| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Amyloid-β (Aβ), Histaminergic receptor, α-adrenergic receptor, Serotonergic receptor[1]
|
|---|---|
| ln Vitro |
Latrepirdine has been reported to possess several properties that are potentially relevant to the treatment of neurodegenerative diseases: (1) protection of cultured cells from the cytotoxicity of amyloid-β (Aβ) peptide; (2) stabilization of mitochondrial function and calcium homeostasis; (3) modulation of Aβ release from cultured cells, isolated intact nerve terminals, and from hippocampal neurons in living mouse brain; and (4) promotion of neurogenesis in the murine hippocampus. Treatment of cultured mammalian cells with Latrepirdine leads to enhanced mTOR- and Atg5-dependent autophagy. Latrepirdine modulates Atg5-dependent autophagic activity in a dose-dependent manner and via the mTOR-signaling pathway. HeLa cells stably expressing LC3 fused are treated with EGFP (eGFP-LC3) for 3 or 6 hours in the absence or presence of 50 μM Latrepirdine. Treatment with Latrepirdine for 3 or 6 hours markedly enhances the number of eGFP-LC3 punctae, indicating that Latrepirdine induces formation of autophagosomes. Next, mouse N2a neuroblastoma cells are treated in the absence (vehicle) or presence of 5 nM, 500 nM or 50 μM Latrepirdine for 3 or 6 hours in order to determine the effects of acute drug treatment on the regulation of autophagy. A significant and dose-dependent increase is observed in LC3-II levels in N2a cells following 3- or 6-hour treatment with either 500 nM or 50 μM Latrepirdine. A significant decrease of p-mTOR and p-S6K from N2a cells treated with 50 μM Latrepirdine for 3 hours is observed, whereas the total mTOR and p70S6K levels remain relatively constant[1].
|
| ln Vivo |
Latrepirdine treatment of TgCRND8 transgenic mice is associated with improved learning behavior and with a reduction in accumulation of Aβ42 and α-synuclein. Male, 90-day-old TgCRND8 mice or their wild-type littermates (nTg) receive 31 consecutive once daily ip injections of either 3.5 mg/kg Latrepirdine or 0.9% saline (vehicle). At the culmination of treatment, mice are tested for cued and contextual fear conditioning using a paradigm that has been widely accepted for evaluating learning and memory deficits in APP transgenic mice. A significant increase in cued memory only among Latrepirdine-versus vehicle-treated TgCRND8 mice (p=0.01) is observed. A weak, non-significant trend toward an improvement in contextual memory among Latrepirdine-versus vehicle-treated mice (p=0.099) is also observed[1].
|
| References |
|
| Additional Infomation |
Latepyridine belongs to the methylpyridine and pyridoindole classes of compounds and possesses anti-aging properties. Latepyridine has been used in research to treat Alzheimer's disease and Huntington's disease. The structural formula is shown in the figure. See also: Latepyridine dihydrochloride (its active portion).
|
| Molecular Formula |
C21H25N3
|
|---|---|
| Molecular Weight |
319.44
|
| Exact Mass |
319.205
|
| CAS # |
3613-73-8
|
| PubChem CID |
197033
|
| Appearance |
Typically exists as solids at room temperature
|
| Density |
1.1±0.1 g/cm3
|
| Boiling Point |
505.7±50.0 °C at 760 mmHg
|
| Melting Point |
115-116 °C
|
| Flash Point |
259.7±30.1 °C
|
| Vapour Pressure |
0.0±1.3 mmHg at 25°C
|
| Index of Refraction |
1.629
|
| LogP |
3.96
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
24
|
| Complexity |
425
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC1=CC2=C(C=C1)N(CCC3=CN=C(C)C=C3)C4=C2CN(C)CC4
|
| InChi Key |
JNODQFNWMXFMEV-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C21H25N3/c1-15-4-7-20-18(12-15)19-14-23(3)10-9-21(19)24(20)11-8-17-6-5-16(2)22-13-17/h4-7,12-13H,8-11,14H2,1-3H3
|
| Chemical Name |
2,8-dimethyl-5-[2-(6-methyl-3-pyridinyl)ethyl]-3,4-dihydro-1H-pyrido[4,3-b]indole
|
| Synonyms |
Dimebolin; Dimebone
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 3.1305 mL | 15.6524 mL | 31.3048 mL | |
| 5 mM | 0.6261 mL | 3.1305 mL | 6.2610 mL | |
| 10 mM | 0.3130 mL | 1.5652 mL | 3.1305 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.
Link: https://clinicaltrials.gov/ct2/show/NCT00838110
Conditions:Alzheimer's DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT00827034
Conditions:Alzheimer's Disease|Huntington's DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT00920946
Conditions:Huntington Disease
Title:An Extension of the HORIZON Protocol Evaluating the Safety of Dimebon (Latrepirdine) in Subjects With Huntington Disease
Status:Terminated
updateDate:2016-10-12
Ctid:NCT01085266
Link: https://clinicaltrials.gov/ct2/show/NCT01085266
Conditions:Huntington DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT01152216
Conditions:Alzheimer's DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT00829374
Conditions:Alzheimer's DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT00954590
Conditions:Moderate to Severe AlzheimerLink: https://clinicaltrials.gov/ct2/show/NCT00675623
Conditions:Alzheimer's DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT00704782
Conditions:Alzheimer's DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT00377715
Conditions:Alzheimer's DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT00829816
Conditions:Alzheimer's DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT00497159
Conditions:Huntington's DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT00975481
Conditions:Alzheimer's Disease|Huntington's DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT00939783
Conditions:Alzheimer's DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT01066546
Conditions:Alzheimer's DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT00825084
Conditions:Alzheimer's Disease|Huntington's DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT01066481
Conditions:Alzheimer's Disease|Dementia|Dimebon|Investigational DrugLink: https://clinicaltrials.gov/ct2/show/NCT00824590
Conditions:Alzheimer's Disease|Huntington's DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT00931073
Conditions:Alzheimer's Disease|Huntington's DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT00831532
Conditions:Hepatic FailureLink: https://clinicaltrials.gov/ct2/show/NCT00907322
Conditions:Healthy VolunteersLink: https://clinicaltrials.gov/ct2/show/NCT00831506
Conditions:Alzheimer Disease|Huntington DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT00788047
Conditions:Huntington Disease|Alzheimer DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT00387270
Conditions:Huntington's DiseaseLink: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2008-008005-21
Condition:Alzheimer's DiseaseLink: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2008-006352-22
Condition:Alzheimer's DiseaseLink: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2008-000095-25
Condition:Alzheimer's DiseaseLink: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2007-003293-25
Condition:Huntington's diseaseProducts are for research use only; We do not sell to patients
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