| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg |
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| 1g |
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| Other Sizes |
| Targets |
HIF-PHD-IN-3 targets hypoxia-inducible factor prolyl hydroxylases (HIF-PHDs), enzymes that regulate HIF-1α stability by hydroxylating it under normoxic conditions. By inhibiting HIF-PHDs, HIF-PHD-IN-3 stabilizes HIF-1α, leading to the upregulation of heme oxygenase-1 (HO-1). This mechanism makes it a cardioprotective agent and a potential treatment for anaemia.
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| ln Vitro |
In vitro, HIF-PHD-IN-3 induces upregulation of heme oxygenase-1 (HO-1). It is a potent hiPSC-CM cardioprotective scaffold. HIF-PHD-IN-3 has potential inhibitory effects on HIF-PHDs and can be used to study anaemia. It has a molecular formula of C16H13N3OS2 and a molecular weight of 327.42 g/mol.
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| ln Vivo |
In vivo data for HIF-PHD-IN-3 is not extensively reported in publicly available sources. As a potent inducer of HO-1 through HIF-PHD inhibition, the compound has potential applications in animal models of ischaemic heart disease and anaemia. By upregulating HO-1 and stabilizing HIF-1α, HIF-PHD-IN-3 could provide cardioprotective and erythropoietic effects. However, specific published in vivo efficacy studies are not detailed in the current literature.
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| Enzyme Assay |
The in vitro HIF-PHD inhibition assay for HIF-PHD-IN-3 uses recombinant HIF-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. HO-1 upregulation is assessed in hiPSC-CMs or other cell types by measuring HO-1 protein levels by Western blotting or mRNA levels by qPCR.
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| Cell Assay |
Cellular assays for HIF-PHD-IN-3 are conducted in hiPSC-CMs or other cell types. Cells are treated with varying concentrations of HIF-PHD-IN-3. HO-1 protein levels are measured by Western blotting. HIF-1α protein levels are measured by Western blotting. Cell viability is measured using standard assays such as MTT or CellTiter-Glo. The compound's cardioprotective effects are assessed under stress conditions.
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| Animal Protocol |
In vivo studies for HIF-PHD-IN-3 would typically involve animal models of ischaemic heart disease or anaemia. The compound would be administered via intraperitoneal or oral routes. Efficacy would be assessed by measuring HO-1 expression, cardiac function, or haemoglobin levels. However, specific published in vivo protocols for HIF-PHD-IN-3 are not available in the current literature.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for HIF-PHD-IN-3 is not extensively reported. The compound has a molecular weight of 327.42 g/mol and a molecular formula of C16H13N3OS2. It has a CAS number of 794582-71-1. As a small molecule, it is expected to have moderate bioavailability. Detailed PK parameters such as half-life and bioavailability are not available.
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| Toxicity/Toxicokinetics |
Toxicity data for HIF-PHD-IN-3 is limited. As a research compound, HIF-PHD-IN-3 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 |
[1]. Kirby RJ, et, al. Discovery of Novel Small-Molecule Inducers of Heme Oxygenase-1 That Protect Human iPSC-Derived Cardiomyocytes from Oxidative Stress. J Pharmacol Exp Ther. 2018 Jan;364(1):87-96.
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| Additional Infomation |
HIF-PHD-IN-3 (CAS 794582-71-1) is a potent hiPSC-CM cardioprotective scaffold that induces HO-1 upregulation. It has potential inhibitory effects on HIF-PHDs. It has a molecular formula of C16H13N3OS2 and a molecular weight of 327.42 g/mol. HIF-PHD-IN-3 is a valuable research tool for studying cardioprotection, hypoxia signaling, and anaemia.
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| Molecular Formula |
C16H13N3OS2
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| Exact Mass |
327.05
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| CAS # |
794582-71-1
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| PubChem CID |
2443231
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| Appearance |
White to off-white solid powder
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| LogP |
3.3
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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 |
5
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| Heavy Atom Count |
22
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| Complexity |
363
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C=C1)SCC(=O)NC2=NC(=CS2)C3=CC=CC=N3
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| InChi Key |
FEKFKURUDDXFPS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H13N3OS2/c20-15(11-21-12-6-2-1-3-7-12)19-16-18-14(10-22-16)13-8-4-5-9-17-13/h1-10H,11H2,(H,18,19,20)
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| Chemical Name |
2-phenylsulfanyl-N-(4-pyridin-2-yl-1,3-thiazol-2-yl)acetamide
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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.) |
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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