CVT-12012 is a potent and orally bioavailable stearoyl-coA desaturase inhibitor, with IC50s of 38 nM, 6.1 nM for rat microsomal and human HEPG2, respectively. CVT-12012 demonstrates good oral bioavailability (78%) in a rat PK study.
| Molecular Weight | 434.41 |
| Formula | C21H21F3N4O3 |
| CAS Number | 1018675-35-8 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 60 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 Stearoyl-CoA Desaturase Products |
|---|
| SSI-4
SSI-4 is an inhibitor of Stearoyl CoA desaturase 1 (SCD1) , which can be modified with 11C, used as a ligand to in vivo small animal PET/CT imaging of SCD1. |
| YTX-465
YTX-465 is a stearoyl-CoA desaturase (Ole1/SCD) inhibitor. YTX-465 inhibits Ole1 and SCD1 with IC50s of 0.039 μM and 30.4 μM, respectively. YTX-465 can be used in the research of Parkinson’s disease and other synucleinopathies. |
| SCD1 inhibitor-4
SCD1 inhibitor-4 is a potent, orally active stearoylCoA desaturase-1 (SCD1) inhibitor. SCD1 inhibitor-4 can be used for the research of diabetes. |
| SCD1 inhibitor-3
SCD1 inhibitor-3 is a safe, potent and orally active SCD1 inhibitor. SCD1 inhibitor-3 can be used for the research of metabolic diseases such as obesity, type II diabetes and dyslipidemia, as well as skin diseases, acne and cancer. |
| CVT-11127
CVT-11127 is a potent SCD inhibitor. CVT-11127 induces apoposis and arrests the cell cycle at the G1/S phase. CVT-11127 has the potential for the research of lung cancer. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
