BX471 (hydrochloride)
- Product Name
- BX471 (hydrochloride)
- CAS No.
- 288262-96-4
- Chemical Name
- BX471 (hydrochloride)
- Synonyms
- CS-1298;BX471 (hydrochloride);ZK-811752 hydrochloride;BX471 HYDROCHLORIDE;BX-471 HYDROCHLORIDE;BX 471 HYDROCHLORIDE;(R)-1-(5-Chloro-2-(2-(4-(4-fluorobenzyl)-2-methylpiperazin-1-yl)-2-oxoethoxy)phenyl)urea hydrochloride;N-[5-Chloro-2-[2-[4-(4-fluorobenzyl)-2(R)-methylpiperazin-1-yl]-2-oxoethoxy]phenyl]urea hydrochloride ZK-811752(BX471)
- CBNumber
- CB92715615
- Molecular Formula
- C21H25Cl2FN4O3
- Formula Weight
- 471.35
- MOL File
- 288262-96-4.mol
BX471 (hydrochloride) Property
- storage temp.
- under inert gas (nitrogen or Argon) at 2-8°C
- solubility
- DMSO: 150 mg/mL (318.23 mM)
- form
- Solid
- color
- White to yellow
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Danger
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H317May cause an allergic skin reaction
H318Causes serious eye damage
H330Fatal if inhaled
H411Toxic to aquatic life with long lasting effects
- Precautionary statements
-
P260Do not breathe dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P271Use only outdoors or in a well-ventilated area.
P272Contaminated work clothing should not be allowed out of the workplace.
P273Avoid release to the environment.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P284Wear respiratory protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P333+P313IF SKIN irritation or rash occurs: Get medical advice/attention.
P391Collect spillage. Hazardous to the aquatic environment
P403+P233Store in a well-ventilated place. Keep container tightly closed.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- CS-3284
- Product name
- BX471hydrochloride
- Purity
- 98.00%
- Packaging
- 10mg
- Price
- $150
- Updated
- 2021/12/16
- Product number
- 9145CN
- Product name
- BX471hydrochloride
- Packaging
- 10mg
- Price
- $211
- Updated
- 2021/12/16
- Product number
- CS-3284
- Product name
- BX471hydrochloride
- Purity
- 98.00%
- Packaging
- 50mg
- Price
- $490
- Updated
- 2021/12/16
- Product number
- CSN18182
- Product name
- BX471HCl
- Packaging
- 5mg
- Price
- $82
- Updated
- 2021/12/16
- Product number
- CD31002401
- Product name
- BX471hydrochloride
- Purity
- 98+%
- Packaging
- 10mg
- Price
- $114
- Updated
- 2021/12/16
BX471 (hydrochloride) Chemical Properties,Usage,Production
Biological Activity
BX471 hydrochloride (ZK-811752 hydrochloride) is a potent, selective, non-peptide CCR1 antagonist, inhibits human CCR1 activity with a Ki value of 1 nM and is selective for CCR2, CCR5 and CXCR4 250 times.
in vitro
BX471 hydrochloride 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 .It demonstrats a greater than 10,000-fold selectivity for CCR1 compared with 28 G-protein-coupled receptors.It 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 hydrochloride(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.It also inhibits the RANTES-mediated adhesion of T lymphocytes to activated endothelium.
in vivo
BX471 hydrochloride(4 mg/kg, po or iv) 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.It 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%. It has a borderline significant effect on the number of CCR5-positive CD8 cells in the peripheral blood. It reduces the amount of FSP1-positive cells by 65% in UUO kidneys as compared with vehicle control. Pretreatment witih BX471 hydrochloride reduces macrophage and neutrophil accumulation in kidney after ischemia-reperfusion injury.
target
| MIP-1α-CCR1 1 nM (Ki) | RANTES-CCR1 2.8 nM ( Ki) | MCP-3-CCR1 5.5 nM (Ki) |
BX471 (hydrochloride) Preparation Products And Raw materials
Raw materials
Preparation Products
BX471 (hydrochloride) Suppliers
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- 18149758185 18149758185
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- China
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- +1-800-259-7612
- Fax
- +1-800-259-7612
- info@musechem.com
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- United States
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- United States
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- +86-0371-86658258 +8613203830695
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