SCH 563705

Name: SCH 563705
Brand: MedChemExpress
SKU: HY-10011
Rating: 5.0 (3 reviews)

Cat. No.: HY-10011 Purity: 99.86%: FAQs
Data Sheet SDS COA Handling Instructions

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

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

SCH 563705 Chemical Structure

CAS No. : 473728-58-4

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 869	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 869	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 380	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 790	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 1230	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 2100	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 2840	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 3850	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of SCH 563705:

(S)-SCH 563705 Get quote
(Rac)-SCH 563705 Get quote

3 Publications Citing Use of MCE SCH 563705

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View All Isoforms

CXCR CXCR1 CXCR2 CXCR3 CXCR4 CXCR7 CXCR6

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

SCH 563705 is a potent and orally available CXCR2 and CXCR1 antagonist, with IC₅₀s of 1.3 nM, 7.3 nM and K_is 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)

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	1.3 nM Compound: 16	Displacement of [125I]IL8 from human CXCR2 expressed in CHO cells by SPA Displacement of [125I]IL8 from human CXCR2 expressed in CHO cells by SPA	[PMID: 17459706]
CHO	IC₅₀	7.3 nM Compound: 16	Displacement of [125I]IL8 from human CXCR1 expressed in CHO cells by SPA Displacement of [125I]IL8 from human CXCR1 expressed in CHO cells by SPA	[PMID: 17459706]
Neutrophil	IC₅₀	0.5 nM Compound: 16	Inhibition of GROalpha-induced migration of human neutrophils by chemotaxis assay Inhibition of GROalpha-induced migration of human neutrophils by chemotaxis assay	[PMID: 17459706]
Neutrophil	IC₅₀	37 nM Compound: 16	Inhibition of IL8-induced migration of human neutrophils by chemotaxis assay Inhibition of IL8-induced migration of human neutrophils by chemotaxis assay	[PMID: 17459706]

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 K_is 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.

473728-58-4

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 : 100 mg/mL (235.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (11.75 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (11.75 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (11.75 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.86%

Select Batch:

Data Sheet (284 KB) SDS (701 KB)

COA (248 KB) HNMR (143 KB) RP-HPLC (162 KB) LCMS (106 KB)

Handling Instructions (2659 KB)

References

[1]. Chao J, et al. C(4)-alkyl substituted furanyl cyclobutenediones as potent, orally bioavailable CXCR2 and CXCR1 receptor antagonists. Bioorg Med Chem Lett. 2007 Jul 1;17(13):3778-83. [Content Brief]

[2]. Min SH, et al. Pharmacological targeting reveals distinct roles for CXCR2/CXCR1 and CCR2 in a mouse model of arthritis. Biochem Biophys Res Commun. 2010 Jan 1;391(1):1080-6. [Content Brief]

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

[1]. Chao J, et al. C(4)-alkyl substituted furanyl cyclobutenediones as potent, orally bioavailable CXCR2 and CXCR1 receptor antagonists. Bioorg Med Chem Lett. 2007 Jul 1;17(13):3778-83. [Content Brief]

[2]. Min SH, et al. Pharmacological targeting reveals distinct roles for CXCR2/CXCR1 and CCR2 in a mouse model of arthritis. Biochem Biophys Res Commun. 2010 Jan 1;391(1):1080-6. [Content Brief]

Complete Stock Solution Preparation Table

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
	80 mM	0.0294 mL	0.1469 mL	0.2938 mL	0.7345 mL
	100 mM	0.0235 mL	0.1175 mL	0.2350 mL	0.5876 mL

SCH 563705 Related Classifications

Inflammation/Immunology Endocrinology

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.

Keywords:

SCH 563705473728-58-4SCH563705SCH-563705CXCRCXC chemokine receptorsC-X-C motif chemokine receptorsInhibitorinhibitorinhibit

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SCH 563705

Customer Review

Other Forms of SCH 563705:

SCH 563705 Related Antibodies

3 Publications Citing Use of MCE SCH 563705

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All CXCR Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

SCH 563705 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

SCH 563705 Related Classifications

Keywords:

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