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473727-83-2 (SCH 527123)

1

Identification

SCH 527123 SCH 527123
Name SCH 527123
Formula C21H23N3O5
MW 397.42
CAS No. 473727-83-2
EINECS
Smiles O=C1C(C(NC2=CC=CC(C(N(C)C)=O)=C2O)=C1N[[email protected]](CC)C3=CC=C(O3)C)=O
Synonyms SCH-527123;SCH527123; (R)-2-hydroxy-N,N-dimethyl-3-((2-((1-(5-methylfuran-2-yl)propyl)amino)-3,4-dioxocyclobut-1-en-1-yl)amino)benzamide
InChI InChI=1S/C21H23N3O5/c1-5-13(15-10-9-11(2)29-15)22-16-17(20(27)19(16)26)23-14-8-6-7-12(18(14)25)21(28)24(3)4/h6-10,13,22-23,25H,5H2,1-4H3/t13-/m1/s1
2

Introduction

SCH-527123 is a potent antagonist of both CXCR1 and CXCR2 with IC50 of 42 nM and 3 nM, respectively. IC50 value: 42 nM (CXCR1); 3 nM (CXCR2) [1] Target: CXCR1/2 in vitro: Sch527123 inhibits chemokine binding to CXCR1 and CXCR2 receptors in an insurmountable manner and is categorized as an allosteric antagonist.

Background Information

SCH527123 is a potent and selective antagonist of the human CXCR1 and CXCR2 receptors with IC50 of 42 nM and 3 nM, respectively. SCH-527123 bound with high affinity to the CXCR2 receptors of mouse (K(d) = 0.20 nM), rat (K(d) = 0.20 nM), and cynomolgus monkey (K(d) = 0.08 nM) and was a potent antagonist of CXCR2-mediated chemotaxis (IC(50) approximately 3-6 nM). In contrast, SCH527123 bound to cynomolgus CXCR1 with lesser affinity (K(d) = 41 nM) and weakly inhibited cynomolgus CXCR1-mediated chemotaxis (IC(50) approximately 1000 nM). Oral treatment with SCH527123 blocked pulmonary neutrophilia (ED(50) = 1.2 mg/kg) and goblet cell hyperplasia (32-38% inhibition at 1-3 mg/kg) in mice following the intranasal lipopolysaccharide (LPS) administration. SCH-527123 also suppressed the pulmonary neutrophilia (ED(50) = 1.3 mg/kg), goblet cell hyperplasia (ED(50) = 0.7 mg/kg), and increase in BAL mucin content (ED(50) = <1 mg/kg) in rats after i.t. administration of vanadium pentoxide. In vivo, SCH-527123 treatment decreased tumor growth and microvessel density when compared with vehicle-treated tumors. ......by AbMole BioScience
SCH527123 is a potent and selective antagonist of the human CXCR1 and CXCR2 receptors with IC50 of 42 nM and 3 nM, respectively. ......by AdooQ BioScience, LLC
Description ......by Apexbio Technology LLC
A potent antagonist of both CXCR1 and CXCR2 with IC50 of 42 nM and 3 nM, respectively. ......by BOC Sciences
SCH 527123 is a potent, allosteric antagonist of both CXCR1 and CXCR2, with IC50 values of 1000 nM and 3-6 nM, respectivelly. ......by MedChemexpress Co., Ltd.
Navarixin, also known as SCH527123, PS291822 and MK-7123, is a potent CXCR2 antagonist. SCH-527123 shows antitumor activity and sensitizes cells to oxaliplatin in preclinical colon cancer models. SCH-527123 showed concentration-dependent antiproliferative effects in HCT116, Caco2, and their respective IL-8-overexpressing variants colorectal cancer cell lines. CH-527123 was able to suppress CXCR2-mediated signal transduction as shown through decreased phosphorylation of the NF-κB/mitogen-activated protein kinase (MAPK)/AKT pathway. SCH-527123 treatment decreased tumor growth and microvessel density when compared with vehicle-treated tumors. ......by MedKoo Biosciences, Inc.
A potent, selective, orally bioavailable CXCR2/CXCR1 receptor antagonist with Kd of 0.08 and 41 nM for cynomolgus CXCR2 and CXCR1, respectively; potently inhibits CXCR2-mediated chemotaxis with IC50 of 3-6 nM; inhibits neutrophil recruitment, mucus production, and goblet cell hyperplasia in animal models of pulmonary inflammation.COPDPhase 2 Discontinued ......by ProbeChem
SCH-527123 is a novel antagonist of both CXCR1 and CXCR2 with IC50 of 42 nM and 3 nM, respectively. ......by Selleck Chemicals LLC
3

Protocol(Only for Reference)

