| Size | Price | Stock | Qty |
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| 1mg |
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| Targets |
Guanylyl imidodiphosphate targets G proteins, which are molecular switches that transduce signals from cell surface receptors to intracellular effectors. As a non-hydrolyzable GTP analog, it binds to the guanine nucleotide-binding site of G proteins and activates them irreversibly in the presence of Mg2+. Unlike GTP, which is hydrolyzed to GDP by the intrinsic GTPase activity of G proteins, guanylyl imidodiphosphate cannot be hydrolyzed, leading to persistent activation of G proteins and their downstream signaling pathways. This makes it a valuable tool for studying G protein-coupled receptor signaling, GTPase cycles, and enzyme activation pathways.
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| ln Vitro |
In vitro, guanylyl imidodiphosphate lithium is used to study G protein activation and signaling. It increases adenylate cyclase activity by activating Gs proteins. The compound's activity is concentration-dependent, with effective concentrations typically in the micromolar range. In cell-free systems, it is used to measure GTPase activity, nucleotide exchange, and G protein-effector interactions. It is also used in studies of protein synthesis, as GTP binding and release are essential for the initiation of protein translocation across the endoplasmic reticulum. Its non-hydrolyzable nature makes it an essential tool for dissecting G protein signaling pathways.
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| ln Vivo |
In vivo, guanylyl imidodiphosphate lithium is not used as a therapeutic agent but as a research tool in cell signaling studies. It is used in isolated membrane preparations or permeabilized cells to study G protein-mediated signaling. The compound's irreversible activation of G proteins makes it useful for studying the consequences of sustained G protein signaling. However, its in vivo applications are limited to ex vivo and in vitro studies due to its inability to cross cell membranes and its non-specific effects. The compound is for research use only.
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| Enzyme Assay |
The in vitro G protein activation assay for guanylyl imidodiphosphate lithium typically uses membranes from cells expressing G proteins or purified G protein subunits. The assay is performed by incubating membranes or purified proteins with varying concentrations of the test compound (typically 0.1 to 100 µM) in the presence of Mg2+ and [³⁵S]-GTPγS or other labeled nucleotides. The binding of the nucleotide analog is measured by filtration through glass fiber filters followed by liquid scintillation counting. For adenylate cyclase assays, membranes are incubated with the compound, and cAMP production is measured by ELISA or RIA. For GTPase assays, the hydrolysis of GTP is measured by the release of inorganic phosphate using a colorimetric assay. Positive controls (e.g., GTP, GTPγS) and negative controls (GDP, buffer) are included in each assay run.
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| Cell Assay |
For in vitro cellular assays, guanylyl imidodiphosphate lithium is typically used in cell-free systems or permeabilized cells. Cells are permeabilized using digitonin or streptolysin O to allow the compound to access intracellular G proteins. The compound is added at concentrations ranging from 1 to 100 µM, and G protein activation is assessed by measuring downstream signaling events such as cAMP production, calcium mobilization, or MAPK activation. For protein synthesis studies, the compound is used in translation assays to study the role of GTP in protein translocation. All experiments include appropriate controls (GTP, GDP) and are performed in triplicate.
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| Animal Protocol |
For in vivo studies, guanylyl imidodiphosphate lithium is not typically administered to animals due to its inability to cross cell membranes and its non-specific effects. The compound is used in ex vivo studies where tissues or cells are isolated and treated with the compound. In these studies, tissues are incubated with the compound, and G protein signaling is assessed. All animal procedures should be conducted in accordance with institutional guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of guanylyl imidodiphosphate lithium are not relevant, as it is a research reagent rather than a therapeutic agent. The compound has a molecular weight of 545.93 and is a polar nucleotide analog. It is not expected to cross cell membranes due to its charged nature. The compound is used in vitro and in ex vivo studies. Detailed PK data are not available.
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| Toxicity/Toxicokinetics |
The toxicology of guanylyl imidodiphosphate lithium is not relevant, as it is a research reagent used in vitro at low concentrations. The compound is not intended for human or animal consumption. Standard laboratory safety precautions should be followed when handling the compound. It is for research use only and is not approved for human therapeutic use.
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| References |
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| Additional Infomation |
Guanylyl imidodiphosphate lithium is a non-hydrolyzable GTP analog that irreversibly activates G proteins. It increases adenylate cyclase activity and is used in cell signaling research. The compound is not approved for human use and is intended for research purposes only. It is available as a high-purity research reagent for laboratory use.
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| Molecular Formula |
C10H13N6O13P3-4.4[LI+]
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|---|---|
| Molecular Weight |
545.92802
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| Exact Mass |
546.039
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| CAS # |
64564-03-0
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| PubChem CID |
136494784
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| Appearance |
White to off-white solid powder
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| LogP |
0.374
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
16
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
36
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| Complexity |
900
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| Defined Atom Stereocenter Count |
4
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| SMILES |
[Li+].[Li+].[Li+].[Li+].C1=NC2=C(N1[C@H]3[C@@H]([C@@H]([C@H](O3)COP(=O)([O-])OP(=O)(NP(=O)([O-])[O-])[O-])O)O)N=C(NC2=O)N
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| InChi Key |
NUKFMILQQVRELO-ZVQJTLEUSA-J
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| InChi Code |
InChI=1S/C10H17N6O13P3.4Li/c11-10-13-7-4(8(19)14-10)12-2-16(7)9-6(18)5(17)3(28-9)1-27-32(25,26)29-31(23,24)15-30(20,21)22;;;;/h2-3,5-6,9,17-18H,1H2,(H,25,26)(H3,11,13,14,19)(H4,15,20,21,22,23,24);;;;/q;4*+1/p-4/t3-,5-,6-,9-;;;;/m1..../s1
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| Chemical Name |
tetralithium;[[(2R,3S,4R,5R)-5-(2-amino-6-oxo-1H-purin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-oxidophosphoryl]oxy-(phosphonatoamino)phosphinate
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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 | 1.8317 mL | 9.1587 mL | 18.3174 mL | |
| 5 mM | 0.3663 mL | 1.8317 mL | 3.6635 mL | |
| 10 mM | 0.1832 mL | 0.9159 mL | 1.8317 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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