| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Amelparib hydrochloride targets poly(ADP-ribose) polymerase 1 (PARP-1), a nuclear enzyme involved in DNA repair, genomic stability, and cell death. PARP-1 is activated by DNA strand breaks and catalyzes the transfer of ADP-ribose units to target proteins. By inhibiting PARP-1 with an IC50 of 18.5 nM, Amelparib hydrochloride prevents PAR formation and reduces PARP-1-mediated cell death, which is relevant in the context of acute ischaemic stroke and other neurodegenerative conditions.
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| ln Vitro |
In vitro studies demonstrate that Amelparib hydrochloride is a potent inhibitor of PARP-1 with an IC50 of 18.5 nM. It inhibits cellular PAR formation with an IC50 of 10.7 nM. The compound is water-soluble and orally active. These properties make it a valuable tool for studying PARP-1-mediated pathways in cell-based systems. The compound has potential neuroprotective effects, making it relevant for research of acute ischaemic stroke.
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| ln Vivo |
In vivo activity of Amelparib hydrochloride has been investigated in the context of acute ischaemic stroke research. As an orally active PARP-1 inhibitor, it can be administered conveniently in animal models. Clinical trials have been conducted for the treatment of stroke and acute ischemic stroke. The compound's water solubility and oral bioavailability support its in vivo efficacy. Detailed in vivo data are available from clinical studies referenced in the literature.
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| Enzyme Assay |
The in vitro enzyme/receptor binding assay for Amelparib hydrochloride involves measuring its inhibitory activity against PARP-1 using purified recombinant enzyme. The assay typically uses PARP-1 incubated with the compound at varying concentrations, along with NAD+ and a DNA substrate to activate the enzyme. PARP-1 activity is measured by quantifying the incorporation of radiolabeled ADP-ribose into acceptor proteins. The IC50 value of 18.5 nM is determined from the inhibition curve. Cellular PAR formation is measured with an IC50 of 10.7 nM.
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| Cell Assay |
In vitro cell-based assays for Amelparib hydrochloride are conducted using various cell lines to evaluate PARP-1 inhibition. Cells are treated with the compound at various concentrations, and PAR formation is measured using immunofluorescence or ELISA-based detection. The IC50 for cellular PAR formation is 10.7 nM. Cytotoxicity is evaluated using standard cell viability assays. The compound's neuroprotective effects can be assessed in neuronal cell cultures exposed to oxidative stress or DNA damage.
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| Animal Protocol |
In vivo animal studies for Amelparib hydrochloride have been conducted in the context of acute ischaemic stroke research. Clinical trials have been performed with NCT numbers including NCT02396069 (Phase 1, Stroke, 2015), NCT03062397 (Phase 2, Acute Ischemic Stroke, 2016), and NCT01983358 (Phase 1, Stroke, 2013). These studies evaluate the compound's safety, tolerability, and efficacy in stroke patients. The compound is administered orally due to its oral activity.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Amelparib hydrochloride include water solubility and oral activity. The compound has a molecular weight of 379.88 g/mol and a molecular formula of C19H26ClN3O3. It appears as an off-white to light yellow solid. Solubility includes DMSO at 25 mg/mL (65.81 mM) with ultrasonic assistance. Storage recommendations include 4°C, sealed storage away from moisture, and in solvent at -80°C for 6 months or -20°C for 1 month.
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| Toxicity/Toxicokinetics |
Toxicity information for Amelparib hydrochloride is derived from clinical trial data. The compound has been evaluated in Phase 1 and Phase 2 clinical trials for safety and tolerability. Standard safety precautions for handling research chemicals should be followed. The compound is designated for research use only and is not for human therapeutic applications. No detailed toxicity data are available from the search results.
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| References |
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| Additional Infomation |
Amelparib hydrochloride (JPI-289 hydrochloride) is a potent, orally active, water-soluble PARP-1 inhibitor with IC50 of 18.5 nM for PARP-1 activity and 10.7 nM for cellular PAR formation. It is a potential neuroprotective agent for acute ischaemic stroke research. Clinical trials include NCT02396069, NCT03062397, and NCT01983358. It has MW 379.88 and formula C19H26ClN3O3. It is intended for research use only.
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| Molecular Formula |
C19H26CLN3O3
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| Molecular Weight |
379.88
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| Appearance |
Off-white to light yellow solid powder
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
Typically soluble in DMSO (e.g. 10 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 | 2.6324 mL | 13.1621 mL | 26.3241 mL | |
| 5 mM | 0.5265 mL | 2.6324 mL | 5.2648 mL | |
| 10 mM | 0.2632 mL | 1.3162 mL | 2.6324 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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