Cell Experiment

Animal Experiment

4

Physical and Chemical Properties

Appearance:Light yellow to yellow solid EBNumber:EB000028557

Storage condition

Solubility

DMSO by MedChemexpress Co., Ltd.
DMSO mg/mL (<1 mM) ; Water mg/mL (<1 mM) ; Ethanol mg/mL (<1 mM) by Selleck Chemicals LLC
5

Mechanism and Indication

6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
SCH 527123 Merck & Co Inc Chronic obstructive pulmonary disease 2009/10/31 2011/11/30 Phase 2 Clinical
SCH 527123 Merck & Co Inc Asthma 2010/1/31 2012/8/31 Phase 2 Clinical
SCH 527123 Merck & Co Inc Asthma 2008/6/30 2009/2/28 Phase 2 Clinical
SCH 527123 Schering-Plough Corp Asthma 2008/5/31 2009/2/28 Phase 2 Clinical
SCH 527123 Merck & Co Inc Psoriasis 2007/6/30 2007/10/31 Phase 2 Clinical
SCH 527123 - Discontinued
SCH 527123 - Phase 2
7

Safety Data of SCH 527123

8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AbMole BioScience USA
AdooQ BioScience, LLC USA
Apexbio Technology LLC USA
Ark Pharm, Inc. USA
BOC Sciences
Biochempartner Co., Ltd China
CHEMSCENE, LLC 5mg/USD168();10mg/USD288() USA
MedChemexpress Co., Ltd. 5mg/USD168();10mg/USD288() USA
MedKoo Biosciences, Inc. USA
ProbeChem
Selleck Chemicals LLC USA
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD168();10mg/USD288() China
Shanghai XingMo Biotechnology Co., Ltd. 1g/USD1300(In stock) CHINA
Thompson Biological Technology Co., Ltd. China
10

Related Products

Other Forms of 473727-83-2

Name CAS No Formula MW

Recommended Compounds in CXCR

Name CAS No Formula MW
AMD 3465 185991-24-6 C24H38N6 410.6
AMD 3465 185991-24-6 C24H38N6 410.5987
AZD8797 911715-90-7 C19H25N5OS2 403.5647
Baohuoside I 113558-15-9 C27H30O10 514.52
AMD-070 hydrochloride C21H30Cl3N5 458.86
WZ811 55778-02-4 C18H18N4 290.36
SRT3109 1204707-71-0 C18H23F2N5O4S2 475.53
UNBS5162 956590-23-1 C17H18N4O3 326.3498
NBI-74330 855527-92-3 C32H27F4N5O3 605.58
AMG 487 473719-41-4 C32H28F3N5O4 603.59
Reparixin (L-lysine salt) 266359-93-7 C20H35N3O5S 429.57
Reparixin 266359-83-5 C14H21NO3S 283.39
SCH 546738 906805-42-3 C23H31Cl2N7O 492.44
SCH 563705 473728-58-4 C23H27N3O5 425.48
Plerixafor 110078-46-1 C28H54N8 502.78
AMD-070 558447-26-0 C21H27N5 349.47
Plerixafor (octahydrochloride) 155148-31-5 C28H62Cl8N8 794.47
SRT3190 1204707-73-2 C18H23F2N5O4S2 475.53
Nicotinamide N-oxide 1986-81-8 C6H6N2O2 138.12404
AZD-5069 878385-84-3 C18H22F2N4O5S2 476.52

Recommended Compounds in Same Indication

Name CAS No Formula MW
Carvedilol 72956-09-3 C24H26N2O4 406.47
PRX-08066 866206-54-4 C19H17ClFN5S 401.89
AN-2728 906673-24-3 C14H10BNO3 251.05
BMS-582949 623152-17-0 C22H26N6O2 406.48
Vilanterol 503068-34-6 C24H33Cl2NO5 486.43
Beclometasone dipropionate 5534-09-8 C28H37ClO7 521.04
PH-797804 586379-66-0 C22H19BrF2N2O3 477.3
Glycopyrrolate 596-51-0 C19H28BrNO3 398.33
Setipiprant 866460-33-5 C24H19FN2O3 402.42
Umeclidinium (bromide) 869113-09-7 C29H34BrNO2 508.49
Levalbuterol (tartrate) 661464-94-4 C30H48N2O12 628.71
Indacaterol 312753-06-3 C24H28N2O3 392.49
Aclidinium (Bromide) 320345-99-1 C26H30BrNO4S2 564.55
Sotrastaurin 425637-18-9 C25H22N6O2 438.48
OC000459 851723-84-7 C21H17FN2O2 348.37
Vilanterol (trifenatate) 503070-58-4 C44H49Cl2NO7 774.77
Apremilast 608141-41-9 C22H24N2O7S 460.5
Formoterol 67346-49-0 C19H24N2O4 344.40486
Sildenafil (citrate) 171599-83-0 C28H38N6O11S 666.7
Talarozole 201410-53-9 C21H23N5S 377.51
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Route of Synthesis

12

References

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More Information

SCH 527123

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