Urea, N-[5-chloro-2-[2-[(2R)-4-[(4-fluorophenyl)Methyl]-2-Methyl-1-piperazinyl]-2-oxoethoxy]phenyl]-
- Product Name
- Urea, N-[5-chloro-2-[2-[(2R)-4-[(4-fluorophenyl)Methyl]-2-Methyl-1-piperazinyl]-2-oxoethoxy]phenyl]-
- CAS No.
- 217645-70-0
- Chemical Name
- Urea, N-[5-chloro-2-[2-[(2R)-4-[(4-fluorophenyl)Methyl]-2-Methyl-1-piperazinyl]-2-oxoethoxy]phenyl]-
- Synonyms
- CS-1299;BX471(ZK-811752);ZK811752 (BX471);BX-471(Free base);ZK-811752(BX-471) (free base);BX471 - CAS 217645-70-0 - Calbiochem;ZK 811752;ZK811752;ZK-811752;BX-471; BX 471;BX-471;BX471,ZK811752,CCR,CC chemokine receptor,Inhibitor,inhibit,ZK 811752;(5-Chloro-2-{2-[4-(4-fluoro-benzyl)-2-Methyl-piperazin-1-yl]-2-oxo-ethoxy}-phenyl)-urea;(R)-1-[5-Chloro-2-[2-[4-(4-fluorobenzyl)-2-methylpiperazin-1-yl]-2-oxoethoxy]phenyl]urea
- CBNumber
- CB72628515
- Molecular Formula
- C21H24ClFN4O3
- Formula Weight
- 434.89
- MOL File
- 217645-70-0.mol
Urea, N-[5-chloro-2-[2-[(2R)-4-[(4-fluorophenyl)Methyl]-2-Methyl-1-piperazinyl]-2-oxoethoxy]phenyl]- Property
- Boiling point:
- 593.5±50.0 °C(Predicted)
- Density
- 1.346±0.06 g/cm3(Predicted)
- storage temp.
- Inert atmosphere,2-8°C
- solubility
- DMSO: ≥25mg/mL
- pka
- 13.66±0.70(Predicted)
- form
- White powder
- color
- white to tan
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H312Harmful in contact with skin
H315Causes skin irritation
H319Causes serious eye irritation
H332Harmful if inhaled
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing 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.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P330Rinse mouth.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P362Take off contaminated clothing and wash before reuse.
P403+P233Store in a well-ventilated place. Keep container tightly closed.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- SML0020
- Product name
- BX 471
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $105.6
- Updated
- 2024/03/01
- Product number
- SML0020
- Product name
- BX 471
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $698
- Updated
- 2024/03/01
- Product number
- 5.04345
- Product name
- BX471 - CAS 217645-70-0 - Calbiochem
- Packaging
- 5mg
- Price
- $71.4
- Updated
- 2022/05/15
- Product number
- B6060
- Product name
- BX 471
- Packaging
- 5MG
- Price
- $157
- Updated
- 2024/03/01
- Product number
- B6060
- Product name
- BX 471
- Packaging
- 25MG
- Price
- $557
- Updated
- 2024/03/01
Urea, N-[5-chloro-2-[2-[(2R)-4-[(4-fluorophenyl)Methyl]-2-Methyl-1-piperazinyl]-2-oxoethoxy]phenyl]- Chemical Properties,Usage,Production
Description
The CC chemokine receptor-1 (CCR1), whose ligands include macrophage inflammatory protein-1α (MIP-1α), RANTES, and monocyte chemotactic protein-3 (MCP-3), has a central role in leukocyte trafficking and is highly expressed in certain autoimmune diseases. BX 471 is a nonpeptide CCR1 antagonist that has been shown to displace MIP-1α, RANTES, and MCP-3 with Ki values of 1, 2.8, and 5.5 nM, respectively. It demonstrates >10,000-fold selectivity for CCR1 over 28 additional G protein-coupled receptors, including related chemokine receptors. In a rat experimental allergic encephalomyelitis model of multiple sclerosis, BX 471 at 50 mg/kg was shown to significantly reduce the severity of the disease. BX 471 also decreases the inflammatory response during sepsis, blocks migration of monocytes isolated from rheumatoid arthritis patients, and prevents macrophage and T-cell recruitment in a mouse model of lupus nephritis.
Uses
BX471 has been used in chemotaxis assay to study the responses of HEK293 cells expressing human C-C motif chemokine receptor 1 (CCR1) to CC motif ligand 3 (CCL3)-induced cell migration. It has also been used as a CCR1 inhibitor to assess the effects of CCR1 on the migration and epithelial-mesenchymal transition (EMT).
Biochem/physiol Actions
BX471 blocks CCR1 and downregulates the mRNA expression of ICAM-1, P-selectin and E-selectin. It decreases the inflammatory responses in sepsis, prevents monocyte recruitment in inflammation sites in rheumatoid arthritis patients and inhibits interstitial leukocyte recruitment and fibrosis in mouse model of lupus nephritis.
in vitro
competition binding studies revealed that bx 471 was able to displace the ccr1 ligands macrophage inflammatory protein-1a, rantes, and monocyte chemotactic protein-3 with high affinity. bx 471 was a potent functional antagonist based on its ability to inhibit plenty of ccr1-mediated effects. bx 471 also demonstrated a greater than 10,000-fold selectivity for ccr1 compared with 28 g-protein-coupled receptors [1].
in vivo
pharmacokinetic studies demonstrated that bx 471 was orally active with a 60% bioavailability in dogs. furthermore, in a rat experimental allergic encephalomyelitis model of multiple sclerosis, bx 471 effectively reduces disease [1].
storage
Store at +4°C
References
[1] liang m, mallari c, rosser m, ng hp, may k, monahan s, bauman jg, islam i, ghannam a, buckman b, shaw k, wei gp, xu w, zhao z, ho e, shen j, oanh h, subramanyam b, vergona r, taub d, dunning l, harvey s, snider rm, hesselgesser j, morrissey mm, perez hd. 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.
Urea, N-[5-chloro-2-[2-[(2R)-4-[(4-fluorophenyl)Methyl]-2-Methyl-1-piperazinyl]-2-oxoethoxy]phenyl]- Preparation Products And Raw materials
Raw materials
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View Lastest Price from Urea, N-[5-chloro-2-[2-[(2R)-4-[(4-fluorophenyl)Methyl]-2-Methyl-1-piperazinyl]-2-oxoethoxy]phenyl]- manufacturers
- Product
- BX471 217645-70-0
- Price
- US $1.00/KG
- Min. Order
- 1KG
- Purity
- Min98% HPLC
- Supply Ability
- g/kg/ton
- Release date
- 2019-12-30