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Ropsacitinib

Product Name
Ropsacitinib
CAS No.
2127109-84-4
Chemical Name
Ropsacitinib
Synonyms
Tyk2-IN-8;PF6826647;PF 6826647;PF-6826647;PF-06826647;Ropsacitinib;PF-06826647( Tyk2-IN-8);Ropsacitinib (PF-06826647;Cyclobutaneacetonitrile, 3-cyano-1-[4-[6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrazin-4-yl]-1H-pyrazol-1-yl]-, trans-;cis-3-(Cyanomethyl)-3-{4-[6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrazin-4-yl]-1H-pyrazol-1-yl}cyclobutanecarbonitrile
CBNumber
CB04923831
Molecular Formula
C20H17N9
Formula Weight
383.41
MOL File
2127109-84-4.mol
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Ropsacitinib Property

Density 
1.46±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO: 16.67 mg/mL (43.48 mM)
pka
0.98±0.19(Predicted)
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H312Harmful in contact with skin

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

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

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

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N-Bromosuccinimide Price

ChemScene
Product number
CS-0101462
Product name
PF-06826647
Purity
99.82%
Packaging
5mg
Price
$550
Updated
2021/12/16
ChemScene
Product number
CS-0101462
Product name
PF-06826647
Purity
99.82%
Packaging
10mg
Price
$990
Updated
2021/12/16
ChemScene
Product number
CS-0101462
Product name
PF-06826647
Purity
99.82%
Packaging
50mg
Price
$2550
Updated
2021/12/16
Crysdot
Product number
CD31005026
Product name
PF-06826647
Purity
98%
Packaging
5mg
Price
$790
Updated
2021/12/16
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Ropsacitinib Chemical Properties,Usage,Production

Uses

trans-3-Cyano-1-[4-[6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrazin-4-yl]-1H-pyrazol-1-yl]cyclobutaneacetonitrile is a selective inhibitor of Tyrosine Kinase 2 (TYK2).

Biological Activity

The discovery of ropsacitinib, a dual JAK1/TYK2 inhibitor, was guided by previous research and molecular modeling on brepocitinib that revealed distinct hinge binding to the main chain atoms of Val981. ropsacitinib exhibited high JAK1 and JAK3 selectivity (>160-fold) and  modest JAK2 selectivity (12-fold).

Pharmacokinetics

Ropsacitinib is neutral at physiological pH with a pKa of < 1.7. The crystalline material showed very poor thermodynamic solubility (0.3 μg/mL at pH 7.4), and the lack of a basic group precluded salt formation to improve solubility. The solubility issue was mitigated through a spray-dried dispersion (SDD) formulation, which increased experimental intestinal solubility to approximately 160?180 μM (60?70 μg/mL). Ropsacitinib displayed high passive membrane permeability in MDCK-LE cells (mean Papp = 16.7 × 10?6 cm/s) but is a substrate for MDR1 (efflux ratio > 6) and BCRP (efflux ratio > 2) efflux transport. Following oral administration of the crystalline (non SDD) material to rats at 3 and 30 mpk, ropsacitinib showed an oral bioavailability of 15% and 8% respectively. The SDD formulation increased oral bioavailability to 58% and 63% at 3 and 30 mpk, respectively. The oral bioavailability in humans was expected to be dose-dependent due to poor solubility. In healthy volunteers, the terminal elimination half-life of ropsacitinib in a single ascending dose (SAD) study is also dose-dependent: for example, approximately 6 hours at 10 mg dose and 15 hours at 400 mg dose. Ropsacitinib underwent hepatic clearance in humans primarily through the CYP450-mediated (via CYP1A2, CYP2D6, and CYP3A) metabolism, resulting in N-demethylation of the pyrazole (6), hydroxylation of the pyrazole (5), and addition of oxygen (e.g., 4) and loss of the nitrile group (e.g., 7).

Ropsacitinib Preparation Products And Raw materials

Raw materials

Preparation Products

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Ropsacitinib Suppliers

Nanjing Chemlin Chemical Co., Ltd
Tel
025-83697070
Fax
+86-25-83453306
Email
info@chemlin.com.cn
Country
China
ProdList
19179
Advantage
64
Shanghai Topbiochem Technology Co., Ltd
Tel
021-58170097
Email
info@topbiochem.com
Country
China
ProdList
9458
Advantage
58
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185 18149758185
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
3466
Advantage
58
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696,15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4566
Advantage
55
Shanghai EFE Biological Technology Co., Ltd.
Tel
021-65675885 18964387627
Fax
021-65675885
Email
info@efebio.com
Country
China
ProdList
9806
Advantage
58
ShangHai Biochempartner Co.,Ltd
Tel
177-54423994 17754423994
Fax
QQ:2853530913
Email
2853530910@QQ.com
Country
China
ProdList
8012
Advantage
62
Shanghai Rechem science Co., Ltd.
Tel
21-31433387 15618786686
Fax
QQ:1369748377
Email
sales@rechemscience.com
Country
China
ProdList
2990
Advantage
58
Beijing Solarbio Science & Tecnology Co., Ltd.
Tel
010-50973130 4009686088
Email
3193328036@qq.com
Country
China
ProdList
29785
Advantage
68
Kaixin Chemical (Hong Kong) Limited
Tel
010-88886666-01 13112345678
Fax
CDXH21@126.com
Email
loyson@tcypharm.com
Country
China
ProdList
595
Advantage
55
Shanghai Scochem Technology Co., Ltd.
Tel
021-33758897
Email
sales@scochem.com
Country
China
ProdList
1596
Advantage
58
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View Lastest Price from Ropsacitinib manufacturers

Jinan Million Pharmaceutical Co., Ltd
Product
Ropsacitinib/PF-06826647 2127109-84-4
Price
US $2.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
1200KG/M
Release date
2023-08-11

2127109-84-4, RopsacitinibRelated Search:


  • (1r,3r)-3-(cyanomethyl)-3-(4-(6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrazin-4-yl)-1H-pyrazol-1-yl)cyclobutanecarbonitrile
  • PF-06826647
  • Tyk2-IN-8
  • Cyclobutaneacetonitrile, 3-cyano-1-[4-[6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrazin-4-yl]-1H-pyrazol-1-yl]-, trans-
  • PF-06826647( Tyk2-IN-8)
  • Ropsacitinib (PF-06826647
  • trans-3-(Cyanomethyl)-3-(4-(6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrazin-4-yl)-1H-pyrazol-1-yl)cyclobutanecarbonitrile
  • Ropsacitinib
  • cis-3-(Cyanomethyl)-3-{4-[6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrazin-4-yl]-1H-pyrazol-1-yl}cyclobutanecarbonitrile
  • PF 6826647
  • PF6826647
  • PF-6826647
  • 2127109-84-4