| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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IDO1/TDO-IN-4 is a novel dual IDO1/TDO inhibitor, with IC50 values of 3.53 μM (IDO1) and 1.15 μM (TDO). It has the potential to be used in the treatment of depression, and depression-induced infectious, metabolic, and autoimmune disorders.
| ln Vitro |
According to morphological alterations, LPS-induced BV2 microglial activation is inhibited by IDO1/TDO-IN-4 (Compound 28, 0-2 μM, 1 hour) [1]. IDO1/TDO-IN-4 (0-2 μM, 1 h) stimulates the expression of IL-10 while suppressing the synthesis of pro-inflammatory factors [1]. IDO1/TDO-IN-4 (0-2 μM, 1 hour) inhibits the over-degradation of tryptophan via the kynurenine pathway and lowers IDO1 expression [1].
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| ln Vivo |
Compound 28, administered intraperitoneally at a dose of 20 mg/kg on days 1, 2, and 3, has the ability to rescue mice from LPS-induced neuroinflammation and depressive-like behavior [1]. In normal mice, the intravenous injection (20 mg/kg) of IDO1/TDO-IN-4 shows a high steady-state volume of distribution and high exposure [1].
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| Cell Assay |
RT-PCR[1]
Cell Types: 100 ng/mL LPS-induced BV2 microglia Tested Concentrations: 0, 0.25, 0.5, 1, 2 μM Incubation Duration: 1 h Experimental Results: Inhibition of COX2, iNOS, TNF-α, and IL-1β. IL-10 levels are elevated. |
| Animal Protocol |
Animal/Disease Models: 2 mg/kg LPS-induced depression in mice [1]
Doses: 20 mg/kg Route of Administration: intraperitoneal (ip) injection, days 1, 2, and 3. Experimental Results: Microglial activation was Dramatically attenuated. Hippocampal inflammatory factors were diminished, such as TNF-α, IL-1β, and iNOS. Downregulates LPS-induced IDO1 overexpression. Animal/Disease Models: Male C57BL/6J mice (pharmacokinetic/PK/PK determination) [1] Doses: 20 mg/kg Route of Administration: intraperitoneal (ip) injection and intravenous (iv) (iv)injection Experimental Results: IDO1/TDO-IN-4 (compound 28) pharmacokinetic/PK/PKs Chemical properties T1/2 (h) Tmax (h) Cmax (ng/mL) Bioavailability F (%) iv/ip 2.31/0.77 0.25 5543.99/3878 52.55 |
| References |
| Molecular Formula |
C14H10N4
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|---|---|
| Molecular Weight |
234.26
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| Exact Mass |
234.09
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| CAS # |
461424-21-5
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| PubChem CID |
44269517
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| Appearance |
Yellow to brown solid powder
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| LogP |
2.2
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
18
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| Complexity |
308
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1C=C2C(NC3C2=CC=NC=3C2=CN=CN2)=CC=1
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| InChi Key |
HUTBKGSJEGKJBG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H10N4/c1-2-4-11-9(3-1)10-5-6-16-14(13(10)18-11)12-7-15-8-17-12/h1-8,18H,(H,15,17)
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| Chemical Name |
1-(1H-imidazol-5-yl)-9H-pyrido[3,4-b]indole
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~533.60 mM)
MEthanol : ~16.67 mg/mL (~71.16 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (8.88 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.2688 mL | 21.3438 mL | 42.6876 mL | |
| 5 mM | 0.8538 mL | 4.2688 mL | 8.5375 mL | |
| 10 mM | 0.4269 mL | 2.1344 mL | 4.2688 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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