pain. 2024 Jan 5;25(1):3. [Abstract]
- Atherosclerosis. 2026 Apr:415:120701. [Abstract]
- Int Immunopharmacol. 2026 Sep 1:184:116961. [Abstract]
- Int Immunopharmacol. 2024 Sep 30;143(Pt 1):113274. [Abstract]
- Cell Signal. 2024 Dec:124:111458. [Abstract]
- PLoS One. 2026 Jan 9;21(1):e0340382. [Abstract]
- Stanford University. 2025.
Customer Validation & Images
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In Vivo Efficacy Study
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Bio/Physico-chemical Assay
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WB
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Histological Imaging/Staining
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IF
Actividad biológica
Nangibotide (50-100 μg/mL) TFA significantly reverses TNF-α-induced inhibition of osteogenic differentiation, increasing alkaline phosphatase activity, calcium nodule formation, and Runx2, Osterix mRNA, and COL1A1 protein expression in MC3T3-E1 mouse osteoblasts[2].
Nangibotide (10 ng/mL) TFA promotes LO2 cell proliferation indirectly via CCL20 secretion from macrophages[3].
Nangibotide (25-100 μg/mL; 24 h) TFA significantly suppresses Porphyromonas gingivalis LPS (HY-D1056D)-induced TREM-1 mRNA, membrane-bound TREM-1, and soluble sTREM-1 expression in human primary monocytes, reducing IL-8, TNF-α, and IL-1β secretion[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Nangibotide (5 mg/kg; i.v.; 1 h after TAA injection) TFA promotes liver repair by improving the resolution of inflammation and liver regeneration in mice with Thioacetamide (HY-Y0698)-induced acute liver failure[3].
Nangibotide (5 mg/kg; i.v.; single dose 2 h before LPS) TFA alleviates lung inflammation (reduced MPO activity), decreases lung wet/dry weight ratio, and inhibits NLRP3 inflammasome activation (lower NLRP3 protein expression) in mice with LPS (from E. coli O111:B4) (HY-D1056A1)-induced acute lung injury[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 male mice (2-month-old; ACLT-induced osteoarthritis)[2]
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Dosage:5 mg/kg
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Administration:Intraperitoneal injection; every 2 days for 4 weeks
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Result:Showed lower OARSI score.
Showed lower MMP-13 expression.
Increased MAR and BFR/BS.
Decreased cleaved-caspase3 positive cells.
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Animal Model:BALB/c male mice (6-8-week-old; TAA-induced ALF)[3]
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Dosage:5 mg/kg
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Administration:Intravenous injection; single dose 1 h after TAA
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Result:Decreased liver necrosis.
Reduced inflammatory cell infiltration.
Upregulated CCL20 secretion from macrophages, and activated p38 MAPK pathway in hepatocytes.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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Appearance Solid
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Peso molecular 1457.46
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Fòrmula C56H83F3N14O24S2
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Color White to off-white
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Synonyms
LR12 TFA
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Sequence
Leu-Gln-Glu-Glu-Asp-Ala-Gly-Glu-Tyr-Gly-Cys-Met-NH2
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Sequence Shortening
LQEEDAGEYGCM-NH2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Sealed storage, away from moisture and light, under nitrogen
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
Publications (8)
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Journal Impact Factor
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Most Recent
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J Headache Pain
Microglia TREM1-mediated neuroinflammation contributes to central sensitization via the NF-κB pathway in a chronic migraine model. [Abstract]2024 Jan 5;25(1):3. PMID: 38177990 -
Atherosclerosis
TREM-1 inhibition with LR12 attenuates in-stent neoatherosclerosis through modulating macrophage polarization in a rabbit model: An optical coherence tomography study. [Abstract]2026 Apr:415:120701. PMID: 41832836 -
Int Immunopharmacol
Rheumatoid arthritis synovial fibroblasts promote the glycolysis of myeloid-derived suppressor cells via TREM1/mTOR axis. [Abstract]2026 Sep 1:184:116961. PMID: 42242136 -
Int Immunopharmacol
Triggering receptor expressed on myeloid cells-1 aggravates obliterative bronchiolitis via enhancing the proinflammatory phenotype of macrophages. [Abstract]2024 Sep 30;143(Pt 1):113274. PMID: 39353383 -
Cell Signal
Inhibition of TREM-1 ameliorates angiotensin II-induced atrial fibrillation by attenuating macrophage infiltration and inflammation through the PI3K/AKT/FoxO3a signaling pathway. [Abstract]2024 Dec:124:111458. PMID: 39384003
Nangibotide TFA purchased from MedChemExpress. Usage Cited in: Cell Signal. 2024 Dec:124:111458. [Abstract]
Nangibotide TFA (LR12, 5 mg/kg; i.p.; once daily for 4 weeks). Quantification of AF inducibility (n = 10) and AF duration (n = 6) in each group.
