R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5nM, an approximately 5000-fold more selectivity for ALK5 than p38 mitogen-activated protein kinase (MAPK). Oral administration of R-268712 at doses of 1, 3 and 10mg/kg also inhibited the development of renal fibrosis in a dose-dependent manner in a unilateral ureteral obstruction (UUO) model. R-268712 reduced proteinuria and glomerulosclerosis significantly with improvement of renal function. R-268712 could suppress glomerulonephritis as well as glomerulosclerosis by an inhibitory mechanism that involves suppression of TGF-β signaling.
| Molecular Weight | 363.39 |
| Formula | C20H18FN5O |
| CAS Number | 879487-87-3 |
| Solubility (25°C) | DMSO: ≥ 90 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 TGF-beta/Smad Products |
|---|
| A 83-01 sodium
A 83-01 sodium is a potent inhibitor of TGF-β type I receptors ALK5, ALK4, and ALK7, inhibiting ALK5, ALK4, and ALK7-induced transcription with IC50 values of 12 nM, 45 nM, and 7.5 nM, respectively. |
| Myristoyl tetrapeptide-12
Myristoyl tetrapeptide-12 directly activates SMAD2 and induces the linking of SMAD3 with DNA. |
| H-Leu-Ser-Lys-Leu-OH
H-Leu-Ser-Lys-Leu-OH (LSYL) is a latency-associated peptide at the amino terminus of LAP, with inhibitory effect on TGF-β1 activation. |
| SY-LB-35
SY-LB-35 is a potent bone morphogenetic protein (BMP) receptor agonist. |
| DT-6
DT-6 is an effective TGF-β1 inhibitor. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
