| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
TREM-2 (Triggering Receptor Expressed on Myeloid Cells-2). IA9 TFA is a TREM-2 inhibitor that binds to TREM-2 and blocks its signaling. TREM-2 is a transmembrane receptor of the immunoglobulin superfamily that is expressed on myeloid cells. It associates with the adapter protein DAP12 (TYROBP) to transmit signals via ITAM (immunoreceptor tyrosine-based activation motif) phosphorylation. TREM-2 activation promotes phagocytosis, cell survival, and the production of inflammatory cytokines. In the context of arthritis, TREM-2 signaling in macrophages and other myeloid cells contributes to the inflammatory response that drives joint inflammation and damage. By inhibiting TREM-2, IA9 TFA reduces this inflammatory response.
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| ln Vitro |
IA9 TFA is a TREM-2 inhibitor that diminishes the release of proinflammatory cytokines. In vitro, IA9 TFA inhibits TREM-2 signaling in macrophages and other myeloid cells, reducing the production of inflammatory mediators such as TNF-α, IL-6, and IL-1β in response to inflammatory stimuli. By blocking TREM-2, the peptide prevents the activation of downstream signaling pathways including Syk, PI3K, and MAPK, which are involved in cytokine production and inflammatory responses. The peptide effectively suppresses joint inflammation and damage in collagen-induced arthritis (CIA) mouse models.
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| ln Vivo |
IA9 TFA demonstrates efficacy in collagen-induced arthritis (CIA) mouse models by inhibiting TREM-2 signaling, leading to reduced inflammatory responses and protection against arthritis-associated joint damage. In the CIA model, immunization with type II collagen induces an autoimmune response that leads to joint inflammation, synovial hyperplasia, cartilage destruction, and bone erosion, mimicking human rheumatoid arthritis. Treatment with IA9 TFA dramatically suppresses joint inflammation and damage, as assessed by clinical arthritis scores, paw swelling measurements, and histopathological analysis of joints. The peptide's ability to penetrate the blood-brain barrier also makes it useful for studying neuroinflammation.
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| Enzyme Assay |
TREM-2 binding assays are performed using surface plasmon resonance (SPR) or ELISA with recombinant TREM-2 protein incubated with varying concentrations of IA9 TFA to determine binding affinity (KD). Competition assays with labeled ligands can also be used to assess the ability of IA9 TFA to compete with TREM-2 ligands for receptor binding. The peptide's binding to TREM-2 confirms its direct interaction with the receptor and provides a mechanistic basis for its inhibitory activity.
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| Cell Assay |
Macrophage or microglial cell lines expressing TREM-2 are treated with IA9 TFA at varying concentrations. Cytokine release (e.g., TNF-α, IL-6, IL-1β) is measured by ELISA following LPS or other inflammatory stimuli to assess the anti-inflammatory activity of TREM-2 inhibition. The ability of IA9 TFA to reduce cytokine production in response to inflammatory challenges demonstrates its functional activity as a TREM-2 inhibitor. Cell viability is assessed to confirm that the anti-inflammatory effects are not due to cytotoxicity.
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| Animal Protocol |
Collagen-induced arthritis (CIA) mouse model: DBA/1 mice are immunized with type II collagen in complete Freund's adjuvant and treated with IA9 TFA via intraperitoneal or subcutaneous injection. Arthritis scores are assessed by visual inspection of paws (scoring swelling and erythema). Paw swelling is measured using calipers. At study endpoint, joints are collected for histopathological analysis (e.g., H&E staining, safranin O staining for cartilage, and TRAP staining for osteoclasts) to evaluate inflammation, cartilage destruction, and bone erosion. The dramatic suppression of joint inflammation and damage by IA9 TFA confirms its efficacy in this model.
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| ADME/Pharmacokinetics |
As a peptide, IA9 TFA is expected to have moderate to poor oral bioavailability and is typically administered via parenteral routes (intraperitoneal, subcutaneous, intravenous). Rapid renal clearance and proteolytic degradation are expected, consistent with the pharmacokinetic properties of most peptide therapeutics. The peptide's ability to penetrate the blood-brain barrier is a notable feature that distinguishes it from many other peptides. Pharmacokinetic parameters (Cmax, Tmax, AUC, t1/2) are evaluated in rodents for efficacy study design. Detailed PK data specific to IA9 TFA are not extensively reported in the available literature.
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| Toxicity/Toxicokinetics |
IA9 TFA is a research-grade peptide inhibitor with an expected safety profile typical of peptide therapeutics. Potential toxicities are related to TREM-2 inhibition in the immune system. TREM-2 is involved in the regulation of immune responses, and its inhibition could potentially affect host defense, wound healing, and bone remodeling. However, in the CIA model, TREM-2 inhibition provides therapeutic benefits without obvious adverse effects. Standard toxicology studies in rodents are required for therapeutic development. As a research compound, detailed toxicology data are not publicly available.
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| References | |
| Additional Infomation |
IA9 TFA is a research-grade TREM-2 inhibitor peptide for immunology and inflammation research. It corresponds to human TREM-2 amino acids 182-190 and is supplied as a TFA salt. It is a blood-brain barrier-penetrating peptide that can reduce proinflammatory cytokine release and suppress joint inflammation in collagen-induced arthritis models. IA9 can be used for PET imaging of neuroinflammation. Synonyms: IA9 TFA (human TREM-2 182-190 TFA). For research use only, not for human therapeutic use.
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| Molecular Formula |
C51H88N10O10.XC2HF3O2
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| Molecular Weight |
1001.31 (free acid)
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| Appearance |
Typically exists as solid at room temperature
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :~6.25 mg/mL (with sonication)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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