NV-5138, a leucine analogue, is the first selective, orally active intra-brain mTORC1 agonist in combination with Sestrin2. NV-5138 can be used in biological studies of antidepressants.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO ≥ 100 mg/mL|
|Related mTOR Products|
The selective mTORC1 complex inhibitor RMC-4529 is a bidentate inhibitor that has a rapamycin-derived, FKBP12-induced heterologous mTOR inhibitor covalently linked to an active-site (orthologous) inhibitor.
PQR620 is an orally bioavailable and selective brain penetrant inhibitor of mTORC1/2.
mTOR inhibitor-3 is a remarkably selective mTOR inhibitor with a Ki of 1.5 nM. mTOR inhibitor-3 suppresses mTORC1 and mTORC2 in cellular and in vivo pharmacokinetic (PK)/pharmacodynamic (PD) experiments.
Jr-ab2-011 is a selective mTORC2 inhibitor with an IC50 value of 0.36 μM. Jr-ab2-011 inhibited mTORC2 activity by blocking the Rictor-MTOR complex (Ki: 0.19 μM). Jr-ab2-011 has anti-glioblastoma multiforme (GBM) activity.
MTI-31 (LXI-15029) is a novel low-toxicity mTORC1/mTORC2 inhibitor, demonstrated a potent mTOR binding affinity with >5000 fold selectivity over the related PI3K family isoforms. MTI-31 inhibited mTORC1- and mTORC2 function at ≤120 nM in cellular assays.
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