LM22A-4 is a potent tropomyosin-related kinase B (TrkB) agonist (IC50 = 47 nM). Induces activation of Trk, Akt and ERK in mouse hippocampus and striatum. Reverses deficits in motor task learning in mice following traumatic brain injury; restores respiratory function in a rat model of Rett syndrome. LM22A-4 significantly up-regulates OPN and ALPase mRNA expression in a dose-dependent manner and OC mRNA level is significantly increased by 5 μM of LM22A-4. LM22A-4 significantly increases OPN, ALPase and OC mRNA expression in a time-dependent manner. LM22A-4 stimulated OPN and OC mRNA expression in HCEM cells cultured with mineralizing media.
| Molecular Weight | 339.34 |
| Formula | C15H21N3O6 |
| CAS Number | 37988-18-4 |
| Solubility (25°C) | Water 50 mg/mL DMSO 29 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Trk Products |
|---|
| Cyclotraxin B
Cyclotraxin B, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. |
| Gambogic amide
Gambogic amide is a potent and selective agonist of TrkA and also induces its tyrosine phosphorylation and activation of downstream signaling, including Akt and MAPK. |
| Protein kinase inhibitor 4
Protein kinase inhibitor 4 is a protein kinase inhibitor that inhibits TRK-A and ROS1 (IC50=3.0 nM and 104 nM respectively). |
| TRK-IN-22
TRK-IN-22 is a TRK inhibitor. |
| TrkB-IN-1
TrkB-IN-1 is a potent and orally active TrkB agonist and has favorable PK properties. |
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