Structure of LM11A-31 2HCl
CAS No.: 1243259-19-9
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
LM11A-31 2HCl is a non-peptide p75NTR (nerve growth factor receptor p75) modulator. As an orally active proNGF antagonist, it has good blood-brain barrier permeability and blocks p75-mediated cell death.
Synonyms: LM11A-31 (hydrochloride); LM11A-31 dihydrochloride
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| CAS No. : | 1243259-19-9 |
| Formula : | C12H27Cl2N3O2 |
| M.W : | 316.27 |
| SMILES Code : | CC[C@H](C)[C@H](N)C(NCCN1CCOCC1)=O.[H]Cl.[H]Cl |
| Synonyms : |
LM11A-31 (hydrochloride); LM11A-31 dihydrochloride
|
| MDL No. : | MFCD28166485 |
| GHS Pictogram: |
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| Signal Word: | Warning |
| Hazard Statements: | H302-H315-H319 |
| Precautionary Statements: | P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330 |
In Vitro:
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Cell Line
|
Concentration | Treated Time | Description | References |
| Human neuroblastoma SH-SY5Y cells | 200 nM | 16-18 hours | LM11A-31 decreased mHtt aggregates in SH-SY5Y cells expressing mHtt (exon 1 with 74 CAG repeats) and increased autophagic/lysosomal activity, as indicated by altered levels of relevant markers (e.g., p62/SQSTM1 and mature cathepsin D) and increased autophagy flux. | Neurotherapeutics. 2025 Mar;22(2):e00495 |
| Human retinal endothelial (HRE) cells | 200 nmol/L | To investigate the effect of LM11A-31 on proNGF-mediated cell permeability. Results showed that LM11A-31 significantly attenuated proNGF-mediated increase in HRE cell permeability. | Diabetologia. 2019 Aug;62(8):1488-1500 | |
| microglia | 10 nM | 7 days | To evaluate the effects of LM11A-31 on FIV-infected feline microglia. LM11A-31 reduced FIV-induced microglial accumulation but no direct effects were observed in purified microglial cultures. | J Neuroimmune Pharmacol. 2012 Jun;7(2):388-400 |
| astrocytes | 10 nM | 7 days | To evaluate the effects of LM11A-31 on FIV-infected feline astrocytes. LM11A-31 reduced FIV-induced morphological changes in astrocytes and suppressed calcium destabilization. | J Neuroimmune Pharmacol. 2012 Jun;7(2):388-400 |
| feline neurons | 10 nM | 7 days | To evaluate the neuroprotective effects of LM11A-31 on FIV-infected feline neurons. LM11A-31 significantly reduced FIV-induced neuronal damage, including dendritic beading and neuronal shrinkage, and restored MAP-2 staining intensity. | J Neuroimmune Pharmacol. 2012 Jun;7(2):388-400 |
| microglia | 10 nM | 1 hour | Suppressed HIV gp120-induced neurotoxic factor release, with a secretory profile similar to macrophages | J Neuroimmune Pharmacol. 2022 Jun;17(1-2):242-260 |
| monocyte-derived macrophages (MDM) | 10 nM | overnight | Suppressed HIV gp120-induced release of neurotoxic factors and induced a shift to a ruffled macrophage phenotype | J Neuroimmune Pharmacol. 2022 Jun;17(1-2):242-260 |
| human retinal endothelial cells (HREs) | 200 nM | 12 hours | LM11A-31 treatment enhanced the secretome of MSCs, significantly increasing the release of SDF-1α, VEGF, and NGF, and improved the angiogenic response of HREs | Int J Mol Sci. 2021 Jan 15;22(2):829 |
| mononuclear cells from synovial fluid (SFMC) of patients with JIA | 10 nM | 1 hour | inhibition of proNGF-induced IL-6 production | RMD Open. 2017 Sep 12;3(2):e000441 |
| Detroit-562 cells | 4 μM | Cells. 2019 Sep 28;8(10):1167 | ||
| Cal-27 cells | 4 μM | Cells. 2019 Sep 28;8(10):1167 | ||
| PE/CA-PJ15 cells | 4 μM | 7 hours | inhibition of cell motility | Cells. 2019 Sep 28;8(10):1167 |
In Vivo:
|
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
| Mice | R6/2 and zQ175dn Huntington's disease model mice | Oral gavage | 25, 50, and 100 mg/kg (R6/2 mice); 10, 25, and 50 mg/kg (zQ175dn mice) | R6/2 mice: once daily for 7 weeks; zQ175dn mice: once or twice daily for 4 months | LM11A-31 reduced mHtt aggregates in the striatum of R6/2 and zQ175dn mice, increased AMPK activation, normalized p62/SQSTM1 and LC3II levels, enhanced LAMP1, and decreased LC3B association with mHtt. | Neurotherapeutics. 2025 Mar;22(2):e00495 |
