| Description | Eclazolast (RHC 2871) is a lipophilic anti-allergic compound that inhibits mediator release in a mast cell model.Eclazolast inhibits extracellular secretion by affecting only the direct processes associated with Fc(epsilon)RI in the cell.The effect of Eclazolast is highly dependent on the concentration of antigen that triggers the cell. |
| In vitro | Eclazolast 降调了IP3水平。与亲脂药物不同，Eclazolast 不影响人造双层膜和红细胞膜，且不干扰thapsigargin诱导的Ca2+流入。Eclazolast的效果高度依赖于细胞触发时所用抗原浓度。[1] |
| In vivo | REV 2871（CHBZ）在大鼠模型中，已被证实是强效且经口有效的被动皮肤过敏（PCA）抑制剂（ED50=12 mg/kg）。在豚鼠肺切片模型中，CHBZ能够抑制AIR（IC50=800 microM）。[2] |
| Target activity | Rat:12 mg/kg(ED50), AIR:800 microM |
| Synonyms | RHC2871, RHC-2871, REV2871, REV 2871, RHC 2871 |
| molecular weight | 269.68 |
| Molecular formula | C12H12ClNO4 |
| CAS | 80263-73-6 |
| Storage | |Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 27.5 mg/mL (101.97 mM) |
| References | 1. Fischer MJ, et al. Mechanism of action of the nonlipophilic antiallergic drug eclazolast (REV 2871) in the inhibition of mediator release in a mast cell model. Inflamm Res. 1999 ; 48(11):569-574. 2. Coutts SM, et al. REV 2871 (CHBZ): a potent antiallergic agent with a novel mechanism of action. II. Studies on the mechanism of action. Biochem Pharmacol. 1987 ; 36(5):673-682. 3. Khandwala A, et al. REV 2871 (CHBZ): a potent antiallergic agent with a novel mechanism of action. I. Activity profile as an inhibitor of mediator release. Biochem Pharmacol. 1987 ; 36(5):663-672. 4. Coutts SM, et al. REV 2871 (CHBZ): a novel inhibitor of histamine release. Agents Actions. 1986 ; 18(3-4):318-324. |