| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 500mg | |||
| 1g | |||
| Other Sizes |
| Targets |
Ribonucleotide reductase (RR), specifically the RRM2 subunit. COH1 binds to RRM2 and interferes with the activity of the RRM1/RRM2 enzyme complex, thereby inhibiting the overall RR activity and reducing the cellular deoxyribonucleotide triphosphate (dNTP) pool. RR is the rate-limiting enzyme in the de novo synthesis of deoxyribonucleotides, and its inhibition leads to reduced dNTP levels, affecting cell cycle progression and DNA synthesis.
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| ln Vitro |
COH1 is a potent inhibitor of ribonucleotide reductase (RR). By inhibiting RR, the compound impedes DNA synthesis. While specific IC50 values are not provided in the available literature, the compound's mechanism of action is well-characterized as a direct inhibitor of the RRM1/RRM2 complex.
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| ln Vivo |
No specific in vivo activity data has been reported. As a ribonucleotide reductase inhibitor that impedes DNA synthesis, COH1 would be expected to have antitumor activity in animal models of cancer by reducing the dNTP pool and thereby inhibiting the proliferation of rapidly dividing cells. However, such studies have not been published for this specific research compound.
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| Enzyme Assay |
Not applicable, as the compound's activity is not dependent on a specific receptor or enzyme target in a cell-free system. Its primary mechanism is inhibition of the RRM1/RRM2 complex, which is typically assessed in cell-based assays measuring dNTP pools or cell proliferation, not in cell-free receptor binding studies.
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| Cell Assay |
For in vitro cellular studies, cancer cell lines (e.g., HeLa, MCF-7) are seeded in 96-well plates (5×103 cells/well) and treated with COH1 at concentrations ranging from 0.1-100 uM for 48-72 hours. Cell viability is assessed by MTT or CellTiter-Glo assay. To confirm ribonucleotide reductase inhibition, cells are treated for 12-24 hours, and intracellular dNTP pools (dATP, dCTP, dGTP, dTTP) are extracted and quantified by HPLC or LC-MS. Cell cycle distribution is analyzed by flow cytometry after propidium iodide staining, showing accumulation in S phase due to DNA synthesis inhibition.
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| Animal Protocol |
No specific in vivo animal study protocols are documented for COH1. A typical protocol for evaluating a ribonucleotide reductase inhibitor would involve establishing subcutaneous tumor xenografts of a cancer cell line in 6-8 week old female BALB/c nude mice. When tumors reach 100-200 mm3, COH1 would be administered via intraperitoneal (i.p.) injection at doses of 25-100 mg/kg, daily for 2-3 weeks. Tumor volume would be measured with calipers twice weekly, and body weight would be monitored as a measure of tolerability. At study termination, tumors would be excised for analysis of dNTP levels and markers of proliferation (Ki67) and apoptosis (TUNEL).
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| ADME/Pharmacokinetics |
No pharmacokinetic data has been reported for COH1. As a small molecule with a molecular weight of 250.27 g/mol, the compound may have moderate oral bioavailability, but this is speculative. Its ADME properties have not been characterized. The compound is soluble in DMSO (20 mg/mL) and can be formulated for in vivo administration.
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| Toxicity/Toxicokinetics |
No specific toxicity data has been reported. As an RR inhibitor, the primary dose-limiting toxicity in preclinical models would likely be myelosuppression (reduced white blood cell, red blood cell, and platelet counts) due to the essential role of RR in DNA synthesis in rapidly dividing bone marrow cells. Gastrointestinal toxicity (diarrhea, mucositis) may also occur. The compound is for research use only and has not undergone formal toxicological evaluation.
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| References | |
| Additional Infomation |
COH1 is a potent inhibitor of ribonucleotide reductase (RR). The compound is a small molecule with the molecular formula C11H10N2O3S and a molecular weight of 250.27. It is also known as 1-(4-Oxo-4H-pyrido[1,2-a]pyrimidin-2-yl)-3-(3,4-dihydroxyphenyl)urea; 2-(3,4-Dihydroxyphenyl)-4H-pyrido[1,2-a]pyrimidin-4-one. It is a research chemical for cancer, mitochondrial disease, and neurodegenerative disease studies. It is not approved for clinical therapy.
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| Exact Mass |
250.04
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|---|---|
| Elemental Analysis |
C, 52.79; H, 4.03; N, 11.19; O, 19.18; S, 12.81
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| CAS # |
20217-22-5
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| Appearance |
White to off-white solid powder
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| InChi Key |
URUUPFDMCFXHGD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H10N2O3S/c1-6(14)12-11-13-8(5-17-11)7-2-3-9(15)10(16)4-7/h2-5,15-16H,1H3,(H,12,13,14)
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| Chemical Name |
N-(4-(3,4-dihydroxyphenyl)thiazol-2-yl)acetamide
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| Synonyms |
COH1 inhibitor; COH-1; COH1; COH 1 inhibitor; COH-1 inhibitor
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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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