| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| Other Sizes |
| Targets |
The primary target of Ropsacitinib is TYK2 (tyrosine kinase 2), a member of the JAK family of non-receptor tyrosine kinases. TYK2 is involved in cytokine signaling pathways, particularly those mediated by IL-12, IL-23, and type I interferons. By selectively inhibiting TYK2, Ropsacitinib modulates these immune pathways, making it a potential therapeutic for inflammatory diseases like psoriasis.
|
|---|---|
| ln Vitro |
In vitro, Ropsacitinib is a selective TYK2 inhibitor with an IC50 of 15-17 nM. It shows good selectivity over other JAK family members. Its activity is assessed by measuring TYK2 kinase activity in biochemical assays and by assessing downstream signaling (e.g., STAT phosphorylation) in cellular assays.
|
| ln Vivo |
In vivo, Ropsacitinib has been studied for its potential in treating inflammatory diseases, particularly psoriasis. It is currently being investigated in clinical studies. Its selectivity for TYK2 over other JAKs may offer a favorable safety profile by reducing off-target effects.
|
| Enzyme Assay |
For TYK2 kinase assays, the enzymatic activity of recombinant TYK2 is measured. The enzyme is incubated with varying concentrations of Ropsacitinib in a reaction buffer containing ATP and a peptide substrate. The reaction is monitored, and IC50 values are calculated. For selectivity, the compound is tested against JAK1, JAK2, and JAK3.
|
| Cell Assay |
For cellular studies, immune cells (e.g., PBMCs) are cultured in appropriate medium. Ropsacitinib is dissolved in DMSO and diluted in culture medium. Cells are stimulated with cytokines (e.g., IL-12, IL-23), and STAT phosphorylation is measured by Western blot or flow cytometry. Cytokine production is measured by ELISA.
|
| Animal Protocol |
For in vivo efficacy studies, animal models of psoriasis or other inflammatory diseases are used. Ropsacitinib is formulated in vehicle and administered orally. Disease severity is assessed by clinical scores, histopathology, and measurement of inflammatory markers. For pharmacokinetic studies, blood samples are collected for compound quantification.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for Ropsacitinib indicate that it is orally active. Its half-life, Cmax, and AUC have been characterized in preclinical and clinical studies. Its pharmacokinetic properties support once- or twice-daily dosing.
|
| Toxicity/Toxicokinetics |
Toxicological data for Ropsacitinib are being evaluated in clinical studies. As a TYK2 inhibitor, it is expected to have a manageable safety profile. Common adverse effects may include infections and other immune-related events. As with all drugs, appropriate safety precautions should be taken during handling.
|
| References |
|
| Additional Infomation |
Ropsacitinib (CAS 2127109-84-4) is a selective TYK2 inhibitor with an IC50 of 15-17 nM. It is selective over JAK1, JAK2, and JAK3. It has the molecular formula C₂₀H₁₇N₉ and a molecular weight of 383.40. It is being investigated for inflammatory diseases and is strictly for research use.
|
| Molecular Formula |
C₂₀H₁₇N₉
|
|---|---|
| Molecular Weight |
383.409281492233
|
| Exact Mass |
383.16
|
| CAS # |
2127109-84-4
|
| Related CAS # |
2127109-85-5 (cis-isomer);2127109-84-4;
|
| PubChem CID |
130339268
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.46±0.1 g/cm3(Predicted)
|
| LogP |
-0.4
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
29
|
| Complexity |
716
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
N1(C=C(C2C3=CC=NN3C=C(C3C=NN(C)C=3)N=2)C=N1)C1(CC#N)CC(C#N)C1
|
| InChi Key |
XPLZTJWZDBFWDE-OYOVHJISSA-N
|
| InChi Code |
InChI=1S/C20H17N9/c1-27-11-15(9-24-27)17-13-28-18(2-5-23-28)19(26-17)16-10-25-29(12-16)20(3-4-21)6-14(7-20)8-22/h2,5,9-14H,3,6-7H2,1H3/t14-,20-
|
| Chemical Name |
(1r,3r)-3-(cyanomethyl)-3-(4-(6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrazin-4-yl)-1H-pyrazol-1-yl)cyclobutane-1-carbonitrile
|
| Synonyms |
PF-06826647 Ropsacitinib PF6826647 Tyk2-IN-8PF 06826647 PF 6826647 Tyk2-IN 8PF06826647 PF-6826647 Tyk2-IN8
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6082 mL | 13.0409 mL | 26.0817 mL | |
| 5 mM | 0.5216 mL | 2.6082 mL | 5.2163 mL | |
| 10 mM | 0.2608 mL | 1.3041 mL | 2.6082 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
