| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
The inositol 1,4,5-trisphosphate receptor (IP3R), a ligand-gated calcium channel located on the membrane of the endoplasmic reticulum.
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|---|---|
| ln Vitro |
In cell-free assays, IP3 binds to the IP3 receptor (IP3R) on microsomal membrane preparations (vesicles derived from the ER). This binding triggers the opening of the IP3R channel and the subsequent release of Ca2+. Binding affinity (Kd) is typically in the low nanomolar range (e.g., 10-50 nM).
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| ln Vivo |
A general in vitro activity of IP3 is to mobilize Ca2+ from intracellular stores in almost all cell types. Treatment of permeabilized cells or cells with the caged form of IP3 leads to a rapid and transient increase in cytoplasmic Ca2+ concentration.
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| Enzyme Assay |
A standard protocol to measure IP3 binding is to use a radioligand binding assay with [3H]-IP3. Microsomes (or membranes) prepared from rat cerebellum (a rich source of IP3Rs) are incubated with varying concentrations of [3H]-IP3 (0.5-50 nM) in a buffer (50 mM Tris-HCl, pH 8.3, 1 mM EDTA) at 4degC for 10 minutes. Non-specific binding is determined by adding 1 uM unlabeled IP3. The reaction is terminated by rapid filtration. The filters are washed, and bound radioactivity is counted. The Kd and Bmax are calculated from saturation binding curves. For competition assays, a fixed concentration of [3H]-IP3 (e.g., 5 nM) is incubated with increasing concentrations of unlabeled test compounds.
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| Cell Assay |
A standard protocol to measure IP3-mediated Ca2+ release uses permeabilized cells or cell homogenates loaded with a Ca2+ indicator. Cells (e.g., SH-SY5Y neuroblastoma) are harvested and permeabilized with digitonin (20 ug/mL) in an intracellular-like buffer (140 mM KCl, 10 mM NaCl, 2 mM MgCl2, 10 mM HEPES, pH 7.1, 1 mM ATP) to allow access of IP3 to the ER. The permeabilized cells are then incubated with a low concentration of Ca2+ (e.g., 100 nM) and the Ca2+ indicator Fluo-3 or Fura-2. The baseline fluorescence is recorded. The addition of D-myo-Inositol 1,4,5-trisphosphate (IP3) (e.g., 0.1-10 uM) triggers a rapid release of Ca2+ from the ER, leading to a sharp increase in fluorescence that decays as the Ca2+ is re-sequestered or diffuses away. The peak fluorescence increase is proportional to the IP3 concentration.
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| Animal Protocol |
A general in vivo protocol for studying the effects of this second messenger is challenging, as it is not permeable to intact cells. Therefore, in vivo experiments often utilize a "caged" form of IP3 (e.g., Ci-IP3/PM), which is membrane-permeable and can be injected into animals or loaded into cells. Upon a flash of UV light, the cage is removed, releasing active IP3. For example, in a study on mice, the caged compound can be microinjected into a specific brain region. A brief UV flash then releases IP3, which binds to its receptor, causing Ca2+ release and activating downstream processes, such as the activation of calcium-dependent potassium channels. This can be measured using behavioral tests (e.g., pain sensitivity) or electrophysiological recordings.
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| ADME/Pharmacokinetics |
Not applicable. As a second messenger, IP3 is not a drug with a classical PK profile. It is rapidly metabolized in the body by inositol polyphosphate 5-phosphatase and 3-kinase.
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| Toxicity/Toxicokinetics |
Not applicable. IP3 is an endogenous signaling molecule with a low molecular weight. While it has no general toxicity, its role in mobilizing calcium means that excessive or prolonged elevation could be cytotoxic, as calcium is a key mediator of apoptosis.
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| References |
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| Additional Infomation |
A general principle of its mechanism: In the phosphoinositide pathway, a stimulus activates a Gq-coupled receptor, which in turn activates phospholipase C (PLC). PLC hydrolyzes the membrane phospholipid, phosphatidylinositol 4,5-bisphosphate (PIP2), into two second messengers: diacylglycerol (DAG) and IP3. DAG remains in the membrane and activates protein kinase C (PKC), while IP3 diffuses into the cytoplasm to bind to its receptor on the ER. The molecular weight of the tripotassium salt is 534.37 g/mol. One common salt form is the potassium salt, which is highly soluble in water, making it easy to use in assays.
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| Molecular Formula |
C6H12K3O15P3
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|---|---|
| Molecular Weight |
534.37
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| Exact Mass |
533.83
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| CAS # |
141611-11-2
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| PubChem CID |
71299709
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| Appearance |
Solid powder
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
15
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
27
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| Complexity |
567
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| Defined Atom Stereocenter Count |
6
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| SMILES |
O([C@@H]1[C@H]([C@H](OP(O)(O)=O)[C@H](O)[C@H](O)[C@H]1OP(O)(O)=O)O)P(O)(O)=O.[KH]
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| InChi Key |
MQMSEISCCNPXIL-ZKVWPJASSA-K
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| InChi Code |
InChI=1S/C6H15O15P3.3K/c7-1-2(8)5(20-23(13,14)15)6(21-24(16,17)18)3(9)4(1)19-22(10,11)12;;;/h1-9H,(H2,10,11,12)(H2,13,14,15)(H2,16,17,18);;;/q;3*+1/p-3/t1-,2+,3+,4-,5-,6-;;;/m1.../s1
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| Chemical Name |
tripotassium;[(1R,2S,3R,4R,5S,6R)-2,3,5-trihydroxy-4,6-bis[[hydroxy(oxido)phosphoryl]oxy]cyclohexyl] hydrogen phosphate
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| Synonyms |
Inositol 1,4,5-trisphosphate tripotassium; Ins(1,4,5)-P3 tripotassium
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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) |
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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8714 mL | 9.3568 mL | 18.7136 mL | |
| 5 mM | 0.3743 mL | 1.8714 mL | 3.7427 mL | |
| 10 mM | 0.1871 mL | 0.9357 mL | 1.8714 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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