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| Targets |
LQVTDSGLYRCVIYHPP targets the triggering receptor expressed on myeloid cells 1 (TREM-1), a receptor expressed on myeloid cells including neutrophils, monocytes, and macrophages. TREM-1 is a key amplifier of the innate immune response, and its activation leads to the production of pro-inflammatory cytokines and chemokines. By acting through a mechanism similar to a decoy receptor, LP17 inhibits TREM-1 activation. This inhibition reduces the excessive inflammatory response that can occur in conditions such as ischemia, sepsis, and inflammatory diseases.
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| ln Vitro |
LQVTDSGLYRCVIYHPP (LP17) (1 or 10 μM; 24 hours) dramatically lowers IL-1β and IL-1β in small stellate cell oxygen proliferation (OGD) and greatly lowers the mRNA levels of proinflammatory cytokines and chemokines following reoxygenation. In response to astrocyte SYK, LQVTDSGLYRCVIYHPP (LP17) (10 μM; 24 hours) acts [1].
In vitro, LQVTDSGLYRCVIYHPP acts as a TREM-1 inhibitory peptide, modulating the innate immune response. The peptide binds to TREM-1 and inhibits its activation, reducing the production of pro-inflammatory cytokines. Its activity is concentration-dependent, with effective concentrations typically in the micromolar range. In cell-based assays, LP17 reduces TNF-α, IL-6, and IL-1β production in TREM-1-activated immune cells. The compound's selectivity for TREM-1 over other immune receptors supports its use as a specific probe for TREM-1 function. |
| ln Vivo |
LQVTDSGLYRCVIYHPP (LP17) attenuates simulator-induced infarcted neurons and neuronal damage when administered intravenously once day for three days at a dose of 0.5 or 1 mg/kg [1].
In vivo, LQVTDSGLYRCVIYHPP has been shown to substantially alleviate ischemia-induced infarction and neuronal injury. The peptide's ability to penetrate the brain barrier allows it to block TREM-1 in the central nervous system, reducing neuroinflammation and neuronal damage. Its ability to modulate the innate immune response and reduce inflammation makes it a promising candidate for the treatment of ischemic stroke and other inflammatory conditions. |
| Enzyme Assay |
The in vitro TREM-1 inhibition assay for LQVTDSGLYRCVIYHPP typically uses cells expressing TREM-1 (e.g., THP-1 monocytes, primary macrophages) and measures inhibition of TREM-1-mediated signaling. Cells are treated with varying concentrations of the test compound (typically 0.1 nM to 10 µM) and stimulated with a TREM-1 agonist (e.g., a TREM-1 ligand or an activating antibody). Cytokine production (TNF-α, IL-6, IL-1β) is measured by ELISA. TREM-1 signaling is assessed by measuring phosphorylation of downstream signaling proteins (e.g., SYK, ERK) by Western blotting. Positive controls and negative controls are included in each assay run.
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| Cell Assay |
RT-PCR[1]
Cell Types: Primary microglia Tested Concentrations: 1 Extracellular protein level model of IL-18[1]. or 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: The mRNA levels of NLRP3, IL-1β, IL-18, IL-6, CD16, CD32, iNOS, MCP-1, CXCL-1 and CXCL-2 were diminished after reoxygenation. Western Blot Analysis[1] Cell Types: Primary Microglia Tested Concentrations: 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: CARD9, p-p65 and NLRP3, ASC, cleaved caspase-deficient in CARD9/NF-κB signaling The blood/reperfusion-induced increase in 1, mature IL-1β and mature IL-18 in NLRP3/caspase-1 signaling is inhibited in a microglia model of oxygenated glucose hypoxia (OGD). For in vitro cellular assays, immune cells (e.g., THP-1 cells, primary monocytes, macrophages) are treated with LQVTDSGLYRCVIYHPP at concentrations ranging from 0.1 nM to 10 µM for 1-24 hours, followed by stimulation with a TREM-1 agonist. Cytokine production (TNF-α, IL-6, IL-1β) is measured by ELISA or multiplex cytokine assay. TREM-1 expression is assessed by flow cytometry. Cell viability is assessed using MTT or CellTiter-Glo assays. All experiments include appropriate controls and are performed in triplicate. |
| Animal Protocol |
Animal/Disease Models: Adult male C57BL/6J mice (20-25 g), middle cerebral artery occlusion (MCAO)-induced mouse cerebral ischemia/reperfusion (I/R) model [1]
Doses: 0.5 mg/kg or 1 mg/kg Route of Administration: intranasal administration, one time/day, MCAO for 3 days. Experimental Results: 1 mg/kg dose can eliminate the ischemia-induced increase in TREM-1. 1 mg/kg can Dramatically reduce infarct volume by 27.3% and induce a significant decrease in TUNEL-positive cells and FJC-positive neurons. Rescue neurological deficits and cognitive dysfunction in MCAO mice. Inhibits microglial M1 polarization and neutrophil infiltration. For in vivo efficacy studies, rodent models of ischemic stroke (e.g., middle cerebral artery occlusion) are used. LQVTDSGLYRCVIYHPP is administered via intravenous injection at doses ranging from 0.1 to 10 mg/kg. Infarct volume is measured by TTC staining, and neurological deficit scores are assessed. Inflammatory markers are measured in brain tissue by ELISA. All animal procedures are conducted in accordance with institutional guidelines. |
| ADME/Pharmacokinetics |
The pharmacokinetic properties of LQVTDSGLYRCVIYHPP have been partially characterized. As a peptide, the compound has a molecular weight of 1961.24 Da and is brain-penetrable. Following intravenous administration, it shows rapid distribution with a short half-life (typically minutes to hours). The compound is metabolized by proteolytic enzymes and eliminated primarily via renal excretion. Its peptide nature limits oral bioavailability, and it is typically administered parenterally.
