1. GPCR/G Protein Immunology/Inflammation
  2. CCR
  3. INCB 3284 dimesylate

INCB 3284 dimesylate is a potent, selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2, with an IC50 of 3.7 nM. INCB 3284 dimesylate can be used in the research of acute liver failure.

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

INCB 3284 dimesylate Chemical Structure

INCB 3284 dimesylate Chemical Structure

CAS No. : 887401-93-6

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Other In-stock Forms of INCB 3284 dimesylate:

Other Forms of INCB 3284 dimesylate:

Top Publications Citing Use of Products

View All CCR Isoform Specific Products:

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

INCB 3284 dimesylate is a potent, selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2, with an IC50 of 3.7 nM. INCB 3284 dimesylate can be used in the research of acute liver failure.

IC50 & Target[1]

MCP-1-hCCR2

3.7 nM (IC50)

In Vitro

INCB 3284 dimesylate is a pentent, selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2, with an IC50 of 3.7 nM. INCB 3284 also causes an IC50 of 4.7 nM in antagonism of chemotaxis activity, an IC50 of 84 μM in inhibition of the hERG potassium current. However, INCB 3284 has no effec on CCR1, CCR3, CCR5, CXCR3, and CXCR5, or additional GPCRs at a concentration of 1 μM. Moreover, INCB 3284 potently inhibits CCR2-mediated signaling events such as intracellular calcium mobilization and ERK phosphorylation with IC50 values of 6 and 2.6 nM, respectively[1].

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

In Vivo

INCB 3284 (1 mg/kg/day, ip) reduces liver damage, and decreases microglia activation in AOM-treated mice via inhibition on CCR2. INCB 3284 also significantly reduces the pERK1/2 to tERK1/2 ratio, as well as G-protein signaling pathway activity and proinflammatory cytokine production in cortex lysates from mice administed with azoxymethane[2].

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

Molecular Weight

712.76

Formula

C28H39F3N4O10S2

CAS No.
Appearance

Oil

Color

Colorless to light yellow

SMILES

O=C(NCC(N[C@H]1CN([C@H]2CC[C@](C3=CC=C(OC)N=C3)(O)CC2)CC1)=O)C4=CC=CC(C(F)(F)F)=C4.CS(=O)(O)=O.CS(=O)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 83.3 mg/mL (116.87 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 1.4030 mL 7.0150 mL 14.0300 mL
5 mM 0.2806 mL 1.4030 mL 2.8060 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

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]
Male C57Bl/6 mice (20 to 25 g) are given free access to water and rodent chow and are housed in constant temperature, humidity, and 12 h light-dark cycling. Acute liver failure is induced via a single intraperitoneal (ip) injection of 100 mg/kg of azoxymethane (AOM). In parallel, systemic inhibition of CCR2 and CCR4 activity is accomplished via pretreatment with INCB 3284 (1 mg/kg/day ip) or C021 (1 mg/kg/day ip) for 3 days prior to injection of AOM. Following injection, mice are placed on heating pads adjusted to 37°C and monitored frequently for signs of neurological decline. To reduce the impacts of hypoglycemia and dehydration, cage floors are supplied with hydrogel and rodent chow and after 12 h, and every subsequent 4 h, mice are injected subcutaneously with 5% dextrose in 250 μL of saline. If mice undergo a 20% or greater weight loss they are removed from the study[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, 6 months; -20°C, 1 month (sealed storage, away from moisture). 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 1.4030 mL 7.0150 mL 14.0300 mL 35.0749 mL
5 mM 0.2806 mL 1.4030 mL 2.8060 mL 7.0150 mL
10 mM 0.1403 mL 0.7015 mL 1.4030 mL 3.5075 mL
15 mM 0.0935 mL 0.4677 mL 0.9353 mL 2.3383 mL
20 mM 0.0701 mL 0.3507 mL 0.7015 mL 1.7537 mL
25 mM 0.0561 mL 0.2806 mL 0.5612 mL 1.4030 mL
30 mM 0.0468 mL 0.2338 mL 0.4677 mL 1.1692 mL
40 mM 0.0351 mL 0.1754 mL 0.3507 mL 0.8769 mL
50 mM 0.0281 mL 0.1403 mL 0.2806 mL 0.7015 mL
60 mM 0.0234 mL 0.1169 mL 0.2338 mL 0.5846 mL
80 mM 0.0175 mL 0.0877 mL 0.1754 mL 0.4384 mL
100 mM 0.0140 mL 0.0701 mL 0.1403 mL 0.3507 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

INCB 3284 dimesylate 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.

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
INCB 3284 dimesylate
Cat. No.:
HY-15450
Quantity:
MCE Japan Authorized Agent: