Empagliflozin (BI 10773) 864070-44-0
Product Description
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Molecular Weight:
450.91 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.
Biological Activity
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.
High exposure of empagliflozin is achieved in dogs, with plasma
concentrations >100-fold above IC50 measured 24 h after
administration of 5 mg/kg empagliflozin. The total plasma clearance of
empagliflozin in ZDF rat is 43 mL/min/kg, while in dogs is lower at 1.8
mL/min/kg. Cmax of empagliflozin in ZDF rat and dogs is 167 nM and 17254 nM, respectively.
Terminal elimination half-life in ZDF rat and dogs is 1.5 h and 6.3 h,
respectively. Bioavailability of empagliflozin in ZDF rat is 33.2%,
while in dogs is higher at 89.0%. Long-term treatment with
empagliflozin, improves glycaemic control
and features of metabolic syndrome in diabetic rats.
Contact us if you need more details on 864070-44-0. We are ready to answer your questions on packaging, logistics, certification or any other aspects about Empagliflozin 864070-44-0、864070-44-0 BI 10773. If these products fail to match your need, please contact us and we would like to provide relevant information.
Molecular Weight:
450.91 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.
Biological Activity
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.
High exposure of empagliflozin is achieved in dogs, with plasma
concentrations >100-fold above IC50 measured 24 h after
administration of 5 mg/kg empagliflozin. The total plasma clearance of
empagliflozin in ZDF rat is 43 mL/min/kg, while in dogs is lower at 1.8
mL/min/kg. Cmax of empagliflozin in ZDF rat and dogs is 167 nM and 17254 nM, respectively.
Terminal elimination half-life in ZDF rat and dogs is 1.5 h and 6.3 h,
respectively. Bioavailability of empagliflozin in ZDF rat is 33.2%,
while in dogs is higher at 89.0%. Long-term treatment with
empagliflozin, improves glycaemic control
and features of metabolic syndrome in diabetic rats.
Contact us if you need more details on 864070-44-0. We are ready to answer your questions on packaging, logistics, certification or any other aspects about Empagliflozin 864070-44-0、864070-44-0 BI 10773. If these products fail to match your need, please contact us and we would like to provide relevant information.
Product Categories : GPCR & G Protein > SGLT Inhibitor
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