1. GPCR/G Protein
    Immunology/Inflammation
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  3. R243

R243 

Cat. No.: HY-122219 Purity: 98.90%
Handling Instructions

R243 is a potent and selective CCR8 antagonist. R243 inhibits CCL1/CCR8 interaction and inhibits CCR8 signaling and chemotaxis. R243 has antinociceptive and anti-inflammatory effects.

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

R243 Chemical Structure

R243 Chemical Structure

CAS No. : 688352-84-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 99 In-stock
Estimated Time of Arrival: December 31
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
25 mg USD 280 In-stock
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 750 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

R243 is a potent and selective CCR8 antagonist. R243 inhibits CCL1/CCR8 interaction and inhibits CCR8 signaling and chemotaxis. R243 has antinociceptive and anti-inflammatory effects[1][2].

IC50 & Target[1]

CCR8

 

In Vitro

R243 has CCR8-antagonistic effects on CCL1-induced Ca2+ flux and CCL1-driven peritoneal macrophages aggregation[1].
R243 attenuates secretion of TNF-α, IL-6, and most strikingly IL-10 from wild-type peritoneal macrophages (WT PMφ)[1].
R243-treated WT PMφ shows suppressed c-jun N-terminal kinase activity and NF-κB signaling after lipopolysaccharide (LPS) treatment when compared with WT PMφ[1].

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

In Vivo

R243 (0.1-1 mg/kg; intraperitoneal injection; once; male Swiss mice) treatment inhibits the analgesic effect evoked by CCL1 in a dose-dependent manner[2].

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

Animal Model: Male Swiss mice (7-9 weeks old) injected with CCL1[2]
Dosage: 0.1 mg/kg, 0.3mg/kg, 1 mg/kg
Administration: Intraperitoneal injection; once
Result: The analgesic effect evoked by CCL1 (10 μg/kg; 1 h; s.c.) was dose-dependently inhibited.
Molecular Weight

357.44

Formula

C₂₁H₂₇NO₄

CAS No.

688352-84-3

SMILES

[[email protected]@H]12CC(C[[email protected]](C3)C1)(C[[email protected]@H]3C2)OCCN4CC(C=C(OCO5)C5=C6)=C6OC4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (349.71 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7977 mL 13.9884 mL 27.9767 mL
5 mM 0.5595 mL 2.7977 mL 5.5953 mL
10 mM 0.2798 mL 1.3988 mL 2.7977 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.82 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.82 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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  • Molarity Calculator

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Keywords:

R243R 243R-243CCRCC chemokine receptorInhibitorinhibitorinhibit

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Product Name:
R243
Cat. No.:
HY-122219
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