Home > Products > Novel inhibitors

Cenicriviroc

  Cat. No.:  DC10316   Featured
Chemical Structure
497223-25-3
For research use only. We do not sell to patients.
We match the best price and quality on market.
Email:order@dcchemicals.com  sales@dcchemicals.com
Tel:+86-021-58447131
Get Quotation Now
We are official vendor of:
  • 20
  • 19
  • 18
  • 17
  • 16
  • 15
  • 14
  • 12
  • 11
  • 10
  • 9
  • 8
  • 13
  • 6
  • 5
  • 4
  • 3
  • 2
  • 1
More than 5000 active chemicals with high quality for research!
Field of application
Cenicriviroc is an orally active, dual CCR2/CCR5 antagonist, and displays potent anti-inflammatory and aninfective activity.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 497223-25-3
Chemical Name: (S,E)-8-(4-(2-Butoxyethoxy)phenyl)-1-isobutyl-N-(4-(((1-propyl-1H-imidazol-5-yl)methyl)sulfinyl)phenyl)-1,2,3,4-tetrahydrobenzo[b]azocine-5-carboxamide
Synonyms: TAK-652; TAK652; TAK 652; TBR-652; TBR 652; TBR652; Cenicriviroc.
SMILES: O=C(/C1=C/C2=CC(C3=CC=C(OCCOCCCC)C=C3)=CC=C2N(CC(C)C)CCC1)NC4=CC=C([S@](CC5=CN=CN5CCC)=O)C=C4
Formula: C41H52N4O4S
M.Wt: 696.95
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [1]. Lefebvre E, et al. Antifibrotic Effects of the Dual CCR2/CCR5 Antagonist Cenicriviroc in Animal Models of Liver and Kidney Fibrosis. PLoS One. 2016 Jun 27;11(6):e0158156 [2]. Kuwata T, et al. Incompatible Natures of the HIV-1 Envelope in Resistance
Description: Cenicriviroc is an orally active, dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2, and displays potent anti-inflammatory and antiinfective activity.
In Vivo: Cenicriviroc (≥20 mg/kg/day) significantly reduces monocyte/macrophage recruitment in vivo. At these doses, cenicriviroc shows antifibrotic effects, with significant reductions in collagen deposition, and collagen type 1 protein and mRNA expression across the three animal models of fibrosis. In the NASH model, cenicriviroc significantly reduces the non-alcoholic fatty liver disease activity score. Cenicriviroc treatment has no notable effect on body or liver/kidney weight[1].
In Vitro: Cenicriviroc prevents human immunodeficiency virus type 1 (HIV-1) from cellular entry[2]. Regarding the 4 R5 HIV-2 clinical isolates tested, effective concentration 50% EC50 for cenicriviroc are 0.03, 0.33, 0.45 and 0.98 nM. The dual-tropic and the X4-tropic HIV-2 strains are resistant to cenicriviroc with EC50 at >1000 nM, and MPI at 33% and 4%, respectively[3].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC31074 Isopropyl myristate Isopropyl myristate is the ester of isopropyl alcohol and myristic acid.
DC75202 Fosaprepitant free acid Fosaprepitant, also known as MK0517, is an antiemetic drug, administered intravenously. It is a prodrug of aprepitant. Fosaprepitant was developed by Merck & Co. and was approved. It is a prodrug of Aprepitant. It aids in the prevention of acute and delayed nausea and vomiting associated with chemotherapy treatment. Fosaprepitant is a weak inhibitor of CYP3A4, and aprepitant, the active moiety, is a substrate, inhibitor, and inducer of CYP3A4
DC74557 PREX-in1 PREX-in1 is a specific small-molecule inhibitor of P-Rex1 and P-Rex2 Rac-GEF activity with IC50 of 4.5 uM (P-Rex1 DHPH Rac-GEF activity) in liposome-based GEF assay, inhibits P-Rex1 and P-Rex2 through their catalytic DH domain.
DC74555 GYS32661 GYS32661 (GYS 32661) is a potent Rac inhibitor capable of inhibiting both Rac1 and Rac1b, inhibited activated Rac1 with IC50 of 1.18 uM in in vitro pull-down assays.
DC74540 MTX-3937 MTX-3937 is a small-molecule inhibitor targeting Siglec-9 (Sialic acid-binding immunoglobulin-type lectin-9), a member of the Siglec family of immunomodulatory receptors. Siglec-9 is primarily expressed on immune cells, such as myeloid cells and natural killer (NK) cells, and plays a role in regulating immune responses by transmitting inhibitory signals through its intracellular immunoreceptor tyrosine-based inhibitory motifs (ITIMs).
DC74539 L557-0155 L557-0155 is a small molecule inhibitor of VSIG-8, prevents VSIG-8 binding to VISTA, promotes cytokine production and cell proliferation in PBMCs and suppresses melanoma growth.
DC74528 K284 K284 is a selective small molecule inhibitor of chitinase 3 like1 (CHI3L1) with strong binding affinity (Kd=-9.7 kcal·mol-1), inhibits lung metastasis by blocking IL-13Rα2-mediated JNK-AP-1 signals.
DC74225 YB-537 YB-537 (YB537) is a potent, highly specific quinone reductase 2 (QR2) inhibitor with IC50 of 3 nM, shows no activity against QR1 (IC50>10 uM).
DC74224 XST-20 XST-20 is a small molecule that selectively targets the DNA-binding domain (DBD) of FOXM1, atranscription factor involved in cell cycle progression, proliferation, and cancer development. Witha surface plasmon resonance (SPR)-derived binding affinity (Kd) of 20 uM, XST-20 effectivelysuppresses FOXM1's transcriptional activities, making it a promising candidate for targetingFOXM1-driven cancers, such as ovarian cancer.
DC74223 X-Neu5Ac X-Neu5Ac (sodium) is a substrate for chromogenic assay of neuraminidase activity in bacterial expression systems; with a Km of 0.89 mM for neuraminidase.
X
Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.
Site Map|Privacy PolicyCopyright © 2018-2020 All Rights Reserved. Technical Support:KuuJia