ZK811752 (BX471)
BX471
CAS: 217645-70-0
Molecular Formula: C21H24ClFN4O3
ZK811752 (BX471) - Names and Identifiers
ZK811752 (BX471) - Physico-chemical Properties
| Molecular Formula | C21H24ClFN4O3 |
| Molar Mass | 434.89 |
| Density | 1.346±0.06 g/cm3(Predicted) |
| Boling Point | 593.5±50.0 °C(Predicted) |
| Solubility | DMSO: ≥ 51 mg/mL |
| Appearance | White powder |
| Color | white to tan |
| pKa | 13.66±0.70(Predicted) |
| Storage Condition | Inert atmosphere,2-8°C |
| In vitro study | BX471 is a potent functional antagonist based on its ability to inhibit a number of CCR1-mediated effects including Ca 2+ mobilization, increase in extracellular acidification rate, CD11b expression, and leukocyte migration. BX471 demonstrats a greater than 10,000-fold selectivity for CCR1 compared with 28 G-protein-coupled receptors. BX471 is also able to displace 125 I-MIP-1α/CCL3 binding to mouse CCR1 in a concentration-dependent manner with a K i of 215±46 nM. Increasing concentrations of BX471 inhibits the Ca 2+ transients induced by MIP-1α/CCL3 in both human and mouse CCR1 with IC 50 of 5.8±1 nM and 198±7 nM, respectively. BX471 (0.1-10 μM) shows a dose-dependent inhibition of RANTES-mediated and shear-resistant adhesion on IL-1β-activated microvascular endothelium in shear flow in isolated blood monocytes. BX471 also inhibits the RANTES-mediated adhesion of T lymphocytes to activated endothelium. |
| In vivo study | BX471 (4 mg/kg, p.o. or i.v.) is orally active with a bioavailability of 60% in dogs. Furthermore, BX471 effectively reduces disease in a rat experimental allergic encephalomyelitis model of multiple sclerosis. BX471 (20 mg/kg, s.c.) reaches peak plasma levels of 9 μM by around 30 minutes, and this rapidly declines to approximately 0.4 μM after 2 hours. From 4 to 8 hours the drug plasma levels drops to 0.1 μM or lower. Mice treated with 20 mg/kg of BX471 for 10 days shows a reduction of interstitial CD45 positive leukocytes of approximately 55%. BX471 has a borderline significant effect on the number of CCR5-positive CD8 cells in the peripheral blood. BX471 reduces the amount of FSP1-positive cells by 65% in UUO kidneys as compared with vehicle control. Pretreatment witih BX471 reduces macrophage and neutrophil accumulation in kidney after ischemia-reperfusion injury. |
ZK811752 (BX471) - Risk and Safety
| Risk Codes | R22 - Harmful if swallowed R50 - Very Toxic to aquatic organisms |
| Safety Description | 61 - Avoid release to the environment. Refer to special instructions / safety data sheets. |
| WGK Germany | 3 |
ZK811752 (BX471) - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.299 ml | 11.497 ml | 22.994 ml |
| 5 mM | 0.46 ml | 2.299 ml | 4.599 ml |
| 10 mM | 0.23 ml | 1.15 ml | 2.299 ml |
| 5 mM | 0.046 ml | 0.23 ml | 0.46 ml |
Last Update：2024-01-02 23:10:35
ZK811752 (BX471) - Reference Information
| biological activity | BX471 (ZK-811752) is an orally effective, selective, non-polypeptide CCR1 antagonist with a Ki value of 1 nM, and its selectivity is 250 times for CCR2,CCR5 and CXCR4. |
| target | MIP-1α-CCR1 nM (Ki) RANTES-CCR1 2.8 nM (Ki) MCP-3-CCR1 5.5 nM (Ki) |
| in vitro study | BX471 is a potent functional antagonist based on its ability to inhibit a number of CCR1-mediated effects including Ca 2 + mobilization, increase in extracellular acidification rate, CD11b expression, and leukocyte migration. BX471 demonstrats a greater than 10,000-fold selectivity for CCR1 compared with 28 G-protein-coupled receptors. BX471 is also able to displace 125 I-MIP-1α/CCL3 binding to mouse CCR1 in a concentration-dependent banner with a K I of 215±46 nM. Increasing concentrations of BX471 inhibits the Ca 2 + transients induced by MIP-1α/CCL3 in both human and mouse CCR1 with IC 50 of 5.8±1 nM and 198±7 nM, respectively. BX471 (0.1-10 μ m) show a dose-dependent inhibition of RANTES-mediated and shear-resistant adhesion on IL-1β-activated microvascular endothelium in shear flow in isolated blood monocytes. BX471 also inhibits the RANTES-mediated adhesion of T lymphocytes to activated endothelium. |
| in vivo study | BX471 (4 mg/kg, p.o. or I. v.) is orally active with a bioavailability of 60% in dogs. Furthermore, BX471 effectively reduces disease in a rat experimental allergic encephalomyelitis model of multiple sclerosis. BX471 (20 mg/kg, s.c.) reaches peak plasma levels of 9 μ m by around 30 minutes, and this rapidly declines to approximately 0.4 μM after 2 hours. From 4 to 8 hours the drug levels drops to 0.1 μM or lower. Mica treated with 20 mg/kg of BX471 for 10 days shows a reduction of interstitial CD45 positive leukocytes of approximately 55%. BX471 has a borderline significant effect on the number of CCR5-positive CD8 cells in the peripheral blood. BX471 reduces the amount of FSP1-positive cells 65% in UUO kidneys as compared with vehicle control. Pretreatment witih BX471 reduces macrophage and neutrophil accumulation in kidney after ischemia-reperfusion injury. |
Last Update：2024-04-09 20:49:11
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Product Name: BX471 Visit Supplier Webpage Request for quotationCAS: 217645-70-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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