Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
---|
SKU | Size | Availability | Price | Qty |
---|---|---|---|---|
G646629-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $695.90 | |
G646629-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $1,250.90 | |
G646629-50mg | 50mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $3,750.90 |
Synonyms | 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)-1hbenzo(d)imidazole-6-carbonitrile | URCMKDJBULWNAI-DQEYMECFSA-N | GSK2798745 | GSK-2798745 | 1-(((5S,7S)-3-(5-(2-hydroxypropan-2-yl)pyrazin-2-yl)- |
---|---|
Specifications & Purity | ≥99% |
Biochemical and Physiological Mechanisms | GSK2798745 is a potent, selective, and orally active transient receptor potential vanilloid 4 ( TRPV4 ) ion channel blocker with IC 50 s of 1.8 and 1.6 nM for hTRPV4 and rTRPV4, respectively. GSK2798745 can be used in cardiac and respiratory diseases rese |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Product Description | GSK2798745 is a potent, selective, and orally active transient receptor potential vanilloid 4 ( TRPV4 ) ion channel blocker with IC 50 s of 1.8 and 1.6 nM for hTRPV4 and rTRPV4, respectively. GSK2798745 can be used in cardiac and respiratory diseases research In Vitro GSK2798745 inhibits TRPV4 agonist-induced impedance reduction in human umbilical vein endothelial cells (HUVECs). MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo GSK2798745 inhibits TRPV4 agonist-mediated lung edema in rats in a dose-dependent manner. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: TRPV4-mediated lung edema in male Sprague-Dawley ratsDosage: 0, 16, 50, or 150 ng/kg Administration: Intravenous injection; 0, 16, 50, or 150 ng/kg per minute; 60 min Result: Inhibited the formation of pulmonary edema, with complete inhibition seen at the highest dose tested where the basal lung wet weight to body weight ratio was held to control levels (LW/BW=4.21). Form:Solid IC50& Target:IC50: 1.8 nM (hTRPV4) and 1.6 nM (rTRPV4) |
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
---|
Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
---|
Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
---|
IUPAC Name | 3-[[(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]benzimidazole-5-carbonitrile |
---|---|
INCHI | 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 |
InChi Key | URCMKDJBULWNAI-DQEYMECFSA-N |
Canonical SMILES | CC1(CCCC2(C1)CN(C(=O)O2)C3=NC=C(N=C3)C(C)(C)O)CN4C=NC5=C4C=C(C=C5)C#N |
Isomeric 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 |
Alternate CAS | 1419609-94-1 |
PubChem CID | 71227359 |
MeSH Entry Terms | 3-(((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)benzimidazole-5-carbonitrile;GSK2798745 |
Molecular Weight | 460.53 |
Enter Lot Number to search for COA:
Solubility | DMSO : 250 mg/mL (542.85 mM; Need ultrasonic) |
---|