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Chemical Structure| 288262-96-4 Chemical Structure| 288262-96-4

Structure of BX471 HCl
CAS No.: 288262-96-4

Chemical Structure| 288262-96-4

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BX471 HCl 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 hydrochloride; BX471 hydrochloride

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Product Details of BX471 HCl

CAS No. :288262-96-4
Formula : C21H25Cl2FN4O3
M.W : 471.35
SMILES Code : O=C(N)NC1=CC(Cl)=CC=C1OCC(N2[C@H](C)CN(CC3=CC=C(F)C=C3)CC2)=O.[H]Cl
Synonyms :
ZK-811752 hydrochloride; BX471 hydrochloride
MDL No. :MFCD28167805
InChI Key :FRUCNQBAWUHKLS-PFEQFJNWSA-N
Pubchem ID :5311124

Safety of BX471 HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of BX471 HCl

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HEK_CCR1Gqi5 cells 47 nM 2 h Evaluate the inhibitory effect of BX471 on CCL3 binding to HEK_CCR1Gqi5 cell membranes Br J Pharmacol. 2014 Nov;171(22):5127-38
macrophages 10 μM 24 h BX-471 treatment inhibited CCL22 and TNF-α release and promoted IL-10 release. Additionally, BX-471 increased toll-like receptor-9 (TLR9) expression and decreased TLR2 and TLR6 expression in these cells. Br J Pharmacol. 2005 Aug;145(8):1160-72
Mouse chondrocytes 10 μM 24 h Evaluate the effect of BX471 on IL-1β-induced inflammatory indicators, results showed that BX471 significantly reduced the expression of COX2 and iNOS Mol Med. 2024 Jun 3;30(1):74
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 chondrocyte 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 days 0, 4, and 8 inhibition of 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 dose-dependently reduced 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, total of 5 injections Evaluate the effect of BX471 on cartilage destruction in the DMM model, results showed that BX471 significantly alleviated cartilage destruction Mol Med. 2024 Jun 3;30(1):74
Mice OVA-induced allergic asthma model Subcutaneous injection 20 mg/kg Every 8 hours for 3 days Alleviation of OVA-induced pulmonary eosinophilic inflammation 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

2.12mL

0.42mL

0.21mL

10.61mL

2.12mL

1.06mL

21.22mL

4.24mL

2.12mL

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