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BX 513 hydrochloride

Catalog No.GC13299

Selective CCR1 antagonist

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BX 513 hydrochloride Chemical Structure

Cas No.: 1216540-18-9

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10mg
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50mg
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Sample solution is provided at 25 µL, 10mM.

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Background

Ligands for the CCR1 receptor (MIP-1α and RANTES) have been implicated in plenty of chronic inflammatory diseases, most notably multiple sclerosis and rheumatoid arthritis. BX 513 is a novel non-peptide CCR1 receptor antagonists.

In vitro: BX 513 has been shown to have at least 200-fold selectivity for CCR1 inhibition over other human 7-TM receptors, including other chemokine receptors. In addition, data obtained from in-vitro functional assays demonstrated the functional antagonism of BX 513 and structurally related analogues against the CCR1 receptor in a dose-dependent manner [1]. BX 513 also showed concentration-dependent inhibition of MIP-1α-induced extracellular acidification and Ca2+ mobilization demonstrating functional antagonism. When given alone, the compound did not elicit any responses, suggesting the absence of intrinsic agonist activity. BX 513 inhibited MIP-1α- and RANTES-induced migration in peripheral blood cells in a dose-responsive manner. Selectivity testing against a panel of 7 transmembrane domain receptors indicated that BX 513 is inactive on a number of receptors at concentrations up to 10 μM [2].

In vivo: Currently, there is no animal in-vivo data available.

Clinical trial: Up to now, BX 513 is still in the preclinical development stage.

Reference:
[1] Ng HP, May K, Bauman JG, Ghannam A, Islam I, Liang M, Horuk R, Hesselgesser J, Snider RM, Perez HD, Morrissey MM.  Discovery of novel non-peptide CCR1 receptor antagonists. J Med Chem. 1999 Nov 4;42(22):4680-94.
[2] Hesselgesser J, Ng HP, Liang M, Zheng W, May K, Bauman JG, Monahan S, Islam I, Wei GP, Ghannam A, Taub DD, Rosser M, Snider RM, Morrissey MM,Perez HD, Horuk R.  Identification and characterization of small molecule functional antagonists of the CCR1 chemokine receptor. J Biol Chem. 1998 Jun 19;273(25):15687-92.

Chemical Properties

Cas No. 1216540-18-9 SDF
Chemical Name 5-(4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl)-2,2-diphenylpentanenitrile hydrochloride
Canonical SMILES ClC1=CC=C(C(CC2)(O)CCN2CCCC(C3=CC=CC=C3)(C4=CC=CC=C4)C#N)C=C1.Cl
Formula C28H29ClN2O.HCl M.Wt 481.46
Solubility <48.15mg/ml in DMSO; <24.07mg/ml in ethanol Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.077 mL 10.3851 mL 20.7702 mL
5 mM 0.4154 mL 2.077 mL 4.154 mL
10 mM 0.2077 mL 1.0385 mL 2.077 mL
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Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 26 reference(s) in Google Scholar.)

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