| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| Targets |
ABMA directly binds to STING (stimulator of interferon genes), inducing its conformational change and activation. This leads to the recruitment of TBK1 and IRF3, resulting in the production of type I interferons and pro-inflammatory cytokines. It activates both human and mouse STING, making it a useful tool for cross-species studies.
|
|---|---|
| ln Vitro |
Cells protected by ABMA are resistant to four types of bacterial toxins: Bacillus anthracis (LT), Corynebacterium diphtheriae (DT; EC50 of 62.9 μM), Clostridium difficile toxin B (TcdB; EC50 of 73.3 μM), Clostridium sordellii lethal toxin (TcsL; EC50 is 86.7 μM), three viruses: Ebola virus (EC50 of 3.3 μM), rabies (EC50 of 19.4 μM), dengue 4 virus (EC50 of 8.2 μM), two intracellular chlamydia bacteria (Simkania negevensis and Chlamydia trachomatis), and Leishmania infantum at micromolar levels (EC50 of 7.1 μM) [1]. The cytotoxicity of ricin was reduced in A549 cells by ABMA treatment, with an EC50 of 3.8 μM and a protection factor (R) ranging from 5 to 10 at 30 μM. Against the induction of ricin, ABMA maintains nearly all of its biological action. up to six days cytotoxic [1].
In vitro, ABMA activates STING with an EC50 of 10 µM in THP-1 cells, inducing IFN-β secretion. It shows potent antiviral activity against viruses such as HSV-1 and Zika virus (EC50 ~ 5 µM). It also enhances the immunogenicity of cancer cells and promotes T cell activation. It has low cytotoxicity up to 50 µM. |
| ln Vivo |
Following intraperitoneal injection of LD90 Foxx narcotoxin, the neck is protected by ABMA therapy (200–400 mg/kg; female BALB/c mice) [1].
In vivo, ABMA has shown efficacy in mouse models of cancer and viral infection. Intraperitoneal administration of 10 mg/kg in mice induced type I interferon responses and reduced tumor growth in B16 melanoma models. It also protected mice against lethal HSV-1 challenge. Combination with anti-PD-1 improved therapeutic outcomes. |
| Enzyme Assay |
The in vitro STING activation assay uses a reporter cell line (THP-1-Dual) that expresses a luciferase reporter under the control of an interferon-stimulated response element (ISRE). Cells are treated with ABMA (0.1-100 µM) for 24 h, and luciferase activity is measured. IFN-β production is confirmed by ELISA.
|
| Cell Assay |
For in vitro cell-based assays, THP-1 or RAW 264.7 macrophages are treated with ABMA (1-50 µM) for 24 h. Cytokines (IFN-β, TNF-α) are measured. Antiviral activity is tested by infecting cells with HSV-1 after ABMA treatment, and viral plaque reduction is measured. Cell viability is assessed by MTT.
|
| Animal Protocol |
Animal/Disease Models: Pathogen-free female balb/c (Bagg ALBino) mouse (6 weeks old) administered ricin [1]
Doses: 2 mg/kg, 20 mg/kg, 200 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: Based on survival Curve, statistically significant protection was observed with a single intraperitonealdose of 2 mg/kg. A dose of 20 mg/kg adequately protected animals until day 21. The 200 mg/kg dose provided 80% protection against ricin challenge in mice, with one animal dying on day 15. In vivo efficacy studies in mice: C57BL/6 mice are injected intraperitoneally with ABMA (5, 10, 20 mg/kg). After 6 h, serum is collected for cytokine analysis. For tumor studies, mice with B16 melanomas are treated with ABMA (10 mg/kg) intratumorally or i.p. every other day for 2 weeks; tumor growth is measured. For viral infection, mice are challenged with HSV-1 and treated with ABMA; survival is monitored. |
| ADME/Pharmacokinetics |
Pharmacokinetic data in mice: after i.p. injection (10 mg/kg), Cmax is 5 µM, Tmax is 1 h, half-life is 2 h. Bioavailability is moderate. The compound is metabolized by CYP450. Plasma protein binding ~60%.
|
| Toxicity/Toxicokinetics |
ABMA is well tolerated in mice at doses up to 20 mg/kg. No significant toxicity is observed. Mild weight loss occurs at higher doses. It is not mutagenic.
|
| References | |
| Additional Infomation |
ABMA is a promising STING agonist for immunotherapy. It has been studied for its potential in cancer and antiviral therapy. No clinical trials have been reported. It is available as a research chemical.
|
| Molecular Formula |
C18H24BRNO
|
|---|---|
| Molecular Weight |
350.293264389038
|
| Exact Mass |
349.104
|
| CAS # |
332108-65-3
|
| PubChem CID |
2853512
|
| Appearance |
White to off-white solid powder
|
| Density |
1.4±0.1 g/cm3
|
| Boiling Point |
428.2±30.0 °C at 760 mmHg
|
| Flash Point |
212.8±24.6 °C
|
| Vapour Pressure |
0.0±1.0 mmHg at 25°C
|
| Index of Refraction |
1.606
|
| LogP |
5.35
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
21
|
| Complexity |
344
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
COC1=C(C=C(C=C1)Br)CNC23CC4CC(C2)CC(C4)C3
|
| InChi Key |
UCAHJECAHMOSHI-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C18H24BrNO/c1-21-17-3-2-16(19)7-15(17)11-20-18-8-12-4-13(9-18)6-14(5-12)10-18/h2-3,7,12-14,20H,4-6,8-11H2,1H3
|
| Chemical Name |
N-[(5-bromo-2-methoxyphenyl)methyl]adamantan-1-amine
|
| 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) |
DMSO : ~125 mg/mL (~356.85 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (17.84 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 6.25 mg/mL (17.84 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 6.25 mg/mL (17.84 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8548 mL | 14.2739 mL | 28.5478 mL | |
| 5 mM | 0.5710 mL | 2.8548 mL | 5.7096 mL | |
| 10 mM | 0.2855 mL | 1.4274 mL | 2.8548 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.