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| SKU | Size | Availability |
Price | Qty |
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E409159-1ml
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1ml |
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
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$196.90
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SGLT2 Selective Inhibitors
| Synonyms | D-Glucitol, 1,5-anhydro-1-C-[4-chloro-3-[[4-[[(3S)-tetrahydro-3-furanyl]oxy]phenyl]methyl]phenyl]-, (1S)- |
|---|---|
| Specifications & Purity | Moligand™, 10mM in DMSO |
| Biochemical and Physiological Mechanisms | Empagliflozin (BI-10773) is a potent and selective SGLT-2 inhibitor with IC50 of 3.1 nM, exhibits >300-fold selectivity over SGLT-1, 4, 5 and 6. Phase 3. |
| Storage Temp | Store at -80°C |
| Shipped In |
Ice chest + Ice pads This product requires cold chain shipping. Ground and other economy services are not available. |
| Grade | Moligand™ |
| Action Type | INHIBITOR |
| Mechanism of action | Sodium/glucose cotransporter 2 inhibitor |
| Product Description |
Information Empagliflozin (BI-10773) is a potent and selectiveSGLT-2inhibitor withIC50of 3.1 nM, exhibits >300-fold selectivity over SGLT-1, 4, 5 and 6. Phase 3. Empagliflozin shows >2500-fold selectivity for hSGLT-2 over hSGLT-1 (IC50 8300 nM) and >3500-fold selectivity over hSGLT-4, it exhibits >350-fold selectivity over hSGLT-5 (IC50=1100 nM) and >600-fold selectivity over hSGLT-6. No relevant inhibition of GLUT1 is observed up to 10 μM Empagliflozin. In a kinetic binding experiments, [3H]-empagliflozin displays a high affinity for SGLT-2 with a mean Kd of 57 nM in the absence of glucose, and shows a half-life of [3H]-empagliflozin-binding to SGLT-2 of 59 min in the absence of glucose.Its binding to SGLT-2 is competitive with glucose. In vivo
cell lines: Concentrations:~ 500 nM Incubation Time:72 h Powder Purity:≥99% |
| ALogP | 1.839 |
|---|---|
| hba_count | 3 |
| HBD Count | 4 |
| Rotatable Bond | 6 |
| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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| Smiles | OCC1OC(C(O)C(O)C1O)C2=CC(=C(Cl)C=C2)CC3=CC=C(OC4CCOC4)C=C3 |
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| Molecular Weight | 450.91 |
| Reaxy-Rn | 31635249 |
| Reaxys-RN_link_address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=31635249&ln= |
| Solubility | Solubility (25°C) In vitro DMSO: 30 mg/mL (199.82 mM); Water: 30 mg/mL (199.82 mM); Ethanol: Insoluble; |
|---|---|
| DMSO(mg / mL) Max Solubility | 90 |
| DMSO(mM) Max Solubility | 199.6 |
| Water(mg / mL) Max Solubility | <1 |