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

China 45 United States 3 Global 48

TargetMol Chemicals Inc.

Tel: +1-781-999-5354 +1-00000000000
Email: marketing@targetmol.com
Country: United States
ProdList: 32161
Advantage: 58

TargetMol Chemicals Inc.

Tel
Email: support@targetmol.com
Country: United States
ProdList: 38631
Advantage: 58

Aladdin Scientific

Tel: +1-+1(833)-552-7181
Email: sales@aladdinsci.com
Country: United States
ProdList: 52924
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