| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| Targets |
BT18 targets the GDNF family receptor GFRα1 and the RET receptor tyrosine kinase. By mimicking GDNF, it activates RET-dependent intracellular signaling pathways, promoting neuronal survival and growth. It is a molecule mimic with function similar to glial cell line-derived neurotrophic factor.
|
|---|---|
| ln Vitro |
In the MG87RET cell line, BT18 (50 μM; 1-90 min) time-dependently activates AKT and ERK1/2 [1]. In the MG87RET cell line, BT18 (1-50 μM; 90 min) activates AKT in a dose-dependent manner [1]. GFP-transfected cells and GFRD1-transfected cells appear to phosphorylate RET at a dose of 50 μM when exposed to BT18 (5-50 μM; 15 mimutes) [1].
In vitro, BT18 (1-50 μM; 90 minutes) activates AKT in a dose-dependent manner in MG87RET cells. In the same cell line, BT18 (50 μM; 1-90 minutes) time-dependently activates AKT and ERK1/2. BT18 (5-50 μM; 15 minutes) phosphorylates RET at 50 μM in both GFP- and GFRD1-transfected cells. |
| ln Vivo |
In vivo, BT18 is used as a research tool to study GDNF-like signaling and neuroprotection. It has shown an effect on GDNF family receptor GFRα1 and RET receptor tyrosine kinase RetA function, suggesting potential for treating neurodegenerative diseases.
|
| Enzyme Assay |
The in vitro kinase assay for BT18 involves measuring its ability to activate RET phosphorylation and downstream signaling. Cells are treated with the compound, and the phosphorylation of RET, AKT, and ERK1/2 is measured by Western blotting.
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: MG87RET Cell line Tested Concentrations: 50 μM Incubation Duration: 1, 5, 15, 45, 90 minutes Experimental Results: AKT and ERK1/2 activation was time-dependent. In vitro cell culture studies for BT18 utilize MG87RET cells to study RET activation. Cells are treated with varying concentrations of the compound, and the activation of downstream signaling pathways is assessed by Western blotting. |
| Animal Protocol |
In vivo animal experiments for BT18 are not extensively documented. Its neurotrophic effects could be studied in animal models of neurodegenerative diseases, such as Parkinson's disease or spinal cord injury.
|
| ADME/Pharmacokinetics |
BT18 has a molecular weight of 637.64 g/mol and is soluble in DMSO (98 mg/mL). For in vivo studies, it can be formulated in 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% saline. Powder formulations are stable for up to 3 years at -20°C.
|
| Toxicity/Toxicokinetics |
Toxicological data for BT18 are limited, as it is a research compound. It is not intended for human use. Standard safety precautions for handling chemical reagents should be followed.
|
| References | |
| Additional Infomation |
BT18 is a research compound with no clinical approval. It is a valuable tool for studying GDNF family receptor signaling and the role of RET in neuronal survival and growth. It is used in drug discovery programs to explore the therapeutic potential of GDNF mimetics for neurodegenerative diseases.
|
| Molecular Formula |
C30H31F4N3O6S
|
|---|---|
| Molecular Weight |
637.642260789871
|
| Exact Mass |
637.186
|
| CAS # |
924811-53-0
|
| PubChem CID |
46088742
|
| Appearance |
White to light yellow solid powder
|
| LogP |
4.5
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
12
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
44
|
| Complexity |
1090
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(N1CCN(C2C(OC)=CC=C(S(N3CCC4C(=CC(=C(C=4)OC)OC)C3)(=O)=O)C=2)CC1)C1C(C(F)(F)F)=CC(F)=CC=1
|
| InChi Key |
QVIIZVVDZZHGCB-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C30H31F4N3O6S/c1-41-26-7-5-22(44(39,40)37-9-8-19-14-27(42-2)28(43-3)15-20(19)18-37)17-25(26)35-10-12-36(13-11-35)29(38)23-6-4-21(31)16-24(23)30(32,33)34/h4-7,14-17H,8-13,18H2,1-3H3
|
| Chemical Name |
[4-[5-[(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)sulfonyl]-2-methoxyphenyl]piperazin-1-yl]-[4-fluoro-2-(trifluoromethyl)phenyl]methanone
|
| 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 : ~100 mg/mL (~156.83 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.92 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 25.0 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: ≥ 2.5 mg/mL (3.92 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5683 mL | 7.8414 mL | 15.6828 mL | |
| 5 mM | 0.3137 mL | 1.5683 mL | 3.1366 mL | |
| 10 mM | 0.1568 mL | 0.7841 mL | 1.5683 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
