Nangibotide TFA (Synonyms: LR12 TFA) |
Catalog No.GC63949
One-Click Copy Product Info
|
Nangibotide TFA es un péptido sintético e inhibidor del receptor TREM-1
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.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
Nangibotide TFA es un péptido sintético e inhibidor del receptor TREM-1 [1]. TREM-1 (Triggering Receptor Expressed on Myeloid Cells-1) es un receptor inmune perteneciente a la superfamilia de inmunoglobulinas, expresado principalmente en la superficie de células mieloides como monocitos, macrófagos y neutrófilos[2]. Este receptor juega un papel crucial en la amplificación de las respuestas inflamatorias, mejorando significativamente la respuesta inflamatoria del huésped a los patógenos[3]. Al apuntar a TREM-1, Nangibotide TFA se puede utilizar en la investigación de afecciones como el shock séptico, la osteoartritis, la lesión pulmonar aguda y la insuficiencia hepática aguda [4-7].
In vitro, el tratamiento de células MC3T3-E1 con Nangibotide TFA (50 o 100μg/mL; 7-21 días) revirtió significativamente la inhibición de la diferenciación osteogénica, el aumento de la actividad de la fosfatasa alcalina, la formación de nódulos de calcio y la expresión de la proteína Runx2, Osterix y COL1A1[5].
In vivo, Nangibotide TFA (5mg/kg; i.p.; cada 2 días durante 4 semans) alivió significativamente la degeneración del cartílago, mejoró la microestructura ósea subcondral e inhibió la apoptosis de los osteoblastos en ratas osteoartríticos inducidos por ACLT[5]. Nangibotide TFA (5mg/kg; i.v.; administrado 2 horas antes de la inyección de LPS) atenuó la lesión pulmonar aguda nducida por LPS en ratones al reducir la inflamación pulmonar (disminuir la actividad de MPO), reducir la relación de peso húmedo/seco pulmonar e inhibir la activación del inflamasoma NLRP3 (reduciendo la expresión de la proteína NLRP3)[6]. Nangibotide TFA (5mg/kg; i.v.; administrado 1 hora después de la inyección de TAA) promovió la reparación del hígado en ratones con insuficiencia hepática aguda inducidos por thioacetamide al mejorar la resolución de la inflamación y la regeneración del hígado [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.
References:
[1] 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.
[2] 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.
| Cas No. | 2014384-91-7 | SDF | |
| Sinónimos | LR12 TFA | ||
| Formula | C56H83F3N14O24S2 | M.Wt | 1457.46 |
| Solubility | 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. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- 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.)