| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
DABMA (compound 3j) (2 hours before infection and 48 hours after infection) inhibited SARS-CoV-2 infection in Vero E6 cells with an IC50 value of 4.9 μM [1]. DABMA (2 hours before infection and 20 hours after infection) inhibited SARS-CoV-2 infection in U2OS-ACE2 cells with an IC50 value of 3.3 μM [1]. DABMA (5-minute bath solution) directly activated the hTMEM175 channel in the isolated endosomal of HEK293T cells with an EC50 value of 17.9 μM. Its mechanism of action is through extracellular/cytoplasmic or transmembrane domains without changing the expression level of the channel [1]. DABMA (15-30 μM; 20 h) protected against diphtheria toxin (DT) cytotoxicity in A549 cells, while the absence of TMEM175 significantly weakened this protective effect, with the protective factor decreasing from 6.2 to 3.5 at 15 μM and from 75.7 to 28.8 at 30 μM [1]. DABMA (30 μM; 24 h) protected against cell rounding induced by Clostridium difficile toxin B (TcsL) in Vero cells, while the absence of TMEM175 significantly weakened this protective effect, with the cell rounding rate of knockdown cells being only 83.0%, compared to 54.6% for control cells [1]. DABMA (30 μM; 5 h) delayed the lysosomal degradation of DQ-BSA, while the absence of TMEM175 significantly weakened this effect, reducing the inhibitory effect of the compound by about 40% compared to control cells [1]. DABMA (30 μM; 6 h) significantly enhanced the fluorescence intensity of LysoTracker Green in TMEM175 wild-type HeLa cells, but this effect was completely lost in TMEM175 knockout HeLa cells, and had no effect on mitochondrial staining in either cell type [1]. DABMA (30 μM; 6 h) significantly enhanced the signal intensity of Rab7 in TMEM175 wild-type HeLa cells, but this effect was lost in TMEM175 knockout HeLa cells where the basal level of Rab7 was already elevated [1]. DABMA effectively inhibited DT-induced A549 cytotoxicity, with an EC50 value of 25.7 μM [2]. DABMA (30-60 μM) showed low long-term toxicity to A549 cells, with a CC50 value of 119.7 μM, and did not affect cell viability or colony formation [2]. DABMA stably inhibited DT-induced cytotoxicity in Vero, PC3, A431, DLD1, and primary HUVEC cells, indicating that it has non-cell type-specific efficacy [2]. DABMA (30 μM; 2 h) altered the morphology of acidic endosomes in A549 cells and increased Lysotracker Deep Red staining intensity, indicating that lysosomal function was interfered with [2]. DABMA (30 μM; 18 h) induced cholesterol accumulation in A549 cells, as evidenced by increased Filipin III staining intensity [2]. DABMA (30 μM; 6 h) targeted late endosomes in A549 cells, as evidenced by increased Rab7 immunostaining intensity [2]. DABMA (15 μM) synergistically protected A549 cells from DT-induced cytotoxicity with more than 300 combined protective factors and no additive toxicity [2]. DABMA (30 μM; 4 h) inhibited TcdB-induced cell rounding in Vero cells, with an EC50 of 38.6 μM and a selectivity index of 6.34[2]. DABMA (30 μM; 16 h) inhibited TcsL-induced cell rounding in Vero cells, with an EC50 of 15.8 μM and a selectivity index of 7.38[2]. DABMA (30 μM; 18 h) inhibited PE-induced L929 cytotoxicity, with an EC50 of 20.77 μM and a selectivity index of 4.35[2]. DABMA (1-40 μM; 28 h) effectively inhibited RABV infection in BSR cells[2]. DABMA (0.1-10 μM; 25 hours) effectively inhibited EBOV infection in HeLa cells, with an EC50 of 908 nM, a CC50 of 116.7 μM, and a selectivity index greater than 120[2]. DABMA (concentration range; 72 hours) showed cytotoxicity to both MDCK and A549 cells, with CC50 values of 42.71 μM and 47.42 μM, respectively[3]. DABMA (pre-incubated for 5 hours) effectively inhibited influenza virus-induced cytopathic effect (CPE) in MDCK cells, with EC50 values ranging from 1.82 µM to 6.73 µM for amantadine-sensitive, amantadine-resistant, and influenza B virus strains[3]. DABMA (3.75–15 µM; pre-incubation for 5 hours) dose-dependently reduced the viral titers of A/NY/61/LV16A (H1N1) and A/17/HK/2014/8296 (H3N2) viruses in MDCK and A549 cells. Significant reductions in viral titers were observed at concentrations of 3.75, 7.5, and 15 µM after 5 hours of pre-incubation and 48 hours of infection [3]. DABMA (15 µM; pre-incubation for 5 hours) inhibited H1N1 (A/NY/61/LV16A) genomic RNA replication by up to 86.51% and reduced NP synthesis in MDCK cells. It also significantly reduced the fluorescence intensity of NPs in infected A549 cells after 5 hours of pre-incubation and 16 hours of infection [3]. DABMA (15 µM) inhibits the early stages of H1N1 (A/NY/61/LV16A) infection of MDCK cells by inhibiting viral entry into cells, but does not affect viral binding to cells [3].