| Sprague-Dawley rats | Streptococcus pneumoniae meningitis model | Intranasal administration | 15 μg/60 μL/day | Once daily for three consecutive days pretreatment | LM11A-31 pretreatment significantly alleviated S. pneumoniae-induced clinical severity, histopathological injury and the activation of astrocytes and microglia. LM11A-31 pretreatment also significantly ameliorated neuronal apoptosis and necrosis. Moreover, blocking p75NTR with LM11A-31 decreased the expression of inflammation-related transcription factors (NF-κBp65, C/EBPβ) and proinflammatory cytokines/mediators (IL-1β, TNF-α, IL-6 and iNOS). | J Neuroinflammation. 2021 Nov 2;18(1):253 |
| C57BL/6J mice | Streptozotocin-induced diabetic model | Oral gavage | 50 mg/kg | Every 48 hours for 4 weeks | To evaluate the effect of LM11A-31 on diabetes-induced retinal vascular permeability and inflammation. Results showed that LM11A-31 significantly mitigated diabetes-induced increase in retinal vascular permeability and reduced expression of inflammatory mediators TNF-α and IL-1β. | Diabetologia. 2019 Aug;62(8):1488-1500 |
| Mouse | Alzheimer's disease model mice | Oral gavage | 50 mg/kg/day | Once daily for 3 months | To evaluate the modulation of neuroinflammation by LM11A-31 in Alzheimer's disease model mice. Results showed that LM11A-31 treatment significantly reduced TSPO-PET signal in the cortex and hippocampus of mice, corresponding with decreased levels of TSPO immunostaining and microglial Iba1 immunostaining. | Theranostics. 2017 Mar 24;7(6):1422-1436 |
| Mice | P301S tauopathy mouse model | Oral gavage | 50 mg/kg | Five days per week for 3 months | LM11A-31 reduced excess activation of hippocampal cdk5 and JNK kinases, calpain activity, cofilin phosphorylation, tau phosphorylation, acetylation and cleavage, accumulation of multiple forms of insoluble tau aggregates and filaments, and microglial activation, while improving hippocampal behavioral performance | Acta Neuropathol Commun. 2020 Sep 5;8(1):156 |
| Mice | Unilateral sciatic denervation model | Oral | 75mg/kg/day | Once daily for one week | Inhibition of p75NTR significantly reduced JNK activation and inflammatory cytokines in the denervated muscle. | Life Sci. 2021 Dec 1;286:120067 |
| Mice | Retinal ischemia/reperfusion (I/R) injury model | Oral | 50 mg/kg/day | Every other day for 15 days | LM11A-31 significantly mitigated the decline in visual acuity post retinal I/R injury | Int J Mol Sci. 2021 Jan 15;22(2):829 |
| Bio Calculators | ||||
| Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
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1 mM 5 mM 10 mM |
3.16mL 0.63mL 0.32mL |
15.81mL 3.16mL 1.58mL |
31.62mL 6.32mL 3.16mL |
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| Dissolving Methods |
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
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Tags: LM11A-31 | Neurotensin Receptor | p75NTR | neurotrophin | receptor | p75 | Ligand | proNGF | nerve | blood-brain | barrier | cholinergic | neurite | dystrophy | Alzheimer's Disease | inhibitor | 1243259-19-9 |
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| P285 | In case of inadequate ventilation wear respiratory protection. |
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| P235 + P410 | Keep cool. Protect from sunlight. |
Response | |
| Code | Phrase |
| P301 | IF SWALLOWED: |
| P304 | IF INHALED: |
| P305 | IF IN EYES: |
| P306 | IF ON CLOTHING: |
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| P336 | Thaw frosted parts with lukewarm water. Do not rub affected area. |
| P337 | If eye irritation persists: |
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| P340 | Remove victim to fresh air and keep at rest in a position comfortable for breathing. |
| P341 | If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing. |
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| P378 | |
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| P301 + P310 | IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician. |
| P301 + P312 | IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell. |
| P301 + P330 + P331 | IF SWALLOWED: Rinse mouth. Do NOT induce vomiting. |
| P302 + P334 | IF ON SKIN: Immerse in cool water/wrap in wet bandages. |
| P302 + P350 | IF ON SKIN: Gently wash with plenty of soap and water. |