Nangibotide TFA purchased from MedChemExpress. Usage Cited in: Cell Signal. 2024 Dec:124:111458. [Abstract]
Nangibotide TFA (LR12, 5 mg/kg; i.p.; once daily for 4 weeks). Representative electrophysiological mapping images of the atria during sinus rhythm. Bars indicate the time from the first to the last measurement during one heartbeat. Arrows display the direction of electrical conduction on the atrial surface.
Nangibotide TFA purchased from MedChemExpress. Usage Cited in: Cell Signal. 2024 Dec:124:111458. [Abstract]
Nangibotide TFA (LR12, 5 mg/kg; i.p.; once daily for 4 weeks). Representative Western blot images of Cx40 and Cx43 in mouse atrial tissue.
Nangibotide TFA purchased from MedChemExpress. Usage Cited in: Cell Signal. 2024 Dec:124:111458. [Abstract]
Nangibotide TFA (LR12, 5 mg/kg; i.p.; once daily for 4 weeks). Representative images displaying Masson's trichrome staining, highlighting blue-stained areas indicative of fibrosis (upper scale bar = 80 μm, lower scale bar = 40 μm). The black arrows indicate regions of fibrosis.
Nangibotide TFA purchased from MedChemExpress. Usage Cited in: Cell Signal. 2024 Dec:124:111458. [Abstract]
Nangibotide TFA (LR12, 5 mg/kg; i.p.; once daily for 4 weeks). Representative images of immunofluorescence staining for CD68 (green), TREM-1 (red), and DAPI (blue) in mouse atrial tissue (bar = 10 μm). The white arrowsindicate regions of co-localization of TREM-1 with CD68.
Nangibotide TFA purchased from MedChemExpress. Usage Cited in: Cell Signal. 2024 Dec:124:111458. [Abstract]
Nangibotide TFA (LR12, 5 mg/kg; i.p.; once daily for 4 weeks). The expression of TREM-1 in macrophages, and the M1/M2 ratio in mouse atria were analyzed using flow cytometry (n = 6).
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PLoS One
Inhibition of TREM1 attenuates myocardial ischemia-reperfusion injury-induced cardiomyocyte pyroptosis by suppressing the activation of the NF-κB signaling pathway. [Abstract]2026 Jan 9;21(1):e0340382. PMID: 41511954 -
Solvente y solubilidad
DMSO : 50 mg/mL (34.31 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (1.72 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (1.72 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Cuvier V, 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 Oct;84(10):2270-2279. [Content Brief]
[2]. Zhong Y, et al. Nangibotide attenuates osteoarthritis by inhibiting osteoblast apoptosis and TGF-β activity in subchondral bone. Inflammopharmacology. 2022 Jun;30(3):1107-1117. [Content Brief]
[3]. Wang Y, et al. 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 May 28;2021:2327721. [Content Brief]
[4]. Dubar M, et al. Effects of Porphyromonas gingivalis LPS and LR12 peptide on TREM-1 expression by monocytes. J Clin Periodontol. 2018 Jul;45(7):799-805. [Content Brief]
[5]. Liu T, et al. Blocking triggering receptor expressed on myeloid cells-1 attenuates lipopolysaccharide-induced acute lung injury via inhibiting NLRP3 inflammasome activation. Sci Rep. 2016 Dec 22;6:39473. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 0.6861 mL | 3.4306 mL | 6.8613 mL | 17.1531 mL |
| 5 mM | 0.1372 mL | 0.6861 mL | 1.3723 mL | 3.4306 mL | |
| 10 mM | 0.0686 mL | 0.3431 mL | 0.6861 mL | 1.7153 mL | |
| 15 mM | 0.0457 mL | 0.2287 mL | 0.4574 mL | 1.1435 mL | |
| 20 mM | 0.0343 mL | 0.1715 mL | 0.3431 mL | 0.8577 mL | |
| 25 mM | 0.0274 mL | 0.1372 mL | 0.2745 mL | 0.6861 mL | |
| 30 mM | 0.0229 mL | 0.1144 mL | 0.2287 mL | 0.5718 mL |
Nangibotide TFA Related Classifications
HY-P3211A Related Classifications
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