GNF351 is a full aryl hydrocarbon receptor (AHR) antagonist. GNF351 competes with a photoaffinity AHR ligand for binding to the AHR with an IC50 of 62 nM. GNF351 (500 nM, 48 hours) significantly reduces the percentage of Ki67-positive cells and cell number after treating proliferating monolayer cultures of human keratinocytes.
| Molecular Weight | 411.5 |
| Formula | C24H25N7 |
| CAS Number | 1227634-69-6 |
| 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 Aryl hydrocarbon Receptor Products |
|---|
| KYN-101
KYN-101 is a potent, selective and orally active AHR inhibitor. |
| AHR agonist 4
AHR agonist 4 is an agonist of Aryl hydrocarbon receptor (AHR), assocaited with the immune balance of Th17/22 and Treg cells. |
| Benzyl butyl phthalate
Benzyl butyl phthalate can trigger the migration and invasion of hemangioma (HA) cells via upregulation of Zeb1. Benzyl butyl phthalate activates aryl hydrocarbon receptor (AhR) in breast cancer cells to stimulate SPHK1/S1P/S1PR3 signaling and enhances formation of metastasis-initiating breast cancer stem cells (BCSCs). |
| Indole-3-ylacetaldehyde
Indole-3-ylacetaldehyde (I3A) |
| 1,4-Chrysenequinone
1,4-Chrysenequinone, a polycyclic aromatic quinone, acts as an activator of aryl hydrocarbon receptor (AhR). |
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