| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Tertiapin-Q targets G protein-coupled inwardly rectifying potassium (GIRK) channels, specifically the GIRK1/4 heterodimer, and the renal outer medullary potassium channel (ROMK1, Kir1.1). It also inhibits BK-type K+ channels in a concentration-dependent manner. By blocking these potassium channels, Tertiapin-Q modulates potassium ion flux and cellular excitability.
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| ln Vitro |
Tertiapin-Q is a highly specific blocker of the renal extramedullary potassium channel (ROMK1, Kir1.1) and inward rectifier potassium (GIRK1/4) heterodimer that is related to G proteins [1]. Large conductance potassium channels (also known as calcium-activated potassium channels) and Kir3.1-Kir3.4 renal extramedullary potassium channels are all strongly and selectively blocked by tertiapin-Q. Nearly all of the somatostatin (SS-14)-activated current was inhibited (93.2±2.9%, n=5 ;P<0.01). Q)[2].
In vitro, Tertiapin-Q is a highly selective blocker of GIRK1/4 heterodimer and ROMK1 (Kir1.1) channels. It binds to ROMK1 with a Ki of 1.3 nM and to GIRK1/4 with a Ki of 13.3 nM. The compound shows selectivity over Kir2.1 channels. It inhibits BK-type K+ channels in a concentration-dependent manner. |
| ln Vivo |
Tertiapin-Q functions as an IK,Ach K+ current (muscarinic acetylcholine receptor) blocker. The atrial effective refractory period (AERP) of six rapidly atrial paced (RAP) rabbits remained constant throughout the experiment when the rapid atrial pacing was stopped. Effect of ranolazine (10 mg/kg, n = 6 per group) or Tertiapin-Q (0.03 mg/kg, n = 5 per group) on AERP in control and RAP rabbits. Bephidil (1 mg/kg, n = 5 in each group), amiodarone (10 mg/kg, n = 5 in each group), vernakalan (3 mg/kg, n = 5 in each group). The duration of each pacing cycle was markedly extended by tertiapin-Q in both control and RAP rabbits. In comparison to control animals, RAP rabbits have a higher prolonging effect of Tertiapin-Q on AERP [3].
In vivo activity data for Tertiapin-Q are limited, as the compound is primarily used as a research tool for in vitro electrophysiological studies. By blocking GIRK and ROMK channels, Tertiapin-Q modulates potassium currents that are involved in various physiological processes including cardiac and neuronal excitability. Further in vivo studies are needed to characterize its effects. |
| Enzyme Assay |
In vitro receptor/channel binding assays for Tertiapin-Q are performed using membrane preparations or whole-cell patch-clamp electrophysiology. The compound's affinity for potassium channels is determined by measuring its ability to displace radiolabeled ligands or by measuring the reduction in potassium currents. Ki values of 1.3 nM (ROMK1) and 13.3 nM (GIRK1/4) have been reported.
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| Cell Assay |
In vitro cellular assays for Tertiapin-Q are performed using cells expressing potassium channels. Patch-clamp electrophysiology is used to measure potassium currents in the presence of the compound. The reduction in current amplitude is quantified to determine the compound's inhibitory potency and selectivity. These assays provide functional evidence of potassium channel blockade.
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| Animal Protocol |
In vivo animal experimental protocols for Tertiapin-Q are not extensively documented in the available literature. As a research peptide, in vivo studies would typically involve administration to animal models to study the role of GIRK and ROMK channels in various physiological processes. The compound would be administered via appropriate routes.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Tertiapin-Q have not been systematically characterized. The peptide has a molecular weight of 2452 and molecular formula C106H175N35O24S4. It is soluble in water at 50 mg/mL and at 2 mg/mL. The compound should be stored as a powder at -20°C for up to 3 years. Further PK studies are needed.
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| Toxicity/Toxicokinetics |
Toxicological data for Tertiapin-Q are not extensively reported. As a research-use peptide derived from bee venom toxin, its safety profile has not been formally evaluated. The compound is intended for research purposes only. Standard laboratory safety precautions should be followed when handling this peptide.
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| References |
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| Additional Infomation |
Tertiapin-Q (TPNQ) is a synthetic peptide derivative of bee venom toxin tertiapin with CAS number 910044-56-3, molecular formula C106H175N35O24S4, and molecular weight 2452. It is a high-affinity blocker of ROMK1 (Kir1.1) and GIRK1/4 (Kir3.1/3.4) channels with Ki values of 1.3 nM and 13.3 nM, respectively. This product is for research use only.
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| Molecular Formula |
C106H175N35O24S4
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|---|---|
| Molecular Weight |
2452.00381588936
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| Exact Mass |
2450.243
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| CAS # |
910044-56-3
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| PubChem CID |
90479782
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.693
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| LogP |
-9.12
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| Hydrogen Bond Donor Count |
33
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| Hydrogen Bond Acceptor Count |
35
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| Rotatable Bond Count |
51
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| Heavy Atom Count |
169
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| Complexity |
5230
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| Defined Atom Stereocenter Count |
23
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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 : ~50 mg/mL (~20.39 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 | 0.4078 mL | 2.0392 mL | 4.0783 mL | |
| 5 mM | 0.0816 mL | 0.4078 mL | 0.8157 mL | |
| 10 mM | 0.0408 mL | 0.2039 mL | 0.4078 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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