1. Metabolic Enzyme/Protease Anti-infection
  2. HIF/HIF Prolyl-Hydroxylase Bacterial
  3. Izilendustat

Izilendustat is a potent prolyl hydroxylase inhibitor. Izilendustat competitively inhibits HIFPH2 activity, blocks HIF-1α degradation, stabilizes HIF-1α and HIF-2α proteins, and upregulates downstream target gene expression. Izilendustat can reduce intestinal inflammation and damage, enhance the ability of phagocytes to clear pathogens, and improve ischemia-related pathological phenotypes. Izilendustat can be used for the research of inflammatory bowel disease, ischemic vascular disease and anemia.

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

Izilendustat

Izilendustat Chemical Structure

CAS No. : 1303512-02-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
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Description

Izilendustat is a potent prolyl hydroxylase inhibitor. Izilendustat competitively inhibits HIFPH2 activity, blocks HIF-1α degradation, stabilizes HIF-1α and HIF-2α proteins, and upregulates downstream target gene expression. Izilendustat can reduce intestinal inflammation and damage, enhance the ability of phagocytes to clear pathogens, and improve ischemia-related pathological phenotypes. Izilendustat can be used for the research of inflammatory bowel disease, ischemic vascular disease and anemia[1][2].

IC50 & Target[1]

HIF-1α

 

HIF-2

 

Cellular Effect
Cell Line Type Value Description References
HEK293 EC50
17 μM
Compound: 53
Inhibition of PHD2 in HEK293 cells assessed as VEGF release by immunoassay
Inhibition of PHD2 in HEK293 cells assessed as VEGF release by immunoassay
[PMID: 23977883]
In Vitro

Izilendustat (Compound A41) (1.2 μM) inhibits HIFPH2 (EGLN1) activity in enzymatic assays[1].
Izilendustat (Compound A41) (1-50 μM; 7 h) upregulates PGK and VEGF expression in wild-type MEFs but not in HIF-1α knockout MEFs[2].
Izilendustat (10 μM) enhances bacterial clearance in U937 cells infected with S. aureus (Newman or MRSA strain)[2].

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

In Vivo

Izilendustat (Compound A41) (0.3-5 mg/kg; s.c.; once daily) prevents body weight loss, ameliorates colon shortening, reduces disease activity scores, decreases mesenteric lymph node leukocyte count and maintains hematocrit levels in TNBS-induced colitis mice[1].
Izilendustat (5-10 mg/kg; s.c.; every other day) enhances the antitumor effect of 5-Fluorouracil (HY-90006) in mouse colon 26 carcinoma xenograft models[1].
Izilendustat (Compound A41) (0.5-10 mg/kg; p.o./s.c.; once daily) reduces skin lesion size and bacterial load in S. aureus- and S. pyogenes-infected mice[2].

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

Molecular Weight

433.94

Formula

C22H28ClN3O4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1CCN(CC(C=CN2CC3=CC=C(Cl)C=C3)=C(O)C2=O)CC1)OC(C)(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (57.61 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3045 mL 11.5223 mL 23.0447 mL
5 mM 0.4609 mL 2.3045 mL 4.6089 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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C1

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Volume (start)

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C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.01%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3045 mL 11.5223 mL 23.0447 mL 57.6117 mL
5 mM 0.4609 mL 2.3045 mL 4.6089 mL 11.5223 mL
10 mM 0.2304 mL 1.1522 mL 2.3045 mL 5.7612 mL
15 mM 0.1536 mL 0.7682 mL 1.5363 mL 3.8408 mL
20 mM 0.1152 mL 0.5761 mL 1.1522 mL 2.8806 mL
25 mM 0.0922 mL 0.4609 mL 0.9218 mL 2.3045 mL
30 mM 0.0768 mL 0.3841 mL 0.7682 mL 1.9204 mL
40 mM 0.0576 mL 0.2881 mL 0.5761 mL 1.4403 mL
50 mM 0.0461 mL 0.2304 mL 0.4609 mL 1.1522 mL
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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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Izilendustat
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