| Size | Price | Stock | Qty |
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GSK2798745 (GSK-2798745) is a novel, first-in-class and potent blocker of transient receptor potential vanilloid 4 (TRPV4) ion channel with the potential to be used for the treatment of pulmonary edema associated with congestive heart failure. It inhibits TRPV4 with IC50s of 1.8 and 1.6 nM for hTRPV4 and rTRPV4, respectively.
| ln Vitro |
Human umbilical vein endothelial cells' (HUVEC) TRPV4 agonist-induced decrease in impedance is inhibited by GSK2798745 [3].
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| ln Vivo |
In rats, TRPV4 agonist-mediated pulmonary edema is inhibited in a dose-dependent manner by GSK2798745 [3].
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| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat TRPV4-mediated pulmonary edema [3]
Doses: 0, 16, 50 or 150 ng/kg per minute 0, 16, 50 or 150 ng/kg per minute; 60 minutes Experimental Results: Inhibition of pulmonary edema Complete inhibition of edema formation was observed at the highest dose tested, where the ratio of basal lung wet weight to body weight remained at control levels (LW/BW=4.21). |
| References |
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| Additional Infomation |
GSK2798745 is under investigation in clinical trial NCT03372603 (A Study to Assess the Effectiveness and Side Effects of GSK2798745 in Participants With Chronic Cough).
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| Molecular Formula |
C₂₅H₂₈N₆O₃
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|---|---|
| Molecular Weight |
460.53
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| Exact Mass |
460.222
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| CAS # |
1419609-94-1
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| PubChem CID |
71227359
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
682.1±65.0 °C at 760 mmHg
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| Flash Point |
366.3±34.3 °C
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| Vapour Pressure |
0.0±2.2 mmHg at 25°C
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| Index of Refraction |
1.680
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| LogP |
1.76
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
34
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| Complexity |
844
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C[C@@]1(CCC[C@]2(C1)CN(C(=O)O2)C3=NC=C(N=C3)C(C)(C)O)CN4C=NC5=C4C=C(C=C5)C#N
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| InChi Key |
URCMKDJBULWNAI-DQEYMECFSA-N
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| InChi Code |
InChI=1S/C25H28N6O3/c1-23(2,33)20-11-28-21(12-27-20)31-15-25(34-22(31)32)8-4-7-24(3,13-25)14-30-16-29-18-6-5-17(10-26)9-19(18)30/h5-6,9,11-12,16,33H,4,7-8,13-15H2,1-3H3/t24-,25-/m0/s1
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| Chemical Name |
1-(((5S,7S)-3-(5-(2-Hydroxypropan-2-yl)pyrazin-2-yl)-7-methyl-2-oxo-1-oxa-3-azaspiro[4.5]decan-7-yl)methyl)-1H-benzo[d]imidazole-6-carbonitrile
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| Synonyms |
GSK-2798745 GSK2798745 GSK 2798745
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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) |
DMSO : ~250 mg/mL (~542.85 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.52 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.52 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.52 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1714 mL | 10.8571 mL | 21.7141 mL | |
| 5 mM | 0.4343 mL | 2.1714 mL | 4.3428 mL | |
| 10 mM | 0.2171 mL | 1.0857 mL | 2.1714 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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