1. GPCR/G Protein Immunology/Inflammation
  2. CXCR
  3. SCH 563705

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

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Based on 3 publication(s) in Google Scholar

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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].

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

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].

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

Molecular Weight

425.48

Formula

C23H27N3O5

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C(NC1=CC=CC(C(N(C)C)=O)=C1O)=C2N[C@H](CC)C3=CC(C(C)C)=CO3)C2=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 30 mg/mL (70.51 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3503 mL 11.7514 mL 23.5029 mL 58.7572 mL
5 mM 0.4701 mL 2.3503 mL 4.7006 mL 11.7514 mL
10 mM 0.2350 mL 1.1751 mL 2.3503 mL 5.8757 mL
15 mM 0.1567 mL 0.7834 mL 1.5669 mL 3.9171 mL
20 mM 0.1175 mL 0.5876 mL 1.1751 mL 2.9379 mL
25 mM 0.0940 mL 0.4701 mL 0.9401 mL 2.3503 mL
30 mM 0.0783 mL 0.3917 mL 0.7834 mL 1.9586 mL
40 mM 0.0588 mL 0.2938 mL 0.5876 mL 1.4689 mL
50 mM 0.0470 mL 0.2350 mL 0.4701 mL 1.1751 mL
60 mM 0.0392 mL 0.1959 mL 0.3917 mL 0.9793 mL
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SCH 563705 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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