| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Guanosine 5'-O-(2-thiobisphosphate) (1 µM) can block norepinephrine-induced nitric oxide release in adult rat ventricular myocytes [1]. Guanosine 5'-O-(2-thiobisphosphate) can act as a partial agonist for the activation of adenylate cyclase in the synaptic membrane of the rat cerebral cortex, with an EC50 of 4 × 10⁻⁷ M and a maximum activation level equivalent to 60% of that of GTP triphosphate analogs [2]. Guanosine 5'-O-(2-thiobisphosphate) (1 μM) can enhance the activation of adenylate cyclase mediated by low-dose GTPγS (7) while inhibiting the activation induced by high-dose GTPγS in the synaptic membrane of the rat cerebral cortex [2]. Guanosine 5'-O-(2-thiobisphosphate) promotes the exchange of some nucleotides from Gi/o to Gs (EC50 = 2×10-5 M) and partially reverses the inhibition of adenylate cyclase (EC50 = 5×10-6 M). Its efficacy and effectiveness in the synaptic membrane of the rat cerebral cortex are lower than those of GppNHp[2]. Guanosine 5'-O-(2-thiobisphosphate) competitively inhibits the activity of GTP-stimulated adenylate cyclase in the plasma membrane of the pancreas of rats pretreated with cholera toxin, with Ki ranging from 0.3 to 0.6 μM[3]. Guanosine 5'-O-(2-thiobisphosphate) inhibits the activity of adenylate cyclase stimulated by cholecystokinin-8 (CCK-8) in the plasma membrane of the pancreas of native rats; in the presence of 0.3 μM GTP, its I50 is 2.2 μM and Ki is 0.5 μM[3]. Guanosine 5'-O-(2-thiobisphosphate) inhibited secretin + GTP-stimulated adenylate cyclase activity in the plasma membrane of natural rat pancreas, with an IC50 of 8 μM and a Ki of 3.2 μM [3].
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| References |
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| Molecular Formula |
C10H12N5NA3O10P2S
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|---|---|
| Molecular Weight |
525.21
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| Appearance |
Colorless to light yellow liquid
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| SMILES |
NC1=NC(C2=C(N1)N(C=N2)[C@@H]3O[C@H](COP(OP(O[Na])(S[Na])=O)(O[Na])=O)[C@@H](O)[C@H]3O)=O
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| Synonyms |
GDPβS trisodium
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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 | 1.9040 mL | 9.5200 mL | 19.0400 mL | |
| 5 mM | 0.3808 mL | 1.9040 mL | 3.8080 mL | |
| 10 mM | 0.1904 mL | 0.9520 mL | 1.9040 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.