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| Targets |
Teprasiran targets p53, a key transcription factor and tumor suppressor that plays a central role in regulating apoptosis. By inhibiting p53-mediated cell death, Teprasiran aims to protect cells from injury in conditions such as acute kidney injury. The siRNA mechanism involves binding to p53 mRNA and promoting its degradation, thereby reducing p53 protein levels.
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| ln Vitro |
Teprasiran is a small interfering RNA (siRNA) that is synthetic and chemically stabilized. It works through RNA interference to temporarily block the production of p53, with a half-life of 48 to 72 hours[1].
In vitro, Teprasiran acts through RNA interference to temporarily inhibit p53 expression. The siRNA is designed to specifically target p53 mRNA, leading to its degradation and a reduction in p53 protein levels. This results in the temporary inhibition of p53-mediated cell death, which is the underlying mechanism for its potential therapeutic effect in acute kidney injury. |
| ln Vivo |
In vivo, Teprasiran has been evaluated in clinical trials for acute kidney injury and delayed graft function. In animal models, it is expected to reduce p53 expression in the kidney and protect against ischemic injury. The siRNA is administered via injection and is designed to be taken up by kidney cells. These studies have provided proof-of-concept for its therapeutic potential.
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| Enzyme Assay |
Specific in vitro enzyme/receptor binding assay protocols are not applicable for Teprasiran, as it is an siRNA. Its mechanism of action involves RNA interference and does not involve direct binding to enzymes or receptors. Instead, its activity is assessed by measuring p53 mRNA and protein levels in cells treated with the siRNA. Standard molecular biology techniques such as qPCR and Western blotting are used.
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| Cell Assay |
Cellular assays for Teprasiran are performed using kidney cell lines. Cells are treated with the siRNA, and p53 expression is measured at the mRNA and protein levels. The siRNA's ability to inhibit p53-mediated apoptosis is assessed by subjecting cells to stress conditions and measuring cell death. These assays confirm the siRNA's potency and specificity.
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| Animal Protocol |
In vivo animal protocols for Teprasiran involve administration of the siRNA to animal models of acute kidney injury. The siRNA is typically administered via intravenous injection. Kidney function is monitored by measuring serum creatinine and blood urea nitrogen (BUN) levels. p53 expression in kidney tissue is assessed, and the extent of kidney injury is evaluated histologically.
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| ADME/Pharmacokinetics |
Teprasiran is a synthetic, chemically stabilized small interfering RNA (siRNA). Its pharmacokinetic properties are typical of siRNA therapeutics, which have a short half-life in circulation and are primarily cleared by the kidneys. It is administered via injection, and its distribution is mainly to the liver and kidneys. The siRNA is designed for local delivery to the kidney.
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| Toxicity/Toxicokinetics |
Toxicity data for Teprasiran have been evaluated in clinical trials. As an siRNA, its toxicity is primarily related to off-target effects and immune stimulation. The compound has been shown to be generally well-tolerated in clinical studies. However, comprehensive toxicological data are not detailed in the available literature. It is intended for research use only.
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| References | |
| Additional Infomation |
Teprasiran (QPI-1002) is a p53-targeting siRNA that has been investigated in clinical trials for acute kidney injury (AKI) and delayed graft function (DGF). Phase 2 and Phase 3 clinical trials have been conducted. The compound is not currently approved for clinical use and is intended for research purposes.
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| CAS # |
1231737-88-4
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| Appearance |
White to off-white 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) |
H2O : ≥ 20 mg/mL (1.62 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.) |
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.
Products are for research use only; We do not sell to patients
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