Vercirnon (GSK1605786A) is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon inhibits CCR9-mediated Ca2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 µM for all). Vercirnon is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively.
| Molecular Weight | 444.93 |
| Formula | C22H21ClN2O4S |
| CAS Number | 698394-73-9 |
| Solubility (25°C) | DMSO ≥ 25 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.
[3] Mark Lwenberg, et al. Next-Generation Therapeutics for IBD
[5] Kristen O Arseneau, et al. Vercirnon for the treatment of Crohn's disease
| Related CCR Products |
|---|
| CCR6 antagonist 1
CCR6 antagonist 1 is a CCR6 antagonist that inhibits the CCL20/CCR6 axis. CCR6 antagonist 1 can be used in the research of autoimmune-mediated inflammatory diseases, such as inflammatory bowel diseases (IBDs). |
| IPG7236
IPG7236 is a selective CCR8 antagonist that also exhibits significant tumor suppression in a mouse xenograft model of human breast cancer.IPG7236 can be used in cancer-related studies. |
| CKLF1-C19
CKLF1-C19 is the C-terminal peptide of human chemokine-like factor 1 (CKLF1). |
| Met-RANTES (human)
Met-RANTES (human) is a partial antagonist of CCR5. |
| IPG0521
IPG0521 is a bifunctional antibody targeting CCR8, which can block CCR8 signaling with high intensity and weak ADCC function, and can effectively inhibit the growth of multiple tumor types in homologous and immunohumanized mouse models. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
