| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
The primary target of TM6089 is Prolyl Hydroxylase (PHD). It acts as a unique inhibitor, stimulating HIF activity without iron chelation. By inhibiting PHD, TM6089 stabilizes HIF, leading to the induction of angiogenesis and protection against ischemia.
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| ln Vitro |
In vitro, TM6089 is a PHD inhibitor that stimulates HIF activity without iron chelation. It induces angiogenesis and protects against ischemia in various cell types. The compound's activity has been confirmed in various in vitro models.
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| ln Vivo |
In vivo, TM6089 enhances angiogenesis when administered topically and stimulates activity when administered orally in transgenic rats expressing a reporter vector for the hypoxia response. It exerts organ protection against ischemia.
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| Enzyme Assay |
In vitro enzyme or receptor binding assays for TM6089 involve measuring its inhibition of PHD activity. The assay uses a purified PHD enzyme and a substrate, such as HIF peptide. The hydroxylation of the substrate is measured using a radioactive or mass spectrometry method. The compound is incubated with the enzyme and substrate at varying concentrations to determine the IC50.
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| Cell Assay |
In vitro cell-based assays for TM6089 are performed using various cell lines. Cells are treated with the compound, and HIF stabilization and target gene expression are assessed by Western blotting and qPCR. The compound's effects on angiogenesis and cell survival are evaluated.
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| Animal Protocol |
In vivo animal experiments for TM6089 are conducted using transgenic rats expressing a reporter vector for the hypoxia response. The compound is administered topically or orally, and angiogenesis and HIF activity are assessed. The compound's protective effects against ischemia are evaluated.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of TM6089 indicate that it has a molecular weight of 306.34 and a molecular formula of C13H14N4O3S. The CAS number is 863421-32-3. The IUPAC name is 6-Amino-1,3-dimethyl-5-(2-pyridin-2-ylsulfanylacetyl)pyrimidine-2,4-dione. The compound is soluble in DMSO.
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| Toxicity/Toxicokinetics |
Toxicology (toxicology) data for TM6089 are characteristic of a research compound. As a PHD inhibitor, its safety profile is an important consideration. The compound is generally well-tolerated at effective doses in preclinical models. However, its long-term safety profile requires further evaluation.
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| References | |
| Additional Infomation |
Other information: TM6089 is a unique PHD inhibitor that stimulates HIF activity without iron chelation. It induces angiogenesis and exerts organ protection against ischemia. The compound is used in research to study hypoxia signaling and angiogenesis. Its CAS number is 863421-32-3.
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| Molecular Formula |
C13H14N4O3S
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|---|---|
| Molecular Weight |
306.340260982513
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| Exact Mass |
306.078
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| CAS # |
863421-32-3
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| PubChem CID |
2352701
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| Appearance |
Light yellow to light brown solid powder
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| LogP |
0.9
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
21
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| Complexity |
506
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C1C=CC=CN=1)CC(C1C(N(C)C(N(C)C=1N)=O)=O)=O
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| InChi Key |
UWXHGWIWBWQJNU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H14N4O3S/c1-16-11(14)10(12(19)17(2)13(16)20)8(18)7-21-9-5-3-4-6-15-9/h3-6H,7,14H2,1-2H3
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| Chemical Name |
6-amino-1,3-dimethyl-5-(2-pyridin-2-ylsulfanylacetyl)pyrimidine-2,4-dione
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| Synonyms |
TM 6089; TM-6089; TM6089
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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 : ~41.67 mg/mL (~136.03 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 | 3.2643 mL | 16.3217 mL | 32.6435 mL | |
| 5 mM | 0.6529 mL | 3.2643 mL | 6.5287 mL | |
| 10 mM | 0.3264 mL | 1.6322 mL | 3.2643 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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