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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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R335959-1mg | 1mg | In stock | $20.90 | |
R335959-5mg | 5mg | In stock | $77.90 | |
R335959-10mg | 10mg | In stock | $118.90 | |
R335959-25mg | 25mg | In stock | $267.90 | |
R335959-50mg | 50mg | In stock | $470.90 | |
R335959-100mg | 100mg | In stock | $846.90 |
a CCR2-selective chemokine receptor antagonist
Synonyms | RS 102895 hydrochloride|1173022-16-6|300815-41-2|RS-102895 Hydrochloride|RS102895 hydrochloride|RS102895 (hydrochloride)|MFCD08703093|1'-[2-[4-(trifluoromethyl)phenyl]ethyl]spiro[1H-3,1-benzoxazine-4,4'-piperidine]-2-one;hydrochloride|Spiro[4H-3,1-benzoxa |
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Specifications & Purity | Moligand™, ≥98% |
Storage Temp | Store at 2-8°C,Desiccated |
Shipped In | Wet ice |
Grade | Moligand™ |
Action Type | ANTAGONIST |
Mechanism of action | Antagonist of CCR2 |
Product Description | RS 102895 Hydrochloride is a CKR-2B (CCR2)-selective chemokine receptor antagonist (IC|50|values are 0.36 and 17.8 μM for inhibition of human recombinant CKR-2B and CKR-1 (CCR2b and CCR1 receptors) respectively). Blocks MCP-1-stimulated calcium influx and chemotaxis with IC|50|values of 32 nM and 1.7 μM respectively. Inhibits α|1A|-AR, α|1D|-AR and SR-1A (α1A, α1D and 5-HT|1A|receptors). |
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IUPAC Name | 1'-[2-[4-(trifluoromethyl)phenyl]ethyl]spiro[1H-3,1-benzoxazine-4,4'-piperidine]-2-one;hydrochloride |
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INCHI | 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 |
InChi Key | KRRISOFSWVKYBF-UHFFFAOYSA-N |
Canonical SMILES | C1CN(CCC12C3=CC=CC=C3NC(=O)O2)CCC4=CC=C(C=C4)C(F)(F)F.Cl |
Isomeric SMILES | C1CN(CCC12C3=CC=CC=C3NC(=O)O2)CCC4=CC=C(C=C4)C(F)(F)F.Cl |
WGK Germany | 3 |
PubChem CID | 16759153 |
Molecular Weight | 390.40 |
PubChem CID | 10000456 |
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CAS Registry No. | 300815-41-2 |
ChEMBL Ligand | CHEMBL1593104 |
RCSB PDB Ligand | R6Q |
GPCRdb Ligand | RS-102895 |
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Lot Number | Certificate Type | Date | Item |
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F2309922 | Certificate of Analysis | May 10, 2023 | R335959 |
F2310469 | Certificate of Analysis | May 10, 2023 | R335959 |
F2310473 | Certificate of Analysis | May 10, 2023 | R335959 |
F2310475 | Certificate of Analysis | May 10, 2023 | R335959 |
F2310477 | Certificate of Analysis | May 10, 2023 | R335959 |
F2310479 | Certificate of Analysis | May 10, 2023 | R335959 |
F2310481 | Certificate of Analysis | May 10, 2023 | R335959 |
F2310485 | Certificate of Analysis | May 10, 2023 | R335959 |
F2310486 | Certificate of Analysis | May 10, 2023 | R335959 |
F2310488 | Certificate of Analysis | May 10, 2023 | R335959 |
F2310493 | Certificate of Analysis | May 10, 2023 | R335959 |
F2310495 | Certificate of Analysis | May 10, 2023 | R335959 |
Solubility | Soluble in DMSO (75 mM). |
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Sensitivity | Moisture sensitive |
Refractive Index | n20D~1.59 (Predicted) |
WGK Germany | 3 |
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Starting at $241.90
Starting at $241.90
Starting at $79.90
1. Mirzadegan T, Diehl F, Ebi B, Bhakta S, Polsky I, McCarley D, Mulkins M, Weatherhead GS, Lapierre JM, Dankwardt J et al.. (2000) 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.. J Biol Chem, 275 (33): (25562-71). [PMID:10770925] |
2. Clark RD, Caroon JM, Kluge AF, Repke DB, Roszkowski AP, Strosberg AM, Baker S, Bitter SM, Okada MD. (1983) Synthesis and antihypertensive activity of 4'-substituted spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-ones.. J Med Chem, 26 (5): (657-61). [PMID:6842505] |