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;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

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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

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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..…

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N-Bromosuccinimide Price

ChemScene

Product number: CS-3284
Product name: BX471hydrochloride
Purity: 98.00%
Packaging: 10mg
Price: $150
Updated: 2021/12/16

AK Scientific

Product number: 9145CN
Product name: BX471hydrochloride
Packaging: 10mg
Price: $211
Updated: 2021/12/16

ChemScene

Product number: CS-3284
Product name: BX471hydrochloride
Purity: 98.00%
Packaging: 50mg
Price: $490
Updated: 2021/12/16

Ambeed

Product number: A151361
Product name: BX471hydrochloride
Purity: 98%
Packaging: 25mg
Price: $566
Updated: 2021/12/16

Ambeed

Product number: A151361
Product name: BX471hydrochloride
Purity: 98%
Packaging: 50mg
Price: $735
Updated: 2021/12/16

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BX471 (hydrochloride) Chemical Properties,Usage,Production

Uses

BX471 hydrochloride (ZK-811752 hydrochloride) is a potent, selective non-peptide CCR1 antagonist with Ki of 1 nM for human CCR1, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.

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)

IC 50

MIP-1α-CCR1: 1 nM (Ki); RANTES-CCR1: 2.8 nM (Ki); MCP-3-CCR1: 5.5 nM (Ki)

References

[1] Liang M, et al. Identification and characterization of a potent, selective, and orally active antagonist of the CC chemokine receptor-1. J Biol Chem. 2000 Jun 23;275(25):19000-8. DOI:10.1074/jbc.M001222200
[2] Anders HJ, et al. A chemokine receptor CCR-1 antagonist reduces renal fibrosis after unilateral ureter ligation. J Clin Invest. 2002 Jan;109(2):251-9. DOI:10.1172/JCI14040
[3] Furuichi K, et al. Chemokine receptor CCR1 regulates inflammatory cell infiltration after renal ischemia-reperfusion injury. J Immunol. 2008 Dec 15;181(12):8670-6. DOI:10.4049/jimmunol.181.12.8670
[4] Horuk R, et al. A non-peptide functional antagonist of the CCR1 chemokine receptor is effective in rat heart transplant rejection. J Biol Chem. 2001 Feb 9;276(6):4199-204. DOI:10.1074/jbc.M007457200

BX471 (hydrochloride) Preparation Products And Raw materials

Raw materials

Preparation Products

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BX471 (hydrochloride) Suppliers

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288262-96-4, BX471 (hydrochloride)Related Search:

BX471 (hydrochloride)

N-[5-Chloro-2-[2-[4-(4-fluorobenzyl)-2(R)-methylpiperazin-1-yl]-2-oxoethoxy]phenyl]urea hydrochloride ZK-811752(BX471)

CS-1298

BX471 HYDROCHLORIDE;BX-471 HYDROCHLORIDE;BX 471 HYDROCHLORIDE

ZK-811752 hydrochloride

(R)-1-(5-Chloro-2-(2-(4-(4-fluorobenzyl)-2-methylpiperazin-1-yl)-2-oxoethoxy)phenyl)urea hydrochloride

BX471 hydrochloride (BX-471 hydrochloride

288262-96-4