| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
G proteins (heterotrimeric Gα subunits) and adenylate cyclase. The compound binds to Gα subunits and locks them in an active, GTP-bound-like conformation that cannot be hydrolyzed, leading to persistent activation of downstream effectors such as adenylate cyclase.
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|---|---|
| ln Vitro |
In response to calcium stimulation, permeabilized platelets release dense granules when exposed to guanosyl imine trisodium diphosphate (GppNHp) at concentrations of 100 μM. GTP-Ral increases the calcium sensitivity of this process, which is inhibited by Sec5-RBD[1]. Adenylyl cyclase activity can be stimulated with a substantially shorter lag time when using gamma-trisodium diphosphate (GppNHp) (0.017-333 μM) [3].
The compound itself is not an inhibitor; its “activity” is as a non-hydrolyzable GTP analog. It activates G proteins and stimulates adenylate cyclase in membrane preparations, and it is used at concentrations of 10–100 µM to probe G-protein–coupled signaling in vitro. |
| ln Vivo |
In vivo data are limited; the compound is primarily used in cell-free and permeabilized cell systems. Because it is highly charged and membrane-impermeant, systemic administration is not a standard application.
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| Enzyme Assay |
For cell-free G-protein activation, incubate membrane fractions or purified G proteins with 10–100 µM Gpp(NH)p and 1–10 mM MgCl₂ in a suitable buffer (e.g., 50 mM Tris-HCl, pH 7.5) at 30°C for 30–60 min. Measure downstream adenylate cyclase activity or GTPase activity as the readout. Include GTP as a positive control and GDPβS as a negative control.
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| Cell Assay |
For permeabilized cell assays, permeabilize cells (e.g., with digitonin or saponin) and incubate with 10–100 µM Gpp(NH)p in the presence of Mg²⁺. Measure cAMP accumulation or downstream reporter activation. Include vehicle-treated and GTPγS-treated controls.
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| Animal Protocol |
No standard in vivo protocol exists for systemic administration. For local delivery, microinject or perfuse 10–100 µM Gpp(NH)p in physiological buffer into the target tissue or brain region. Include vehicle-injected controls and, where possible, co-apply a G-protein inhibitor to confirm specificity.
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| References |
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| Additional Infomation |
non-hydrolyzable GTP analog in which the oxygen atom linking the β-phosphate and γ-phosphate is replaced by a nitrogen atom. It binds tightly to G proteins in the presence of Mg2+. This nucleotide is a potent activator of adenylate cyclase.
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| Molecular Formula |
C10H14N6O13P3-3.3[NA+]
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|---|---|
| Molecular Weight |
588.14136
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| Exact Mass |
587.952
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| CAS # |
148892-91-5
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| Related CAS # |
Guanylyl imidodiphosphate lithium; 64564-03-0
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| PubChem CID |
135445723
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| Appearance |
White to off-white solid
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| Melting Point |
230 °C
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
16
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
35
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| Complexity |
909
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C([C@@H]1[C@H]([C@H]([C@H](N2C=NC3=C2NC(=N)N=C3[O-])O1)O)O)OP(=O)(O)OP(=O)(NP(=O)([O-])[O-])O.[Na+].[Na+].[Na+]
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| InChi Key |
QGJNRMUNXAROIT-CYCLDIHTSA-K
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| InChi Code |
InChI=1S/C10H17N6O13P3.3Na/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;3*+1/p-3/t3-,5-,6-,9-;;;/m1.../s1
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| Chemical Name |
trisodium;[[(2R,3S,4R,5R)-5-(2-amino-6-oxo-1H-purin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-oxidophosphoryl]oxy-[[hydroxy(oxido)phosphoryl]amino]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 (e.g. under nitrogen), 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: ~1 mg/mL (~1.7 mM; with ultrasonication and warming by heating to 60°C)
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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 | 1.7003 mL | 8.5014 mL | 17.0028 mL | |
| 5 mM | 0.3401 mL | 1.7003 mL | 3.4006 mL | |
| 10 mM | 0.1700 mL | 0.8501 mL | 1.7003 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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