2. GPCR/G Protein Immunology/Inflammation
  3. CCR
  4. JNJ-27141491

JNJ-27141491 is a selective, noncompetitive and orally active functional antagonist of human CCR2.

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

JNJ-27141491

JNJ-27141491 Chemical Structure

CAS No. : 871313-59-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

JNJ-27141491 Related Antibodies

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CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

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Description

JNJ-27141491 is a selective, noncompetitive and orally active functional antagonist of human CCR2[1].

IC50 & Target[1]

hCCR2

 

In Vitro

JNJ-27141491 inhibits MCP-1-induced [35S]GTPγS binding to hCCR2-CHO cell membranes (IC50=38±9 nM) and reduces MCP-1-induced Ca2+ mobilization in hCCR2-CHO cells (IC50=13±1 nM), in THP-1 cells (IC50=13±2 nM), and in human blood monocytes (IC50=43±4 nM). JNJ-27141491 also inhibits chemotaxis of human PBMC toward MCP-1, with an IC50 value of 97±16 nM[1].
JNJ-27141491 competes with the binding of MCP-1 to hCCR2 and acts as a noncompetitive antagonist of the CCR2 receptor[1].

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

JNJ-27141491 Related Antibodies
In Vivo

JNJ-27141491 (5-40 mg/kg; oral; once or twice daily) inhibits recruitment of monocytes and neutrophils into the alveolar air space of transgenic hCCR2 knockin mice[1].
JNJ-27141491 (20 mg/kg; oral; daily for 16 days) delays experimental autoimmune encephalomyelitis (EAE) in transgenic CCR2 mice[1].

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

Animal Model: Transgenic mCCR2 knockout/hCCR2 knockin C57BL/6 mice[1]
Dosage: 5, 10, 20, or 40 mg/kg
Administration: Oral, once or twice daily
Result: Once-daily oral treatment with 40, 20, 10, or 5 mg/kg inhibited the monocyte influx with 77, 57, 49, and 27%, respectively, compared with vehicle treatment, whereas this value was 74 and 22% after twice-daily oral treatment with 20 or 5 mg/kg. The neutrophil influx was also reduced; neutrophil numbers were decreased, with 56, 45, 20, and 8% after 40, 20, 10, or 5 mg/kg q.d. treatments and with 45 and 20% after 20 and 5 mg/kg b.i.d. treatments.
Molecular Weight

379.38

Formula

C17H15F2N3O3S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC[C@@H](C1=CC(F)=C(F)C=C1)N2C(C(OC)=O)=C(C3=CC=NO3)NC2=S
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture and light

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

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (131.79 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 2.6359 mL 13.1794 mL 26.3588 mL
5 mM 0.5272 mL 2.6359 mL 5.2718 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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Working solution concentration: mg/mL
Purity & Documentation
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 and light). 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 2.6359 mL 13.1794 mL 26.3588 mL 65.8970 mL
5 mM 0.5272 mL 2.6359 mL 5.2718 mL 13.1794 mL
10 mM 0.2636 mL 1.3179 mL 2.6359 mL 6.5897 mL
15 mM 0.1757 mL 0.8786 mL 1.7573 mL 4.3931 mL
20 mM 0.1318 mL 0.6590 mL 1.3179 mL 3.2948 mL
25 mM 0.1054 mL 0.5272 mL 1.0544 mL 2.6359 mL
30 mM 0.0879 mL 0.4393 mL 0.8786 mL 2.1966 mL
40 mM 0.0659 mL 0.3295 mL 0.6590 mL 1.6474 mL
50 mM 0.0527 mL 0.2636 mL 0.5272 mL 1.3179 mL
60 mM 0.0439 mL 0.2197 mL 0.4393 mL 1.0983 mL
80 mM 0.0329 mL 0.1647 mL 0.3295 mL 0.8237 mL
100 mM 0.0264 mL 0.1318 mL 0.2636 mL 0.6590 mL
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JNJ-27141491 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.

Keywords:

JNJ-27141491871313-59-6JNJ27141491JNJ 27141491CCRCC chemokine receptororally activeMCP-1CHOmonocytesneutrophilsexperimental autoimmune encephalomyelitisInhibitorinhibitorinhibit

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