1. GPCR/G Protein
    Immunology/Inflammation
  2. CXCR

SCH 563705 

Cat. No.: HY-10011 Purity: 95.34%
Handling Instructions

SCH 563705 is a potent and orally available CXCR2 and CXCR1 antagonist, with IC50s of 1.3 nM, 7.3 nM and Kis of 1 and 3 nM, respectively.

For research use only. We do not sell to patients.

SCH 563705 Chemical Structure

SCH 563705 Chemical Structure

CAS No. : 473728-58-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 297 In-stock
Estimated Time of Arrival: December 31
2 mg USD 210 In-stock
Estimated Time of Arrival: December 31
5 mg USD 317 In-stock
Estimated Time of Arrival: December 31
10 mg USD 436 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

SCH 563705 is a potent and orally available CXCR2 and CXCR1 antagonist, with IC50s of 1.3 nM, 7.3 nM and Kis of 1 and 3 nM, respectively.

IC50 & Target[1][2]

CXCR2

1 nM (Ki)

CXCR1

3 nM (Ki)

CXCR2

1.3 nM (IC50)

CXCR1

7.3 nM (IC50)

Mouse CXCR2

5.2 nM (IC50)

In Vitro

SCH 563705 (Compound 16) is a potent and orally available CXCR2 and CXCR1 antagonist, with IC50s of 1.3 nM, 7.3 nM and Kis of 1 and 3 nM, respectively. SCH 563705 shows potent inhibition against both Gro-a and IL-8 induced human neutrophil migration (chemotaxis IC50 = 0.5 nM, against 30 nM of Gro-a; chemotaxis IC50 = 37 nM, against 3 nM of IL-8)[1]. SCH 563705 potently inhibits mouse CXCR2 (IC50 = 5.2 nM)[2].

In Vivo

SCH 563705 has good oral pharmacokinetic profiles in rats, mice, monkeys and dogs[1]. SCH 563705 (50 mg/kg p.o) reduces blood Ly6G+ Ly6C+ neutrophil frequency and unchanged levels of Ly6GLy6Chi monocytes. SCH563705 (3-30 mg/kg p.o) treatment causes a dosedependent elevation in plasma levels of CXCL1[2].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 30 mg/mL (70.51 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3503 mL 11.7514 mL 23.5029 mL
5 mM 0.4701 mL 2.3503 mL 4.7006 mL
10 mM 0.2350 mL 1.1751 mL 2.3503 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[2]

Mice[2]
Induction of anti-collagen antibody-induced arthritis. Anti-collagen antibody-induced arthritis (ABIA) is induced in BALB/c mice (n = 8 mice per treatment group) as follows. On day 0, mice are injected intraperitoneally with 4 mg ArthritoMAB Arthritis-inducing Antibody Cocktail. On day 3, mice are boosted intraperitoneally with 50 μg of lipopolysaccharide from Escherichia coli 055:B5 in 200 μL sterile PBS. In all studies, SCH 563705 is administered in a vehicle consisting of 0.4% METHOCEL E15 premium hydroxypropyl methylcellulose (MC). Clinical scores are determined daily as follows. Each paw is assigned a score of 0-4 based on the following criteria: asymptomatic, 0; slight redness, 1; one or more swollen digits in addition to redness, 2; swelling of entire paw, 3; ankylosing of joints and residing of swelling, 4. The sum of the four paw scores for each mouse (0-16) are plotted against time to calculate the area under the curve (AUC) of disease activity. Paw hickness measurements are made daily using a micrometer caliper over the metatarsals of the paw. The percent change in paw thickness relative to baseline (day 0) measurements is then calculated[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

425.48

Formula

C₂₃H₂₇N₃O₅

CAS No.

473728-58-4

SMILES

O=C(C(NC1=CC=CC(C(N(C)C)=O)=C1O)=C2N[[email protected]](CC)C3=CC(C(C)C)=CO3)C2=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
SCH 563705
Cat. No.:
HY-10011
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SCH 563705

Cat. No.: HY-10011