BX-513 hydrochloride
Based on 1 Customer Validation
BX-513 hydrochloride (VUF2274 hydrochloride) is a CCR1 antagonist that inhibits chemokine binding and blocks US28 signaling. BX-513 hydrochloride inhibits human CCR1 with a Ki of 40 nM. BX-513 hydrochloride blocks CCL3-mediated signaling/chemotaxis, CCR1-mediated chemokine signaling, calcium mobilization, extracellular acidification, and US28-mediated HIV entry, with an IC50 of 4.9 μM. BX-513 hydrochloride can be used for research on hcmv infection.
For research use only. We do not sell to patients.
- Purity : 99.94%
- CAS No.: 1216540-18-9
- Formula: C28H30Cl2N2O
- Molecular Weight:481.46
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
Description
IC50 & Target
[2]|
CCR1 40 nM (Ki) |
In Vitro
BX 513 hydrochloride binds to human CCR1 with a Ki of 40 nM and exhibits species-dependent affinity, showing weaker potency against rabbit, mouse, and marmoset CCR1[2].
BX 513 hydrochloride inhibits MIP-1-induced extracellular acidification and intracellular Ca2+ mobilization in cells expressing human CCR1 with a potency of 40 nM[2].
BX 513 hydrochloride inhibits MIP-1 and RANTES-induced PBMC migration, but does not inhibit MIP-1, MCP-1, or SDF-1-stimulated migration[2].
BX-513 hydrochloride inhibits the binding of radiolabeled human MIP-1α to HEK 293 cells expressing human CCR1 with a Ki of 40 nM, while its potency against mouse CCR1 is approximately 88-fold lower[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1216540-18-9
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Appearance Solid
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Molecular Weight 481.46
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Formula C28H30Cl2N2O
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Color White to off-white
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SMILES
N#CC(C1=CC=CC=C1)(C2=CC=CC=C2)CCCN3CCC(O)(C4=CC=C(Cl)C=C4)CC3.[H]Cl
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Synonyms
VUF2274 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (103.85 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Hulshof JW, et al. Synthesis and pharmacological characterization of novel inverse agonists acting on the viral-encoded chemokine receptor US28. Bioorganic & medicinal chemistry. 2006 Nov 01;14(21):7213-30. [Content Brief]
[2]. Horuk R, et al. BX471: a CCR1 antagonist with anti-inflammatory activity in man. Mini reviews in medicinal chemistry. 2005 Sep;5(9):791-804. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0770 mL | 10.3851 mL | 20.7702 mL | 51.9254 mL |
| 5 mM | 0.4154 mL | 2.0770 mL | 4.1540 mL | 10.3851 mL | |
| 10 mM | 0.2077 mL | 1.0385 mL | 2.0770 mL | 5.1925 mL | |
| 15 mM | 0.1385 mL | 0.6923 mL | 1.3847 mL | 3.4617 mL | |
| 20 mM | 0.1039 mL | 0.5193 mL | 1.0385 mL | 2.5963 mL | |
| 25 mM | 0.0831 mL | 0.4154 mL | 0.8308 mL | 2.0770 mL | |
| 30 mM | 0.0692 mL | 0.3462 mL | 0.6923 mL | 1.7308 mL | |
| 40 mM | 0.0519 mL | 0.2596 mL | 0.5193 mL | 1.2981 mL | |
| 50 mM | 0.0415 mL | 0.2077 mL | 0.4154 mL | 1.0385 mL | |
| 60 mM | 0.0346 mL | 0.1731 mL | 0.3462 mL | 0.8654 mL | |
| 80 mM | 0.0260 mL | 0.1298 mL | 0.2596 mL | 0.6491 mL | |
| 100 mM | 0.0208 mL | 0.1039 mL | 0.2077 mL | 0.5193 mL |