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Cenicriviroc

Product Name
Cenicriviroc
CAS No.
497223-25-3
Chemical Name
Cenicriviroc
Synonyms
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
Molecular Formula
C41H52N4O4S
Formula Weight
696.94
MOL File
497223-25-3.mol
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Cenicriviroc Property

Boiling point:
913.5±65.0 °C(Predicted)
Density 
1.17±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMF: 20 mg/ml; DMSO: 20 mg/ml; DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml; Ethanol: 5 mg/ml
form 
A crystalline solid
pka
12.96±0.70(Predicted)
color 
Light yellow to yellow
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical
Product number
23927
Product name
Cenicriviroc
Purity
≥95%
Packaging
500μg
Price
$60
Updated
2024/03/01
Cayman Chemical
Product number
23927
Product name
Cenicriviroc
Purity
≥95%
Packaging
1mg
Price
$93
Updated
2024/03/01
Cayman Chemical
Product number
23927
Product name
Cenicriviroc
Purity
≥95%
Packaging
5mg
Price
$344
Updated
2024/03/01
Cayman Chemical
Product number
23927
Product name
Cenicriviroc
Purity
≥95%
Packaging
10mg
Price
$628
Updated
2024/03/01
TRC
Product number
C256550
Product name
Cenicriviroc
Packaging
100mg
Price
$20790
Updated
2021/12/16
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Cenicriviroc Chemical Properties,Usage,Production

Description

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.

Uses

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.

Definition

ChEBI: Cenicriviroc is a member of the class of benzazocines that is (5Z)-1,2,3,4-tetrahydro-1-benzazocine which is substituted by a 2-methylpropyl, N-{4-[(S)-(1-propyl-1H-imidazol-5-yl)methanesulfinyl]phenyl}carboxamide and 4-(2-butoxyethoxy)phenyl groups at positions 1, 5 and 8, respectively. It is a potent chemokine 2 and 5 receptor antagonist currently in development for the treatment of liver fibrosis in adults with nonalcoholic steatohepatitis (NASH). It has a role as a chemokine receptor 5 antagonist, an anti-HIV agent, a chemokine receptor 2 antagonist, an antirheumatic drug and an anti-inflammatory agent. It is a diether, a member of imidazoles, a sulfoxide, an aromatic ether, a secondary carboxamide and a benzazocine.

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 Preparation Products And Raw materials

Raw materials

Preparation Products

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Cenicriviroc Suppliers

J & K SCIENTIFIC LTD.
Tel
010-82848833 400-666-7788
Fax
86-10-82849933
Email
jkinfo@jkchemical.com
Country
China
ProdList
96815
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76
ChengDu TongChuangYuan Pharmaceutical Co.Ltd
Tel
28-83379370 13880556291
Fax
028-87747383
Email
tcy@tcypharm.com
Country
China
ProdList
510
Advantage
57
WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd.
Tel
17702719238 17702719238
Email
sales@sun-shinechem.com
Country
China
ProdList
985
Advantage
64
QINGDAO CARELONGPHARMATECH CO.,LTD
Tel
0532-0532-88191853 13061484198
Email
sales@carelongchem.com
Country
China
ProdList
413
Advantage
57
BOC Sciences
Tel
1-631-485-4226; 16314854226
Email
info@bocsci.com
Country
United States
ProdList
14055
Advantage
65
MedChemexpress LLC
Tel
021-58955995
Fax
609-228-5909
Email
sales@medchemexpress.cn
Country
United States
ProdList
4861
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58
AdooQ BioScience, LLC
Tel
+1 (866) 930-6790
Fax
+1 (866) 333-9607
Email
info@adooq.com
Country
United States
ProdList
2782
Advantage
58
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185 18149758185
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
3466
Advantage
58
AdooQ Bioscience CHINA
Tel
025-58849295 18951903616;
Fax
025-68650336
Email
info@adooq.cn
Country
China
ProdList
2990
Advantage
60
Cool Pharm, Ltd
Tel
021-58581007 18019463053
Fax
50966098
Email
sales@coolpharm.com
Country
China
ProdList
12346
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58

497223-25-3, CenicrivirocRelated Search:


  • 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
  • (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 , Cenicriviroc
  • 497223-25-3
  • C41H52N4O4S