| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 500mg |
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| Targets |
Izilendustat targets prolyl hydroxylase domain (PHD) enzymes, which regulate HIF-1α and HIF-2α stability by hydroxylating them under normoxic conditions. By inhibiting PHD enzymes, Izilendustat stabilizes HIF-1α and HIF-2, leading to the upregulation of genes involved in erythropoiesis, angiogenesis, and metabolism. This mechanism makes it a potential treatment for anaemia.
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|---|---|
| ln Vitro |
In vitro, Izilendustat is a potent inhibitor of prolyl hydroxylase that stabilizes HIF-1α and HIF-2. It has a molecular weight of 433.94 g/mol and a molecular formula of C22H28ClN3O4. Izilendustat is an investigational small-molecule inhibitor being developed for the treatment of anaemia.
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| ln Vivo |
In vivo, Izilendustat may be used for studying diseases related to the body's immune response, such as intestinal inflammation and other intestinal diseases. It is being developed for the treatment of anaemia, particularly anaemia associated with chronic kidney disease. However, specific published in vivo efficacy studies are not detailed in the current literature.
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| Enzyme Assay |
The in vitro PHD inhibition assay for Izilendustat uses recombinant PHD enzymes and a HIF-1α peptide substrate. Enzyme activity is measured by quantifying the hydroxylation of the substrate using mass spectrometry or antibody-based methods. IC50 values are calculated from dose-response curves. HIF-1α and HIF-2 stabilization is assessed by measuring protein levels by Western blotting.
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| Cell Assay |
Cellular assays for Izilendustat are conducted in various cell lines. Cells are treated with varying concentrations of Izilendustat. HIF-1α and HIF-2 protein levels are measured by Western blotting. The expression of HIF target genes such as erythropoietin (EPO) is measured by qPCR or ELISA. Cell viability is measured using standard assays.
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| Animal Protocol |
In vivo studies for Izilendustat would typically involve animal models of anaemia or inflammatory diseases. The compound would be administered via oral routes. Efficacy would be assessed by measuring haemoglobin levels, red blood cell counts, or inflammatory markers. However, specific published in vivo protocols for Izilendustat are not available in the current literature.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Izilendustat is not extensively reported. The compound has a molecular weight of 433.94 g/mol and a molecular formula of C22H28ClN3O4. It has a CAS number of 1303512-02-8. As a small molecule, it is expected to have good oral bioavailability. Detailed PK parameters such as half-life and bioavailability are not available.
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| Toxicity/Toxicokinetics |
Toxicity data for Izilendustat is limited. As an investigational compound, Izilendustat is intended for research use only and not for human therapeutic applications. Standard in vitro cytotoxicity assays and in vivo tolerability studies would be required for a complete toxicity assessment.
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| References | |
| Additional Infomation |
Izilendustat (CAS 1303512-02-8) is a potent inhibitor of prolyl hydroxylase that stabilizes HIF-1α and HIF-2. It is being developed for the treatment of anaemia, particularly anaemia associated with chronic kidney disease. It has a molecular formula of C22H28ClN3O4 and a molecular weight of 433.94 g/mol. Izilendustat is for research use only.
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| Molecular Formula |
C22H28CLN3O4
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|---|---|
| Molecular Weight |
433.928424835205
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| Exact Mass |
433.176
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| CAS # |
1303512-02-8
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| Related CAS # |
Izilendustat hydrochloride;1303513-80-5
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| PubChem CID |
52912218
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| Appearance |
White to off-white solid powder
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| LogP |
2.4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
30
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| Complexity |
700
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C=CC(=CC=1)CN1C=CC(=C(C1=O)O)CN1CCN(C(=O)OC(C)(C)C)CC1
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| InChi Key |
UPJZLOCUUOIMNC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H28ClN3O4/c1-22(2,3)30-21(29)25-12-10-24(11-13-25)15-17-8-9-26(20(28)19(17)27)14-16-4-6-18(23)7-5-16/h4-9,27H,10-15H2,1-3H3
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| Chemical Name |
tert-butyl 4-[[1-[(4-chlorophenyl)methyl]-3-hydroxy-2-oxopyridin-4-yl]methyl]piperazine-1-carboxylate
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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 : ~25 mg/mL (~57.61 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3045 mL | 11.5226 mL | 23.0452 mL | |
| 5 mM | 0.4609 mL | 2.3045 mL | 4.6090 mL | |
| 10 mM | 0.2305 mL | 1.1523 mL | 2.3045 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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