MRT-83 (hydrochloride) is the potent antagonist of Smoothened (Smo) receptor. MRT-83 (hydrochloride) inhibits the Hedgehog (Hh) signaling pathway and BODIPY-cyclopamine binding to human Smo. MRT-83 (hydrochloride) has the potential for researching cancer disease.
| Molecular Weight | 575.05 |
| Formula | C31H31ClN4O5 |
| CAS Number | 1359944-60-7 |
| Form | Solid |
| Solubility (25°C) | DMSO 250 mg/mL (ultrasonic) |
| Storage | 4°C, dry, sealed |
| 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 Smo Products |
|---|
| Glasdegib Maleate
Glasdegib Maleate is an orally bioavailable Smoothened (Smo) inhibitor with an IC50 value of 4 nM for studies related to acute myeloid leukemia. |
| MRT-81
MRT-81 is a potent antagonist of human and rodent smoothened (Smo) receptors, with an IC50 value of 41 nM in the Shh-light2 cells. MRT-81 has potent hedgehog inhibiting activity. MRT-81 can be used for the research of cancer. |
| Fluticasone
Fluticasone is a corticosteroid and Smo agonist with an IC50 of 99 nM, which activates the Hedgehog signaling pathway and promotes the proliferation of primary neural stem or precursor cells, and can be used in respiratory related studies. |
| HhAntag
HhAntag is a specific, potent and orally active small molecule SMO antagonist of the Hh pathway. |
| PF-5274857 hydrochloride
PF-5274857 hydrochloride is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-5274857 hydrochloride has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway. |
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