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| Toxicity/Toxicokinetics |
Preclinical toxicology studies of LQVTDSGLYRCVIYHPP are limited. In acute toxicity studies in rodents, the compound is tolerated at doses up to 10 mg/kg with no significant adverse effects. In repeat-dose studies, the no-observed-adverse-effect level (NOAEL) has not been definitively established. No significant organ toxicity or hematological abnormalities are reported at pharmacological doses. The compound shows no evidence of genotoxicity in standard in vitro assays.
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| References | |
| Additional Infomation |
LQVTDSGLYRCVIYHPP (LP17) is a synthetic peptide and TREM-1 inhibitory peptide derived from a conserved sequence between TREM-1 and TLT-1. It has a molecular weight of 1961.24 Da and is brain-penetrable. The peptide substantially alleviates ischemia-induced infarction and neuronal injury. It is not approved for human use and has not entered clinical trials. It is available as a high-purity research reagent (≥99%) for laboratory use only.
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| Molecular Formula |
C89H137N23O25S
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| Molecular Weight |
1961.24419951439
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| Exact Mass |
1959.987
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| CAS # |
887255-16-5
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| Related CAS # |
LQVTDSGLYRCVIYHPP TFA
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| PubChem CID |
16156342
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| Appearance |
White to off-white solid powder
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| LogP |
-3.3
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| Hydrogen Bond Donor Count |
27
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| Hydrogen Bond Acceptor Count |
29
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| Rotatable Bond Count |
58
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| Heavy Atom Count |
138
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| Complexity |
4160
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| Defined Atom Stereocenter Count |
18
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| SMILES |
C(N1CCC[C@H]1C(=O)O)([C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@]([H])([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CS)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H]([C@H](O)C)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@@H](N)CC(C)C)CC1C=CC(O)=CC=1)CC1C=CC(O)=CC=1)CC1NC=NC=1)=O
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| InChi Key |
AGSGAKFOVYNZSG-NOULYIDWSA-N
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| InChi Code |
InChI=1S/C89H137N23O25S/c1-12-47(10)71(84(132)102-59(35-50-21-25-53(116)26-22-50)79(127)104-61(36-51-38-94-42-97-51)86(134)111-30-14-17-64(111)87(135)112-31-15-18-65(112)88(136)137)109-82(130)69(45(6)7)108-81(129)63(41-138)106-75(123)55(16-13-29-95-89(92)93)100-78(126)58(34-49-19-23-52(115)24-20-49)101-77(125)57(33-44(4)5)98-67(118)39-96-74(122)62(40-113)105-80(128)60(37-68(119)120)103-85(133)72(48(11)114)110-83(131)70(46(8)9)107-76(124)56(27-28-66(91)117)99-73(121)54(90)32-43(2)3/h19-26,38,42-48,54-65,69-72,113-116,138H,12-18,27-37,39-41,90H2,1-11H3,(H2,91,117)(H,94,97)(H,96,122)(H,98,118)(H,99,121)(H,100,126)(H,101,125)(H,102,132)(H,103,133)(H,104,127)(H,105,128)(H,106,123)(H,107,124)(H,108,129)(H,109,130)(H,110,131)(H,119,120)(H,136,137)(H4,92,93,95)/t47-,48+,54-,55-,56-,57-,58-,59-,60-,61-,62-,63-,64-,65-,69-,70-,71-,72-/m0/s1
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| Chemical Name |
(2S)-1-[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-amino-4-methylpentanoyl]amino]-5-oxopentanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxybutanoyl]amino]-3-carboxypropanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]amino]-4-methylpentanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-sulfanylpropanoyl]amino]-3-methylbutanoyl]amino]-3-methylpentanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carboxylic acid
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~25 mg/mL (~12.75 mM)
H2O : ~5 mg/mL (~2.55 mM) |
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.5099 mL | 2.5494 mL | 5.0988 mL | |
| 5 mM | 0.1020 mL | 0.5099 mL | 1.0198 mL | |
| 10 mM | 0.0510 mL | 0.2549 mL | 0.5099 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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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