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Merck
CN

R1903

RS 102895 hydrochloride

≥98% (HPLC), powder

Synonym(s):

1′-[2-[4-(Trifluoromethyl)phenyl]ethyl]-spiro[4H-3,1-benzoxazine-4,4′-peperidin]-2(1H)-one

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About This Item

Empirical Formula (Hill Notation):
C21H21F3N2O2 · HCl
Molecular Weight:
426.86
NACRES:
NA.32
PubChem Substance ID:
24724588
UNSPSC Code:
12352202
MDL number:
MFCD08703093

Key Documents

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Product Name

RS 102895 hydrochloride, ≥98% (HPLC), powder

InChI key

KRRISOFSWVKYBF-UHFFFAOYSA-N

SMILES string

Cl.FC(F)(F)c1ccc(CCN2CCC3(CC2)OC(=O)Nc4ccccc34)cc1

InChI

1S/C21H21F3N2O2.ClH/c22-21(23,24)16-7-5-15(6-8-16)9-12-26-13-10-20(11-14-26)17-3-1-2-4-18(17)25-19(27)28-20;/h1-8H,9-14H2,(H,25,27);1H

assay

≥98% (HPLC)

form

powder

mol wt

426.86 g/mol

packaging

pkg of 5 mg

storage condition

desiccated

color

white

solubility

DMSO: >10 mg/mL

storage temp.

20-25°C

Quality Level

100

Application

RS 102895 hydrochloride has been used in bromodeoxyuridine (5-bromo-2′-deoxyuridine, BrdU) cell proliferation assay to study effect of IL33 (interleukin 33) on decidual stromal cell proliferation in present of the antagonist and to study the effects of antagonists on the accumulation of bone marrow-derived microglia.

Biochem/physiol Actions

RS 102895 hydrochloride has a high affinity to the β subunit of the C-C motif chemokine receptor 2 (CCR2) and binds specifically to it. This results in the inhibition of CCR2 signaling. It also suppresses monocyte recruitment. Hence, RS 102895 may be useful for obstructing the immune suppressive effects of monocytes during early vaccine responses.

General description

RS 102895 hydrochloride is a small molecule antagonist of C-C motif chemokine receptor 2 (CCR2) which belongs to the spiropiperidine (SP) class.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)

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Certificates of Analysis (COA)

Lot/Batch Number
0000463610
0000463610
0000224027
0000224027
0000150827

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Suppression of bone marrow-derived microglia in the amygdala improves anxiety-like behavior induced by chronic partial sciatic nerve ligation in mice.
Sawada A, Niiyama Y, Ataka K, et al.
Pain, 155(9), 1762-1772 (2014)
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.
Mirzadegan T
The Journal of Biological Chemistry, 275(33), 25562-25571 (2000)
Bone marrow-derived microglia infiltrate into the paraventricular nucleus of chronic psychological stress-loaded mice.
Ataka K
PLoS ONE, 8(11), e81744-e81744 (2013)
Optimized dosing of a CCR2 antagonist for amplification of vaccine immunity.
Mitchell LA
International Immunopharmacology, 15(2), 357-363 (2013)
IL-33 enhances proliferation and invasiveness of decidual stromal cells by up-regulation of CCL2/CCR2 via NF-?B and ERK1/2 signaling.
Hu WT
Molecular Human Reproduction, 20(4), 358-372 (2014)
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