COG 133 is a fragment of Apolipoprotein E (APOE) peptide with potent anti-inflammatory and neuroprotective effects. COG 133 is also a nAChR antagonist with an IC50 of 445 nM. COG 133 (0.02, 0.2, and 2.0 μM) improved cell numbers in glutamine free media. In IEC-6 cells, COG 133 (0.2-20 μM) improved cell migration following 5-FU challenge, reaching the same migration level as controls. COG 133 (3 μM) significantly increased the mitotic crypt numbers in C57BL6J wild-type animals. COG 133 treatment improved crypt architecture and reduced lamina propria inflammation. COG 133 (3 μM) significantly reduced the intestinal MPO levels. COG 133 partially decreased TNF-α level in the proximal small intestine from 5-FU-treated mice. In both wild-type and ApoE knock-out mice, COG 133 (3 μM) reverted the increase in Tunel-positive cells in the proximal intestine induced by 5-FU. COG 133 caused higher expression of the NF-κB in the improved intestinal mucosa.
| Molecular Weight | 2169.71 |
| Formula | C97H181N37O19 |
| CAS Number | 514200-66-9 |
| Solubility (25°C) | Water 1 mg/mL |
| Storage | -20°C, 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.
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