| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg |
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| 250mg |
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| Targets |
BT-13 targets the GDNF receptor RET, a receptor tyrosine kinase. It is a selective agonist that activates the RET signaling pathway independently of GFLs. By promoting RET phosphorylation and activating RET-dependent intracellular signaling cascades, it promotes neuronal survival, differentiation, and regeneration.
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| ln Vitro |
While BT-13 promotes RET's phosphorylation and intracellular signal absorption, RET does not activate intracellular signals or cause NGF or BDNF to bind to TrkA or TrkB, respectively, when RET is not present [1].
In vitro, BT-13 stimulates phosphorylation of RET and RET-dependent intracellular signaling. It activates neither the NGF receptor TrkA nor the BDNF receptor TrkB, nor does it activate intracellular signaling in the absence of RET, confirming its selectivity. It promotes neurite growth from sensory neurons. |
| ln Vivo |
In addition to having modest analgesic and antihyperalgesic effects, BT-13 (20 and 25 mg/kg bound to left L5 and L6 spinal nerve ligation induction) shields DRG neurons from neurological symptoms brought on by surgery [1].
In vivo, BT-13 (20 and 25 mg/kg) in rats with spinal nerve ligation-induced neuropathy has a slight antinociceptive/antihyperalgesic effect and protects dorsal root ganglion (DRG) neurons. It represents a promising neuroprotective agent for studying RET-mediated signaling and neuropathic pain therapy. |
| Enzyme Assay |
The in vitro RET phosphorylation assay for BT-13 involves treating cells with the compound and measuring the phosphorylation of RET and downstream signaling molecules by Western blotting. The selectivity of BT-13 is confirmed by testing its activity against other receptor tyrosine kinases, such as TrkA and TrkB.
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| Cell Assay |
In vitro cell culture studies for BT-13 utilize sensory neurons to study its effects on neurite growth. Neurons are treated with the compound, and neurite length and branching are quantified by microscopy.
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| Animal Protocol |
Animal/Disease Models: Rats were induced by ligating the left L5 and L6 spinal nerves [1].
Doses: 5-25mg/kg, dissolved in sesame oil containing 5% DMSO. Route of Administration: subcutaneous injection on postoperative days 1, 3, 5, 8, 10, and 12. Experimental Results: 20 and 25 mg/kg diminished mechanical hypersensitivity and normalized the expression of sensory neuron markers in dorsal root ganglia. In vivo animal experiments for BT-13 are performed in rat models of neuropathic pain induced by ligation of left L5 and L6 spinal nerves. The compound is administered at doses of 20 and 25 mg/kg, and its antinociceptive and antihyperalgesic effects are assessed. Protection of DRG neurons is evaluated by histology. |
| ADME/Pharmacokinetics |
BT-13 has a molecular weight of 517.54 g/mol and is soluble in DMSO. It is typically stored as a powder at -20°C for up to 3 years. In solution, it is stable at -80°C for 6 months and at -20°C for 1 month.
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| Toxicity/Toxicokinetics |
Toxicological data for BT-13 are limited, as it is a research compound. In preclinical studies, it is well-tolerated at therapeutic doses of 20-25 mg/kg. It is not intended for human use. Standard safety precautions should be followed.
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| References | |
| Additional Infomation |
BT-13 is a research compound with no clinical approval. It is a valuable tool for studying GDNF receptor RET signaling and its role in neuronal survival, differentiation, and regeneration. It is used in drug discovery programs to explore the therapeutic potential of RET agonists for neuropathic pain and neurodegenerative diseases.
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| Molecular Formula |
C23H27F4N3O4S
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|---|---|
| Molecular Weight |
517.536798715591
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| Exact Mass |
517.165
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| CAS # |
924537-98-4
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| PubChem CID |
46088379
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| Appearance |
White to off-white solid powder
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| LogP |
3.8
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
35
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| Complexity |
811
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(N1CCN(C2C(OC)=CC=C(S(N(CC)CC)(=O)=O)C=2)CC1)C1C(C(F)(F)F)=CC(F)=CC=1
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| InChi Key |
GTDJOGZANHPKMR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H27F4N3O4S/c1-4-30(5-2)35(32,33)17-7-9-21(34-3)20(15-17)28-10-12-29(13-11-28)22(31)18-8-6-16(24)14-19(18)23(25,26)27/h6-9,14-15H,4-5,10-13H2,1-3H3
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| Chemical Name |
N,N-diethyl-3-[4-[4-fluoro-2-(trifluoromethyl)benzoyl]piperazin-1-yl]-4-methoxybenzenesulfonamide
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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)
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| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~48.31 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.83 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 (4.83 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 | 1.9322 mL | 9.6611 mL | 19.3222 mL | |
| 5 mM | 0.3864 mL | 1.9322 mL | 3.8644 mL | |
| 10 mM | 0.1932 mL | 0.9661 mL | 1.9322 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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