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Cenicriviroc

Cenicriviroc Struktur
497223-25-3
CAS-Nr.
497223-25-3
Englisch Name:
Cenicriviroc
Synonyma:
TAK652;TBR652;TBR-652;CS-2572;TBR 652;Cenicriviroc;Cenicriviroc(TAK652);TAK-652 or Cenicriviroc;Cenicriviroc mesylate (TAK-652);TAK-652; TBR-652; TAK652; TBR652; TAK 652; TBR 652
CBNumber:
CB72627679
Summenformel:
C41H52N4O4S
Molgewicht:
696.94
MOL-Datei:
497223-25-3.mol

Cenicriviroc Eigenschaften

Siedepunkt:
913.5±65.0 °C(Predicted)
Dichte
1.17±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
L?slichkeit
DMF: 20 mg/ml; DMSO: 20 mg/ml; DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml; Ethanol: 5 mg/ml
Aggregatzustand
A crystalline solid
pka
12.96±0.70(Predicted)
Farbe
Light yellow to yellow
Sicherheit
  • Risiko- und Sicherheitserkl?rung
  • Gefahreninformationscode (GHS)
Bildanzeige (GHS) GHS hazard pictograms
Alarmwort Warnung
Gefahrenhinweise
Code Gefahrenhinweise Gefahrenklasse Abteilung Alarmwort Symbol P-Code
H302 Gesundheitssch?dlich bei Verschlucken. Akute Toxizit?t oral Kategorie 4 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P270, P301+P312, P330, P501
H315 Verursacht Hautreizungen. Hautreizung Kategorie 2 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P280, P302+P352, P321,P332+P313, P362
H319 Verursacht schwere Augenreizung. Schwere Augenreizung Kategorie 2 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P280, P305+P351+P338,P337+P313P
H335 Kann die Atemwege reizen. Spezifische Zielorgan-Toxizit?t (einmalige Exposition) Kategorie 3 (Atemwegsreizung) Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" />
Sicherheit
P261 Einatmen von Staub vermeiden.
P264 Nach Gebrauch gründlich waschen.
P264 Nach Gebrauch gründlich waschen.
P270 Bei Gebrauch nicht essen, trinken oder rauchen.
P271 Nur im Freien oder in gut belüfteten R?umen verwenden.
P280 Schutzhandschuhe/Schutzkleidung/Augenschutz tragen.
P301+P312 BEI VERSCHLUCKEN: Bei Unwohlsein GIFTINFORMATIONSZENTRUM/Arzt/... (geeignete Stelle für medizinische Notfallversorgung vom Hersteller/Lieferanten anzugeben) anrufen.
P302+P352 BEI BERüHRUNG MIT DER HAUT: Mit viel Wasser/... (Hersteller kann, falls zweckm??ig, ein Reinigungsmittel angeben oder, wenn Wasser eindeutig ungeeignet ist, ein alternatives Mittel empfehlen) waschen.
P304+P340 BEI EINATMEN: Die Person an die frische Luft bringen und für ungehinderte Atmung sorgen.
P305+P351+P338 BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach M?glichkeit entfernen. Weiter spülen.
P321 Besondere Behandlung
P330 Mund ausspülen.
P332+P313 Bei Hautreizung: ?rztlichen Rat einholen/?rztliche Hilfe hinzuziehen.

Cenicriviroc Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

Cenicriviroc is a dual antagonist of chemokine receptor types 2 and 5 (CCR2/CCR5). The receptors are found on Kupffer cells and hepatic stellate cells, and preclinical studies suggest its anti-inflammatory and anti-fibrotic activity. In the phase 2b CENTAUR study, cenicriviroc treatment for 1 year failed to achieve the primary outcome of a decrease in NAFLD activity score by ≥2 points with no worsening of fibrosis. Nonetheless, one of the key secondary outcomes, improvement in liver fibrosis without worsening of NASH, was achieved in 20% in the treatment group, compared with 10% in the placebo group. Besides, cenicriviroc reduced the serum levels interleukin- 6, C-reactive protein and fibrinogen, suggesting its action on inflammation that may not be reflected by crude histological assessment. A phase 3 study is planned.

Verwenden

Cenicriviroc is an experimental drug candidate for the treatment of HIV infection. It is an inhibitor of CCR2 and CCR5 receptors, allowing it to function as an entry inhibitor which prevents the virus from entering into a human cell.

Clinical Use

Cenicriviroc is a small molecule inhibitor of both CCR2 and CCR5, and has demonstrated safety in early trials of human patients afflicted with HIV-1, as well as a phase IIb trial (ClinicalTrials.gov NCT01338883). Cenicriviroc has also demonstrated therapeutic potential in animal models of liver fibrosis as well as renal fibrosis. A phase II trial of cenicriviroc in patients with NASH and liver fibrosis is planned to complete in late 2017 and (ClinicalTrials.gov NCT02217475). This trial, also called “CENTAUR: Efficacy and Safety Study of Cenicriviroc for the Treatment of Nonalcoholic Steatohepatitis (NASH) in Adult Subjects With Liver Fibrosis,” is a double-blind, placebo-controlled, randomized multinational study with the primary endpoint being histologic improvement of NASH activity score without worsening of fibrosis in patients with NASH and liver fibrosis. Results of this study are pending. An open label rollover extension study of participants in CENTAUR began in early 2017 and is ongoing (ClinicalTrials. gov NCT03059446).
There is evidence that CCRs are important in fibrosis in the liver, lung and kidney. At least one molecule that inhibits CCRs has demonstrable safety in human subjects. As such, blockade of CCRs with molecules such as Cenicriviroc represent another potential therapeutic avenue for the treatment of fibrotic inflammatory bowel disease.

Cenicriviroc Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


Cenicriviroc Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 85)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795
ivan@atkchemical.com China 32820 60
BOC Sciences
+1-631-485-4226
inquiry@bocsci.com United States 19553 58
Career Henan Chemica Co
+86-0371-86658258 +8613203830695
laboratory@coreychem.com China 30241 58
Chemia Biotechnology(Shanghai) Co., Ltd
+8613816753574
info@chemia-pharm.com CHINA 311 58
Alfa Chemistry

Info@alfa-chemistry.com United States 24072 58
Hangzhou Proserre Chemical Co.,Ltd.
+86-571-86088112
info@proserre.com China 1077 58
InvivoChem
+1-708-310-1919 +1-13798911105
sales@invivochem.cn United States 6391 58
TargetMol Chemicals Inc.

support@targetmol.com United States 38460 58
Zibo Hangyu Biotechnology Development Co., Ltd
+86-0533-2185556 +8617865335152
Mandy@hangyubiotech.com China 10986 58
LEAPCHEM CO., LTD.
+86-852-30606658
market18@leapchem.com China 43340 58

  • Cenicriviroc
  • TAK652
  • Cenicriviroc mesylate (TAK-652)
  • Cenicriviroc(TAK652)
  • TAK-652; TAK652; TAK 652; TBR-652; TBR 652; TBR652; CENICRIVIROC.
  • CS-2572
  • TAK-652; TBR-652; TAK652; TBR652; TAK 652; TBR 652
  • TBR 652
  • TBR652
  • TBR-652
  • 1-Benzazocine-5-carboxamide, 8-[4-(2-butoxyethoxy)phenyl]-1,2,3,4-tetrahydro-1-(2-methylpropyl)-N-[4-[(S)-[(1-propyl-1H-imidazol-5-yl)methyl]sulfinyl]phenyl]-
  • (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
  • TAK-652 or Cenicriviroc
  • (S)-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
  • 497223-25-3
  • C41H52N4O4S
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