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| ln Vitro |
In inside-out patch membrane configurations from rabbit portal vein smooth muscle cells, bath application of GDP (≥ 100 µM) re-activated the pinacidil-sensitive 15 pS ATP-sensitive K⁺ channel that had undergone “run-down” after membrane excision. This effect required the presence of pinacidil (100 µM) either in the pipette or bath.
GDP (1 mM) increased the mean open time and open probability (channel activity) of the 15 pS K⁺ channel more potently than GTP (1 mM). The channel activity induced by 1 mM-GDP was about three times greater than that induced by 1 mM-GTP. The activation by GDP was concentration-dependent (effective concentrations ≥ 30 µM). It increased the mean open time of the channel (e.g., from 369 ms at 100 µM to 1171 ms at 1 mM) without changing the number of channel openings. Other guanine nucleotides (GMP, GTPγS, GDPβS at 1 mM) failed to activate the channel. However, GDPβS (1 mM) inhibited the channel when it was pre-activated by 1 mM-GDP. The activation by GDP did not require the simultaneous presence of Mg²⁺. GDP (1 mM) had no effect on the large-conductance Ca²⁺-dependent K⁺ channel (150 pS) present in the same cells.[1] |
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| Cell Assay |
Single-channel recordings were performed on enzymatically dispersed smooth muscle cells from rabbit portal vein. The patch-clamp technique (cell-attached, inside-out, and outside-out configurations) was used. Cells were placed in a recording chamber on an inverted microscope stage. Patch electrodes (5-10 MΩ resistance) were used to form high-resistance seals (>10 GΩ) on the cell membrane. The bath was perfused with a high-K⁺ solution (140 mM KCl, 0.3 mM EGTA, 5 mM HEPES, pH 7.25) to set the membrane potential and provide a K⁺ gradient. The pipette solution was physiological salt solution (PSS: 134 mM NaCl, 6 mM KCl, 2.5 mM CaCl₂, 12 mM glucose, 5 mM HEPES, pH 7.25) containing pinacidil (100 µM) and charybdotoxin (100 nM) to inhibit the large-conductance K⁺ channel. After obtaining a cell-attached patch, the membrane was excised to form an inside-out configuration. Test compounds, including GDP (dissolved in cold deionized water), were applied to the bath (cytosolic side). Single-channel currents were recorded using a patch-clamp amplifier, filtered at 300 Hz or 1 kHz, digitized, and analyzed using specialized software. Channel activity (NP₀) was calculated from all-point amplitude histograms.[1]
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| References |
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| Additional Infomation |
GDP is a purine ribonucleoside 5'-bisphosphate, formed by the condensation of the 5'-hydroxyl group of guanosine with pyrophosphate. It is a metabolite of both E. coli and mice, and also an inhibitor of uncoupling proteins. It is both guanosine 5'-phosphate and purine ribonucleoside 5'-bisphosphate. It is the conjugate acid of GDP(2-). Guanosine diphosphate is a metabolite present in or produced by E. coli (K12 strain, MG1655 strain). It has been reported to exist in Arabidopsis thaliana, humans, and other organisms with relevant data. Guanosine diphosphate is a purine ribonucleoside diphosphate formed by the binding of a guanine and a pyrophosphate group to a ribose group at their 1' and 5' sites, respectively. Guanosine diphosphate (GDP) is an inactive metabolite and an intermediate in the synthesis of guanosine triphosphate (GTP). Guanosine diphosphate is a metabolite found or produced in Saccharomyces cerevisiae.
It is a guanine nucleotide with its glycosyl moiety esterified with two phosphate groups. See also: ... See more ... Guanine 5'-bisphosphate (GDP) is considered an essential endogenous factor for regulating ATP-sensitive K⁺ channels in rabbit portal vein smooth muscle. This channel (15 pS) can be activated by K⁺ channel openers such as pinafenidil and blocked by glibenclamide, but is insensitive to cytoplasmic Ca²⁺. Channel activity rapidly disappears (“decreases”) after membrane excision or permeabilization with saponins. In the presence of pinafenidil, GDP (but not ATP) can reactivate this degraded channel. Its bisphosphate structure is crucial to its activity because GMP and GTPγS are ineffective. ATP inhibits this GDP-activated channel with an IC₅₀ value of 29 µM, while Mg²⁺ attenuates this inhibition. [1] |
| Molecular Formula |
C10H12N5O11P2-3
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|---|---|
| Molecular Weight |
440.17678
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| Exact Mass |
443.024
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| CAS # |
146-91-8
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| Related CAS # |
Guanosine 5'-diphosphate disodium salt;7415-69-2;Guanosine 5'-diphosphate sodium;43139-22-6
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| PubChem CID |
135398619
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| Appearance |
Typically exists as solid at room temperature
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| Density |
2.63 g/cm3
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| Boiling Point |
961ºC at 760 mmHg
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| Flash Point |
535ºC
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| Vapour Pressure |
0mmHg at 25°C
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| Index of Refraction |
1.94
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| LogP |
-4.6
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
28
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| Complexity |
760
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| Defined Atom Stereocenter Count |
4
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| SMILES |
O[C@@H]([C@H]([C@H](N1C=NC2=C1N=C(N)NC2=O)O3)O)[C@H]3COP(O)(OP(O)(O)=O)=O
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| InChi Key |
QGWNDRXFNXRZMB-UUOKFMHZSA-N
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| InChi Code |
InChI=1S/C10H15N5O11P2/c11-10-13-7-4(8(18)14-10)12-2-15(7)9-6(17)5(16)3(25-9)1-24-28(22,23)26-27(19,20)21/h2-3,5-6,9,16-17H,1H2,(H,22,23)(H2,19,20,21)(H3,11,13,14,18)/t3-,5-,6-,9-/m1/s1
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| Chemical Name |
[(2R,3S,4R,5R)-5-(2-amino-6-oxo-1H-purin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl phosphono hydrogen phosphate
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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 |
| 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 | 2.2718 mL | 11.3590 mL | 22.7180 mL | |
| 5 mM | 0.4544 mL | 2.2718 mL | 4.5436 mL | |
| 10 mM | 0.2272 mL | 1.1359 mL | 2.2718 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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