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RS102895 hydrochloride

Cat. No. M7218
RS102895 hydrochloride Structure
Synonym:

RS 102895 HCl

Size Price Availability Quantity
10mg USD 100  USD100 In stock
25mg USD 210  USD210 In stock
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Quality Control & Documentation
Biological Activity

RS102895 hydrochloride is a cCR2-selective chemokine receptor antagonist (IC50 values are 0.36 and 17.8 μM for inhibition of human recombinant CCR2b and CCR1 receptors respectively). RS102895 hydrochloride blocks MCP-1-stimulated calcium influx and chemotaxis with IC50 values of 32 nM and 1.7 μM respectively. RS102895 hydrochloride also inhibits α1A, α1D and 5-HT1A receptors.

Chemical Information
Molecular Weight 426.86
Formula C21H21F3N2O2.HCl
CAS Number 1173022-16-6
Solubility (25°C) DMSO 30 mg/mL (ultrasonic and warming)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Fei Ren, et al. Cell Biochem Biophys. Analgesic Effect of Intrathecal Administration of Chemokine Receptor CCR2 Antagonist is Related to Change in Spinal NR2B, nNOS, and SIGIRR Expression in Rat with Bone Cancer Pain

[2] T Mirzadegan, et al. J Biol Chem. Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists: binding to a common chemokine receptor motif within the helical bundle

[3] Russell, et al. Nature. A simple cytochemical technique for demonstration of DNA in cells infected with mycoplasmas and viruses.

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