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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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C648383-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $400.90 | |
C648383-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $680.90 | |
C648383-25mg | 25mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $1,350.90 | |
C648383-50mg | 50mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $2,200.90 | |
C648383-100mg | 100mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $3,400.90 |
Specifications & Purity | ≥99% |
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Biochemical and Physiological Mechanisms | CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist ( IC 50 =5.2 nM/1 nM in β-arrestin assay/CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Product Description | CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist ( IC 50 =5.2 nM/1 nM in β-arrestin assay/CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-α induced CD11b expression with an IC 50 of 0.04 μM In Vivo CXCR2-IN-2 (compound 68) (1-10 mg/kg; p.o.; twice daily for 3 days) dose-dependently reduces neutrophil infiltration in vivo in rat and mouse air pouch models . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 6-8 week old male C57Bl/6 mice (Air Pouch Model in Mouse) Dosage: 1, 3, and 10 mg/kg Administration: P.o.; twice daily for 3 days Result: Significantly inhibited neutrophil infiltration into mouse air pouch. Animal Model: 8-10 week old male Wistar rats (Air Pouch Model in Rat) Dosage: 1, 3, and 10 mg/kg Administration: P.o.; twice daily for 3 days Result: Inhibited neutrophil migration to air pouch in rat. Form:Solid IC50& Target:CXCR2 5.2 nM (IC 50 ) CXCR1 3.8 μM (IC 50 ) |
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IUPAC Name | 1-[4-chloro-2-hydroxy-3-[(3S)-3-methyloxolan-3-yl]sulfonylphenyl]-3-[(1R)-2-methylcyclopent-2-en-1-yl]urea |
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INCHI | InChI=1S/C18H23ClN2O5S/c1-11-4-3-5-13(11)20-17(23)21-14-7-6-12(19)16(15(14)22)27(24,25)18(2)8-9-26-10-18/h4,6-7,13,22H,3,5,8-10H2,1-2H3,(H2,20,21,23)/t13-,18+/m1/s1 |
InChi Key | DNXKACKCTLURQN-ACJLOTCBSA-N |
Canonical SMILES | CC1=CCCC1NC(=O)NC2=C(C(=C(C=C2)Cl)S(=O)(=O)C3(CCOC3)C)O |
Isomeric SMILES | CC1=CCC[C@H]1NC(=O)NC2=C(C(=C(C=C2)Cl)S(=O)(=O)[C@]3(CCOC3)C)O |
PubChem CID | 100951623 |
Molecular Weight | 414.90 |
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Solubility | DMSO : 240 mg/mL (578.45 mM; Need ultrasonic) |
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