| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
LSD1/HDAC-IN-3 (Compound (±)-3d) showed inhibitory activity against class I HDACs and LSD1, with IC50 values of 1702 nM (HDAC1), 842 nM (HDAC2), 358 nM (HDAC3) and 1074 nM (LSD1), respectively, but did not show significant inhibitory effects against HDAC6, HDAC8 or HDAC10 [1]. LSD1/HDAC-IN-3 (10-30 μM, 24 h) significantly protected ARPE-19 and 661W cells from H2O2-induced oxidative damage, as evidenced by increased cell viability [1]. LSD1/HDAC-IN-3 (10 μM, 24 h) partially increased the levels of acetylated histone H3 (ac-H3) and methylated histone H3 (met-H3) in ARPE-19 and 661W cells [1].
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|---|---|
| ln Vivo |
LSD1/HDAC-IN-3 (compound (±)-3d) (10 μM (1 μL/eye), intravitreal injection, bilateral single dose) can enhance sensory control in growing tissues with Pde6b homozygous mutant rd10 electrodes with C57Bl/6J background [1].
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| Animal Protocol |
Animal/Disease Models: Rd10 mice (autosomal recessive retinitis pigmentosa model with homozygous Pde6b mutation on C57Bl/6J background, both male and female, postnatal day 40)[1]
Doses: 10 μM (1 μL/eye) Route of Administration: intravitreal injection, single bilateral administration Experimental Results: Enhanced photoreceptor survival. Preserved retinal pigment epithelium (RPE) barrier integrity, significantly increasing the number of Zonula Occludens-1 (ZO-1) positive intersections. Downregulated retinal expression of inflammatory genes, specifically reducing the mRNA levels of GFAP, Ccl2, and Ccl12 in retinal tissues, and decreasing GFAP immunoreactivity. Promoted histone H3 modifications in retinal tissues, inducing an upward trend in the levels of acetylated histone H3 (ac-H3) and methylated histone H3 (met-H3). Showed no improvement in retinal function. Exhibited good in vivo safety, with no signs of general distress or ocular tissue side effects. |
| References |
| Molecular Formula |
C28H32N4O
|
|---|---|
| Molecular Weight |
440.58
|
| 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2697 mL | 11.3487 mL | 22.6974 mL | |
| 5 mM | 0.4539 mL | 2.2697 mL | 4.5395 mL | |
| 10 mM | 0.2270 mL | 1.1349 mL | 2.2697 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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