1. Metabolic Enzyme/Protease
  2. Indoleamine 2,3-Dioxygenase (IDO)

IDO5L 

Cat. No.: HY-15683 Purity: 99.29%
Data Sheet SDS Handling Instructions

IDO-IN-2 is a potent IDO1 inhibitor with IC50 of 19 nM in Hela cell assay.

For research use only. We do not sell to patients.
IDO5L Chemical Structure

IDO5L Chemical Structure

CAS No. : 914471-09-3

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10 mM * 1 mL in DMSO USD 79 In-stock
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10 mg USD 108 In-stock
50 mg USD 300 In-stock
100 mg USD 420 In-stock
200 mg USD 540 In-stock
500 mg USD 660 In-stock
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

IDO-IN-2 is a potent IDO1 inhibitor with IC50 of 19 nM in Hela cell assay.

IC50 & Target

IC50: 19 nM (IDO1, in HeLa cell)[1]

In Vitro

IDO5L is a potent (HeLa IC50=19 nM) competitive inhibitor of IDO[1]. IDO5L is one of the highest potent inhibitors of the IDO1 (IC50=19 nM, in HeLa cell assay)[2].

In Vivo

Testing of IDO5L in mice demonstrates pharmacodynamic inhibition of IDO, as measured by decreased kynurenine levels (>50%) in plasma and dose dependent efficacy in mice bearing GM-CSF-secreting B16 melanoma tumors. Initial oral pharmacokinetic studies show that IDO5L is rapidly cleared (t1/2<0.5 h) and that oral administration will not be a suitable dosing method for in vivo studies. The measured plasma exposure (2.5 μM) of IDO5L during this period exceeded our calculated mouse protein binding adjusted B16 cellular IC50 (PBadjIC50=1.0 μM, murine cellular B16 IC50=46 nM). Notably, kynurenine levels increase back to baseline after 4 h as IDO5L exposure levels decreased below the mouse PBadjIC50 from 1.0 to 0.1 μM[1].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 3.6813 mL 18.4067 mL 36.8134 mL
5 mM 0.7363 mL 3.6813 mL 7.3627 mL
10 mM 0.3681 mL 1.8407 mL 3.6813 mL
Please refer to the solubility information to select the appropriate solvent.
Animal Administration
[1]

IDO-IN-2 is dissolved in DMSO and then diluted with PBS or saline[1].

Mice[1]
A single subcutaneous 100 mg/kg dose of IDO5L is administered to naive C57BL/6 mice bearing GM-CSF-secreting B16 tumors. Blood is harvested from individual mice over 8 h. Kynurenine and IDO5L concentrations are measured by LCMS. Reductions of kynurenine levels by 50−60% are observed between 2 and 4 h, with maximum inhibition seen at 2.5 h. Tumors are allowed to grow until day 7 when 14 days of subcutaneous dosing of IDO5L at 25, 50, and 75 mg/kg b.i.d. is initiated. Dose dependent inhibition of tumor growth is correlated with increasing exposures of IDO5L in plasma. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

271.64

Formula

C₉H₇ClFN₅O₂

CAS No.

914471-09-3

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 52 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.29%

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Product Name:
IDO5L
Cat. No.:
HY-15683
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