| ln Vitro |
LSD1-IN-43 (10 μM) exhibited highly selective and reversible inhibition of LSD1, with extremely low activity against MAO-A (inhibition rate 7%) and MAO-B (inhibition rate 4.9%) [1]. LSD1-IN-43 (25-100 μM) showed low toxicity and effectively reduced the production level of Aβ1-42 in HT22 cells [1]. LSD1-IN-43 (10 μM) had a significant inhibitory effect on Aβ1-42 aggregation, with an inhibition rate of 66.19%, which was much higher than that of curcumin (49.98%) [1].
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| ln Vivo |
LSD1-IN-43 (125-500 μM, 24-56 h) showed the ability to prolong lifespan and reduce paralysis in a concentration-dependent manner in the CL4176 transgenic Caenorhabditis elegans model[1]. LSD1-IN-43 (40-80 mg/kg, gavage) restored the expression of H3K9me2 (a histone marker regulated by LSD1) and improved learning, memory and cognitive deficits in this AD mouse model[1].
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| Animal Protocol |
Animal/Disease Models:APP/PS1 mice (5 weeks old) [1]
Doses: 40, 80 mg/kg Route of Administration: Gavage (ig) Experimental Results: Compared with the saline-treated APP/PS1 group, the APP/PS1 group mice performed better in the Morris water maze. Compared with the saline-treated APP/PS1 group, the APP/PS1 group mice had a shorter escape latency and a stronger ability to locate hidden platforms. Compared with the saline-treated APP/PS1 group, the APP/PS1 group mice had more correct alternations and a stronger spatial recognition ability. Compared with the saline-treated group, the APP/PS1 group mice showed reduced expression of neuroinflammatory markers (IBAI in microglia and GFAP in astrocytes) and inflammatory cytokines (IL-1β and TNF-α) in the CA1 region of the hippocampus. The high-dose (80 mg/kg) treatment group showed reduced Aβ1-42 deposition in the hippocampus, with a more significant reduction compared to the saline-treated APP/PS1 group. Compared to the saline-treated APP/PS1 group, the treatment group restored H3K9me2 expression, a histone marker regulated by LSD1. Compared to the saline-treated APP/PS1 group, the treatment group showed increased neuronal density, more compact arrangement, and reduced nuclear condensation and cytoplasmic vacuolation. |
| References |
| Appearance |
Typically exists as solids 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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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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