1. Metabolic Enzyme/Protease
  2. Indoleamine 2,3-Dioxygenase (IDO)
  3. IDO2-IN-1

IDO2-IN-1 

Cat. No.: HY-151093 Purity: 98.86%
COA Handling Instructions

IDO2-IN-1 is an orally active and potent Indoleamine 2,3-dioxygenase 2 (IDO2) inhibitor with an IC50 value of 112 nM. IDO2-IN-1 can be used for inflammatory autoimmunity research.

For research use only. We do not sell to patients.

IDO2-IN-1 Chemical Structure

IDO2-IN-1 Chemical Structure

CAS No. : 2803768-09-2

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5 mg USD 480 In-stock
10 mg USD 760 In-stock
25 mg USD 1520 In-stock
50 mg USD 2430 In-stock
100 mg USD 3880 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE IDO2-IN-1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

IDO2-IN-1 is an orally active and potent Indoleamine 2,3-dioxygenase 2 (IDO2) inhibitor with an IC50 value of 112 nM. IDO2-IN-1 can be used for inflammatory autoimmunity research[1].

IC50 & Target

IDO1

411 nM (IC50)

IDO2

112 (IC50)

In Vitro

IDO2-IN-1 (compound 22) shows stronger inhibition on IDO2 (IC50 =112 nM) over IDO1 (IC50 =411 nM)[1].
IDO2-IN-1 inhibits hIDO1 expression (EC50=633 nM) in HeLa cell-based IDO1/kynurenine assay, co-incubated with hIFN-γ (100 ng/mL final concentration), which is used for producing N-formylkynurenine[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: HeLa cells line expressing hIDO1 induced by IFN-γ
Concentration: 1 nM-0.1 mM
Incubation Time: 48 hours
Result: Showed additional potency against IDO1 with an EC50 value of 633 nM.
In Vivo

The Adjuvant arthritis (AA) model and Collagen-induced arthritis (CIA) model have similar pathogenesis and pathological characteristics to human rheumatoid arthritis (RA).
IDO2-IN-1 (compound 22) (100 mg/kg; p.o.; once dose) exhibits excellent anti-inflammatory activity, higher than naproxen, a prescription drug reducing pain, swelling, and joint stiffness from arthritis[1].
IDO2-IN-1 (25, 50, 100 mg/kg; i.p.; once daily, for 19 d) exhibits excellent inhibitory effect on mice paw swelling, shows efficacy in a collagen-induced arthritis model in mice[1].
IDO2-IN-1 (30, 60, 120 mg/kg; i.p.; once daily, for 15 d) inhibits joint inflammation and displays potential effect in autoimmune arthritis improvement[1].
Pharmacokinetic Profile in Rat[1]

Route Dose (mg/kg) T1/2/sub> (h) Tmax (h) Cmax (ng/mL) AUC(0-∞) (h•ng/mL) CL (mL/h/kg) Vz (mL/kg) MRT(0-∞) (h) F (%)
i.v. 1 0.69 / / 375.1 2673 2675 0.55 /
p.o. 10 2.02 0.75 153.8 670.5 / / 7.48 17.87

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Xylene-induced ear swelling mouse model (ICR mice, male, 6 weeks old)[1]
Dosage: 100 mg/kg
Administration: Oral gavage; once dose; evenly coated right ear with 25 μL of xylene after 1 h treatment
Result: Significantly relieved mouse ear swelling with a high swelling inhibition rate of 65.32%.
Animal Model: Collagen-induced arthritis (CIA) mice model (DBA/1J mice, male, 6 weeks old)[1]
Dosage: 25, 50, 100 mg/kg
Administration: Intraperitoneal injection; once daily; 19 days, began on day 56 after collagen induced
Result: Decreased the expression of inflammatory cytokines IL-18 and IL-33.
Reduced inflammation and cartilage and bone erosions symptoms.
Animal Model: Adjuvant arthritis (AA) rat model (Sprague-Dawley rats, male, 180 ± 20 g)[1]
Dosage: 30, 60, 120 mg/kg
Administration: Intraperitoneal injection; once daily; 15 days, began on day 21 after chondrex induced
Result: Significantly reduced IL-6 and TNF-α levels.
Decreased synovial hyperplasia accompanied by inflammatory cell infiltration, pannus formation, and bone erosion of cartilage in a dose-dependent manner.
Molecular Weight

541.36

Appearance

Solid

Formula

C21H21BrN10O3

CAS No.
SMILES

BrC1=CC=CC(CN/C(C2=NON=C2NCCN3C=C(N=N3)CNC(C4=NC=CC=C4)=O)=N\O)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 140 mg/mL (258.61 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8472 mL 9.2360 mL 18.4720 mL
5 mM 0.3694 mL 1.8472 mL 3.6944 mL
10 mM 0.1847 mL 0.9236 mL 1.8472 mL
*Please refer to the solubility information to select the appropriate solvent.
Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
IDO2-IN-1
Cat. No.:
HY-151093
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