| Identification | Back Directory | [Name]
Methanone, [4-[5-[(3,4-dihydro-2(1H)-isoquinolinyl)sulfonyl]-2-methoxyphenyl]-1-piperazinyl][4-fluoro-2-(trifluoromethyl)phenyl]- | [CAS]
924759-42-2 | [Synonyms]
BT44
RET agonist BT44
Methanone, [4-[5-[(3,4-dihydro-2(1H)-isoquinolinyl)sulfonyl]-2-methoxyphenyl]-1-piperazinyl][4-fluoro-2-(trifluoromethyl)phenyl]- | [Molecular Formula]
C28H27F4N3O4S | [MOL File]
924759-42-2.mol | [Molecular Weight]
577.59 |
| Chemical Properties | Back Directory | [Boiling point ]
726.5±70.0 °C(Predicted) | [density ]
1.386±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
0.20±0.20(Predicted) | [color ]
White to off-white | [InChIKey]
MFQBJWVTKPJNEP-UHFFFAOYSA-N | [SMILES]
C(N1CCN(C2=CC(S(N3CCC4=C(C3)C=CC=C4)(=O)=O)=CC=C2OC)CC1)(C1=CC=C(F)C=C1C(F)(F)F)=O |
| Hazard Information | Back Directory | [Description]
BT44 is a novel RET agonist for the treatment of experimental neuropathies. | [Uses]
BT44 is a selective RET activator. BT44 can penetrate through the blood-brain barrier and can be used for the research of neurodegenerative disorders and diabetes mellitus[1][2]. | [in vivo]
BT44 (5-25 mg/kg; s.c.; every second day for 10, 42 or 14 days) alleviates sensory signs in the SNL and STZ models of neuropathic[1].
BT44 (12.5 or 25 mg/kg; s.c.; every second day for 10 days) protects IB4-positive neurons in DRGs of animals with experimental neuropathy[1].
BT44 (0.1 and 0.3 μg/24 h; infuse into the right dorsal striatum for 14 days) reverses amphetamine-induced motor imbalance and seems to protect dopaminergic fibers in the striatum in 6-OHDA rat model of Parkinson’s disease[2].
BT44 (10 mg/kg; i.v.) penetrates the blood-brain barrier and is rapidly eliminated from the circulation (half-life (t1/2) = 0.72 h) and brain (t1/2 = 0.47 h) in rats[2]. | Animal Model: | Wistar rats, spinal nerve ligation (SNL) and Streptozotocin (STZ; HY-13753)-induced diabetes mellitus models[1] | | Dosage: | 5, 12.5 or 25 mg/kg | | Administration: | Subcutaneous injecton, every second day for 10, 42 or 14 days | | Result: | Alleviated mechanical allodynia in the SNL animals. Treatment with the dose of 5 mg/kg alleviated mechanical hyperalgesia in the STZ-treated animals, while the 12.5 mg/kg dose was not effective. Concentration of 5 mg/kg attenuated cold allodynia in the STZ-treated animals during the first two weeks while the effect of 12.5 mg/kg was not significant. |
| Animal Model: | Wistar rats, SNL-induced diabetes mellitus model[1] | | Dosage: | 12.5 or 25 mg/kg | | Administration: | Subcutaneous injecton, every second day for 10 days | | Result: | Led to a significant increase in the number of IB4 expressing neurons in the ipsilateral DRGs. The 12.5 mg/kg dose protected IB4-positive neurons from SNL-induced lesion. |
| [References]
[1] Viisanen H, et al. Novel RET agonist for the treatment of experimental neuropathies. Mol Pain. 2020 Jan-Dec;16:1744806920950866. DOI:10.1177/1744806920950866
[2] Renko JM, et al. Neuroprotective Potential of a Small Molecule RET Agonist in Cultured Dopamine Neurons and Hemiparkinsonian Rats. J Parkinsons Dis. 2021;11(3):1023-1046. DOI:10.3233/JPD-202400 |
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