Gardiquimod diTFA, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod diTFA could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod diTFA specifically activates TLR7 when used at concentrations below 10 μM.
| Molecular Weight | 541.44 |
| Formula | C21H25F6N5O5 |
| CAS Number | 1159840-61-5 |
| Form | Solid |
| Solubility (25°C) | DMSO 50 mg/mL (ultrasonic) Water 25 mg/mL (ultrasonic) |
| Storage | 4°C, dry, 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.
| Related TLR Products |
|---|
| Kdo2-Lipid A ammonium
Kdo2-Lipid A ammonium is a chemically defined lipopolysaccharide (LPS) with endotoxic activity equivalent to LPS.Kdo2-Lipid A ammonium is highly selective for TLR4 and stimulates the release of TNF and PGE2. |
| PSMα3
PSMα3 is a peptide for manipulating DCs to become tolerogenic for DC vaccination strategies. |
| Pam2CSK4
Pam2CSK4, a lipopeptide, is a TLR6-independent TLR2 ligand and agonist. |
| MAPK-IN-1
MAPK-IN-1 is a MAPK signaling pathway inhibitor. |
| Cobitolimod
Cobitolimod is a first-of-its-kind (first-in-class), synthetic oligodeoxynucleotide (ODN) containing unmethylated CpG motifs that activates TLR9 in specific cells, including intestinal T and B lymphocytes as well as antigen-presenting cells (APCs), and can be used in studies related to inflammatory bowel disease (IBD). |
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