| Size | Price | |
|---|---|---|
| 5mg | ||
| Other Sizes |
| Targets |
Progesterone receptor membrane component 1 (Pgrmc1). AG-205 is a potent inhibitor of Pgrmc1.
|
|---|---|
| ln Vitro |
In vitro, AG-205 acts as a potent inhibitor of Pgrmc1. It induces genes involved in sterol synthesis, including the INSIG1 protein, which forms a complex with PGRMC1. The compound also inhibits NF-kB signaling and the activation of the BDNF/PI3K/AKT pathway. It is used in cell-based assays to study the role of PGRMC1 in steroidogenesis, cancer, and neuroprotection.
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| ln Vivo |
In vivo, AG-205 has been studied in animal models of hypoxic ischaemia. It mitigates neuronal resistance to hypoxic ischaemia by inhibiting NF-kB signaling and the activation of the BDNF/PI3K/AKT pathway. The compound may have neuroprotective effects in models of stroke or cerebral ischemia. Specific efficacy data are limited.
|
| Enzyme Assay |
Membranes from cells expressing PGRMC1 or purified PGRMC1 protein are incubated with radiolabeled ligand and varying concentrations of AG-205 (0.001-10 µM) in binding buffer for 60 minutes at 25°C. Nonspecific binding is determined with excess unlabeled ligand. Bound and free radioligand are separated by filtration, and radioactivity is counted. IC50 or Ki values are calculated from competition curves.
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| Cell Assay |
Cells expressing PGRMC1 (e.g., cancer cell lines, neuronal cells) are treated with AG-205 (0.1-100 µM) for 24-72 hours. PGRMC1 activity is assessed by measuring downstream signaling pathways (e.g., INSIG1 expression, NF-kB activity, BDNF/PI3K/AKT activation). Cell viability is assessed by MTT or CellTiter-Glo assays. Sterol synthesis genes (e.g., INSIG1) are measured by qPCR.
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| Animal Protocol |
AG-205 is administered to rodents via intraperitoneal or intravenous injection at doses typically ranging from 1-30 mg/kg. In models of hypoxic ischaemia, animals are subjected to oxygen-glucose deprivation or middle cerebral artery occlusion. Neurological outcomes, infarct size, and markers of inflammation and apoptosis are assessed.
|
| References |
| Molecular Formula |
C22H23CLN6OS
|
|---|---|
| Molecular Weight |
454.98
|
| Exact Mass |
454.134
|
| CAS # |
442656-02-2
|
| PubChem CID |
4240652
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
3.553
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
31
|
| Complexity |
650
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
ClC1C=CC(=CC=1)N1C(=NN=N1)SCC(N1C2C=CC(C)=CC=2C2CN(C)CCC12)=O
|
| InChi Key |
GJNBAISSZRNGTM-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C22H23ClN6OS/c1-14-3-8-19-17(11-14)18-12-27(2)10-9-20(18)28(19)21(30)13-31-22-24-25-26-29(22)16-6-4-15(23)5-7-16/h3-8,11,18,20H,9-10,12-13H2,1-2H3
|
| Chemical Name |
2-[1-(4-chlorophenyl)tetrazol-5-yl]sulfanyl-1-(2,8-dimethyl-3,4,4a,9b-tetrahydro-1H-pyrido[4,3-b]indol-5-yl)ethanone
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| Synonyms |
AG 205 AG205 AG-205
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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)
|
| 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 | 2.1979 mL | 10.9895 mL | 21.9790 mL | |
| 5 mM | 0.4396 mL | 2.1979 mL | 4.3958 mL | |
| 10 mM | 0.2198 mL | 1.0989 mL | 2.1979 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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