LX2761 is a locally acting SGLT1 and SGLT2 inhibitor in vitro with IC50 values of 2.2 nM and 2.7 nM for hSGLT1 and hSGLT2, respectively. LX2761 is a very potent, chemically stable, and luminally restricted molecule that achieved proof of concept in OGTT at very low doses. LX2761 was designed to remain in the intestine after oral delivery to inhibit SGLT1 locally without affecting the SGLT1/2 mechanism in the kidney.
| Molecular Weight | 601.8 |
| Formula | C32H47N3O6S |
| CAS Number | 1610954-97-6 |
| Storage | -20°C, dry, protect from light, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related SGLT Products |
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Tianagliflozin is an SGLT2 inhibitor that may be used in studies related to type 2 diabetes. |
| JTT-662
JTT-662 is an SGLT1 inhibitor that can be used in studies related to type 2 diabetes. |
| JP-2266
JP-2266 is a dual SGLT1/2 inhibitor that can be used in studies related to diabetes. |
| Tofogliflozin
Tofogliflozin(CSG-452) is a potent and highly specific sodium/glucose cotransporter 2(SGLT2) inhibitor with Ki values of 2.9, 14.9, and 6.4 nM for human, rat, and mouse SGLT2. |
| Mizagliflozin
Mizagliflozin (DSP-3235 free base) is a potent, orally active and selective SGLT1 inhibitor, with a Ki of 27 nM for human SGLT1. Mizagliflozin displays 303-fold selectivity over SGLT2. Mizagliflozin is used as an antidiabetic agent that can modify postprandial blood glucose excursion. Mizagliflozin also exhibits potential in the amelioration of chronic constipation. |
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