| Identification | Back Directory | [Name]
(E)-3-(2-(1H-tetrazol-5-yl)vinyl)-6-fluoro-1H-indole | [CAS]
1316695-35-8 | [Synonyms]
LM 10
104221
(E)-3-(2-(1H-tetrazol-5-yl)vinyl)-6-fluoro-1H-indole
6-Fluoro-3-[(1E)-2-(2H-tetrazol-5-yl)ethenyl]-1H-indole
1H-Indole, 6-fluoro-3-[(1E)-2-(2H-tetrazol-5-yl)ethenyl]- | [Molecular Formula]
C11H8FN5 | [MDL Number]
MFCD26097257 | [MOL File]
1316695-35-8.mol | [Molecular Weight]
229.21 |
| Chemical Properties | Back Directory | [Boiling point ]
522.5±60.0 °C(Predicted) | [density ]
1.556±0.06 g/cm3(Predicted) | [storage temp. ]
Inert atmosphere,2-8°C | [solubility ]
Soluble in DMSO | [form ]
A solid | [pka]
4.23±0.10(Predicted) | [color ]
Off-white to light yellow | [InChI]
1S/C11H8FN5/c12-8-2-3-9-7(6-13-10(9)5-8)1-4-11-14-16-17-15-11/h1-6,13H,(H,14,15,16,17)/b4-1+ | [InChIKey]
JDBSZVDIUIRSDG-DAFODLJHSA-N | [SMILES]
FC1=CC2=C(C=C1)C(/C=C/C3=NN=NN3)=CN2 |
| Hazard Information | Back Directory | [Uses]
LM 10 is an inhibitor of tryptophan 2,3-dioxygenase (TDO) and shows reversal of tumoral immune resistance via this inhibition process. | [Biological Activity]
LM10 is an orally available, aqueous soluble, potent, selective and non-toxic tryptophan 2,3-dioxygenase (TDO) inhibitor. LM10 diminishes tryptophan degradation and effectively prevents the growth of TDO-expressing P815 tumor cells by reversing immune resistance in immune competent but not in immunodeficient mice ( at a dose of 4 mg/day, 1 mg/ml in water, pH 9.0). LM10 suppresses autoimmune reactions induced by mouse hepatitis virus in mice. | [in vivo]
LM10 (160 mg/kg; p.o.) prevents the growth of TDO-expressing P815 tumor cells and promotes better rejection of control clone P815B cl1, which does not express TDO[1].
LM10 displays a good TDO inhibition (Ki = 5.6 μM) with a competitive inhibition profile[1].
LM10 does not inhibit IDO and has a high solubility and bioavailability without obvious signs of toxicity[1].
The plasma concentration of LM10 after oral administration of 160 mg/kg/day is between 20 and 40 μg/mL (87-175 μM), a concentration about 40 times above the IC50 measured in the cellular assay performed with the physiological concentration of plasma tryptophan[1]. | Animal Model: | DBA/2 mice (6-8 weeks)[1] | | Dosage: | 160 mg/kg/day | | Administration: | p.o. | | Result: | Prevented the growth of TDO-expressing P815 tumor cells and promoted better rejection of control clone P815B cl1, which does not express TDO.
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| Company Name: |
ChemShuttle, Inc.
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| Tel: |
0510-83588313-811 18800520310 |
| Website: |
https://www.jiehuapharma.com/ |
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