Nangibotide  (Synonyms: LR12)

Nangibotide (LR12) is a synthetic peptide and TREM-1 receptor inhibitor. Nangibotide inhibits NF-κB and NLRP3 inflammasome activation and reduces the release of pro-inflammatory factors (such as IL-1β, IL-8). Nangibotide inhibits Apoptosis. Nangibotide reduces excessive inflammatory responses and protects tissues (liver, lung) from damage. Nangibotide can be used in the researches for myocardial ischemia-reperfusion injury, septic shock, acute lung injury, osteoarthritis, and acute liver failure^{[1][2][3][4][5]}.

TREM-1 receptor<^[1]

Nangibotide (50-100 μg/mL) 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) promotes LO2 cell proliferation indirectly via CCL20 secretion from macrophages^[3].
Nangibotide (25-100 μg/mL; 24 h) 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.p.; every 2 days for 4 weeks) significantly attenuates cartilage degradation, improves subchondral bone microarchitecture, and inhibits osteoblast apoptosis in mice with ACLT-induced osteoarthritis^[2].
Nangibotide (5 mg/kg; i.v.; 1 h after TAA injection) 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) 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.

1343.44

C₅₄H₈₂N₁₄O₂₂S₂

2014384-91-7

Solid

White to off-white

LQEEDAGEYGCM-NH2

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

* 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [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]