| P303 + P361 + P353 | IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower. |
| P304 + P312 | IF INHALED: Call a POISON CENTER or doctor/physician if you feel unwell. |
| P304 + P340 | IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing. |
| P304 + P341 | IF INHALED: If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing. |
| P305 + P351 + P338 | IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. |
| P306 + P360 | IF ON CLOTHING: Rinse Immediately contaminated CLOTHING and SKIN with plenty of water before removing clothes. |
| P307 + P311 | IF exposed: call a POISON CENTER or doctor/physician. |
| P308 + P313 | IF exposed or concerned: Get medical advice/attention. |
| P309 + P311 | IF exposed or if you feel unwell: call a POISON CENTER or doctor/physician. |
| P332 + P313 | IF SKIN irritation occurs: Get medical advice/attention. |
| P333 + P313 | IF SKIN irritation or rash occurs: Get medical advice/attention. |
| P335 + P334 | Brush off loose particles from skin. Immerse in cool water/wrap in wet bandages. |
| P337 + P313 | IF eye irritation persists: Get medical advice/attention. |
| P342 + P311 | IF experiencing respiratory symptoms: call a POISON CENTER or doctor/physician. |
| P370 + P376 | In case of fire: Stop leak if safe to Do so. |
| P370 + P378 | In case of fire: |
| P370 + P380 | In case of fire: Evacuate area. |
| P370 + P380 + P375 | In case of fire: Evacuate area. Fight fire remotely due to the risk of explosion. |
| P371 + P380 + P375 | In case of major fire and large quantities: Evacuate area. Fight fire remotely due to the risk of explosion. |
Storage | |
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| P402 | Store in a dry place. |
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| H231 | May react explosively even in the absence of air at elevated pressure and/or temperature |
| H240 | Heating may cause an explosion |
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| H242 | Heating may cause a fire |
| H250 | Catches fire spontaneously if exposed to air |
| H251 | Self-heating; may catch fire |
| H252 | Self-heating in large quantities; may catch fire |
| H260 | In contact with water releases flammable gases which may ignite spontaneously |
| H261 | In contact with water releases flammable gas |
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| H305 | May be harmful if swallowed and enters airways |
| H310 | Fatal in contact with skin |
| H311 | Toxic in contact with skin |
| H312 | Harmful in contact with skin |
| H313 | May be harmful in contact with skin |
| H314 | Causes severe skin burns and eye damage |
| H315 | Causes skin irritation |
| H316 | Causes mild skin irritation |
| H317 | May cause an allergic skin reaction |
| H318 | Causes serious eye damage |
| H319 | Causes serious eye irritation |
| H320 | Causes eye irritation |
| H330 | Fatal if inhaled |
| H331 | Toxic if inhaled |
| H332 | Harmful if inhaled |
| H333 | May be harmful if inhaled |
| H334 | May cause allergy or asthma symptoms or breathing difficulties if inhaled |
| H335 | May cause respiratory irritation |
| H336 | May cause drowsiness or dizziness |
| H340 | May cause genetic defects |
| H341 | Suspected of causing genetic defects |
| H350 | May cause cancer |
| H351 | Suspected of causing cancer |
| H360 | May damage fertility or the unborn child |
| H361 | Suspected of damaging fertility or the unborn child |
| H361d | Suspected of damaging the unborn child |
| H362 | May cause harm to breast-fed children |
| H370 | Causes damage to organs |
| H371 | May cause damage to organs |
| H372 | Causes damage to organs through prolonged or repeated exposure |
| H373 | May cause damage to organs through prolonged or repeated exposure |
Environmental hazards | |
| Code | Phrase |
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| H401 | Toxic to aquatic life |
| H402 | Harmful to aquatic life |
| H410 | Very toxic to aquatic life with long-lasting effects |
| H411 | Toxic to aquatic life with long-lasting effects |
| H412 | Harmful to aquatic life with long-lasting effects |
| H413 | May cause long-lasting harmful effects to aquatic life |
| H420 | Harms public health and the environment by destroying ozone in the upper atmosphere |
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