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(R)-GNE-140 is a selective inhibitor of LDHA and LDHB with IC50 of 3 nM and 5 nM, respectively. (R)-GNE-140 is 18 times more potent than its S-type isomer.
| Molecular Weight | 499.04 |
| Formula | C25H23ClN2O3S2 |
| CAS Number | 2003234-63-5 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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 LDH Products |
|---|
| Nedosiran sodium
Nedosiran sodium is a GalNAc-dsRNA conjugate designed to inhibit production of the hepatic lactate dehydrogenase (LDH) enzyme. |
| MS6105
MS6105 is an LDH protein hydrolysis-targeted chimera (PROTAC) with anticancer activity for studies related to pancreatic cancer. |
| CHK-336
CHK-336 is an inhibitor of the lactate dehydrogenase LDHA and can be used in studies related to primary hyperoxaluria. |
| FX-11
FX-11 (LDHA Inhibitor FX11) is a potent lactate dehydrogenase A (LDHA) inhibitor with an IC50 of 23.3 μM for HeLa cell and a Ki value of 8 μM. FX-11 can reduce ATP levels, induce oxidative stress and ROS production, and cause cell death. |
| GNE-140 racemate
GNE-140 racemate is a racemic mixture of (R)-GNE-140 and (S)-GNE-140. GNE-140 racemate is also a potent lactate dehydrogenase A (LDHA) inhibitor. |
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