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1-methyltryptophan (1 MT) is currently the most widely used IDO1 inhibitor with moderate inhibitory activity. However, the two stereoisomers of 1-mt exhibit different potency :(I) d-1 MT(1) is in phase iii clinical trials as an inhibitor of the Trp -- Kyn pathway, but does not inhibit IDO1 in vitro; (ii)L-1 MT(8), as a competitive substrate inhibitor of L-tryptophan, has moderate inhibitory activity against IDO1 (hIDO1 IC50=42μM, HeLa IDO1 IC50=18.4μM).
| Molecular Weight | 218.25 |
| Formula | C12H14N2O2 |
| CAS Number | 26988-72-7 |
| Solubility (25°C) | Water：2.5 mg/mL |
| Storage | 4°C, protect from light, 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 IDO Products |
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| IDO-IN-18
IDO-IN-18 is an IDO inhibitor. |
| IDO1-IN-21
IDO1-IN-21 is an IDO1 inhibitor (IC50 = 0.64 μM). |
| IDO1-IN-22
IDO1-IN-22 is a IDO1 inhibitor (biochemical hIDO1 IC50: 67.4 nM, HeLa hIDO1 IC50: 17.6 nM). |
| IDO1/TDO-IN-6
IDO1/TDO-IN-6 is a dual inhibitor of IDO1/TDO with IC50s of 2.25 and 2.89 μM, respectively. |
| IDO-IN-13
IDO-IN-13 is a potent indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an EC50 of 17 nM, extracted from patent WO2019040102A1, example 43. |
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