|
|---|---|
| ln Vivo |
DABMA (1.25-5 mg/kg; intraperitoneal injection; once daily; 6 days) increased the survival rate of H1N1-infected BALB/c mice by 67%, while significantly reducing viral load in the lungs, lung index and lung pathology [3].
|
| Cell Assay |
Cytotoxicity assay [1]
Cell Types: Control A549 cells (unlabeled shRNA), TMEM175 knockdown (shTMEM175) A549 cells Tested Concentrations: 15 μM; 30 μM Incubation Duration: 20 h Experimental Results: At 15 μM, shTMEM175 reversed DT-induced protein synthesis inhibition in control A549 cells, with a protection factor of 6.2. At 30 μM, shTMEM175 reversed DT-induced protein synthesis inhibition in control A549 cells, with a protection factor of 75.7. At 15 μM, the protection factor of shTMEM175 A549 cells was significantly reduced to 3.5. In shTMEM175 A549 cells, the protection factor was significantly reduced to 28.8 at 30 μM. Cytotoxicity assay [1] Cell Types: Control SCR RNA Vero cells, TMEM175 knockdown (shTMEM175) Vero cells Tested Concentrations: 30 μM Incubation Duration: 24 h Experimental Results: In control SCR RNA Vero cells, the TcsL-induced cell rounding rate decreased from 96.7% to 54.6%. In shTMEM175 Vero cells, the protective effect was significantly weakened, with 83.0% of cells still remaining round. Immunofluorescence [2] Cell Types: A549 cells Tested Concentrations: 30 μM Incubation Duration: 6 hours Experimental Results: Rab7 fluorescence intensity was significantly increased compared with the DMSO control group, indicating late endosome expansion.
|
| Animal Protocol |
Animal/Disease Models:BALB/c (female, 6-8 weeks old, no specific pathogen) [3]
Doses: 1.25 mg/kg; 5 mg/kg Route of Administration: Intraperitoneal injection; once daily for 6 consecutive days Experimental Results: The survival rate of mice was increased to 67% compared with the placebo group. On days 5-8 after inoculation, the body weight of mice was significantly higher than that of the placebo group. On day 6 after inoculation, the relative viral RNA load, lung index and viral titer in the lungs of mice were significantly lower than those in the placebo group. The pathological damage to lung tissue caused by influenza virus was reduced, including thickening of the lung septa and infiltration of inflammatory cells. No toxicity was observed in uninfected mice. |
| References |
|
| Molecular Formula |
C20H28BRNO
|
|---|---|
| Molecular Weight |
378.35
|
| CAS # |
893603-33-3
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
BrC1=CC=C(C(CNC23CC4CC(C2)(CC(C4)(C3)C)C)=C1)OC
|
| 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 | 2.6431 mL | 13.2153 mL | 26.4306 mL | |
| 5 mM | 0.5286 mL | 2.6431 mL | 5.2861 mL | |
| 10 mM | 0.2643 mL | 1.3215 mL | 2.6431 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
