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Chemical Structure| 217645-70-0 Chemical Structure| 217645-70-0

Structure of BX471
CAS No.: 217645-70-0

Chemical Structure| 217645-70-0

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

Synonyms: ZK-811752; BAY 865047; SH T 04268H

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Product Details of BX471

CAS No. :217645-70-0
Formula : C21H24ClFN4O3
M.W : 434.89
SMILES Code : O=C(N)NC1=CC(Cl)=CC=C1OCC(N2[C@H](C)CN(CC3=CC=C(F)C=C3)CC2)=O
Synonyms :
ZK-811752; BAY 865047; SH T 04268H
MDL No. :MFCD09859709
InChI Key :XQYASZNUFDVMFH-CQSZACIVSA-N
Pubchem ID :512282

Safety of BX471

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of BX471

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
RPMI 8226 cells 47 and 58 nM 2 h Evaluate the inhibitory ability of BX471 on CCL3 binding Br J Pharmacol. 2014 Nov;171(22):5127-38
macrophages 10 μM 24 h BX-471 treatment significantly increased immunoreactive levels of CCL3 and CCL6 and significantly decreased CCL22 levels. Additionally, significantly less TNF-α was present, whereas IL-10 levels were dramatically increased in these cell-free supernatants. BX-471 also increased TLR9 and decreased TLR2 and TLR6 expression. Br J Pharmacol. 2005 Aug;145(8):1160-72
Mouse chondrocytes 5, 10 μM 24 h Evaluate the effect of BX471 on IL-1β-induced chondrocyte senescence, results showed that BX471 significantly attenuated the excessive expression of senescence markers P16INK4a and P21CIP1 Mol Med. 2024 Jun 3;30(1):74
Mouse chondrocytes 2.5, 5, 10 μM 24 h Evaluate the effect of BX471 on cell viability, results showed that different concentrations of BX471 did not affect cell viability Mol Med. 2024 Jun 3;30(1):74
bone marrow-derived eosinophils (BMDEs) 1 μM on days 0, 4, and 8 CCR1 inhibition can decrease committed eosinophil differentiation Signal Transduct Target Ther. 2021 Feb 28;6(1):91

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Chronic fungal asthma model Intraperitoneal injection 3, 10, or 30 mg/kg Once daily from day 15 to day 30 BX-471 treatment significantly attenuated all features of established chronic fungal asthma in mice, including airway inflammation, hyper-responsiveness, and remodeling. The maximal therapeutic effect was observed at the 10 mg/kg dose. Br J Pharmacol. 2005 Aug;145(8):1160-72
C57BL/6J mice Destabilization of the medial meniscus (DMM) model Intra-articular injection 1.5, 3 mg/kg Every 7 days for a total of five injections Evaluate the effect of BX471 on cartilage destruction in the DMM model, results showed that BX471 delayed OA development, reduced OA-related features and improved cartilage histology Mol Med. 2024 Jun 3;30(1):74
Mice OVA-induced allergic asthma model Subcutaneous injection 20 mg/kg Every 8 hours during the OVA challenge period BX471 treatment significantly reversed OVA-induced eosinophilia, reduced pulmonary eosinophil infiltration and inflammatory responses Signal Transduct Target Ther. 2021 Feb 28;6(1):91

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.30mL

0.46mL

0.23mL

11.50mL

2.30mL

1.15mL

22.99mL

4.60mL

2.30mL

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