Deuruxolitinib phosphate
Deuruxolitinib phosphate (CTP-543 phosphate; Ruxolitinib-d8 phosphate) is a deuterated analog of Ruxolitinib (HY-50856) and an orally active, selective inhibitor of JAK1 and JAK2. Deuruxolitinib phosphate blocks Janus kinase-mediated cytokine receptor signaling and proinflammatory cytokine gene expression. Deuruxolitinib phosphate is primarily metabolized in the liver via CYP2C9. Deuruxolitinib phosphate promotes scalp hair regrowth in severe chronic alopecia areata. Deuruxolitinib phosphate is used in alopecia areata-related research.
For research use only. We do not sell to patients.
- CAS No.: 2147706-60-1
- Formula: C17H13D8N6O4P
- Molecular Weight:412.41
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
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JAK1 |
JAK2 |
Tyk2 |
In Vitro
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into candidate compounds, largely as tracers for quantitation during the development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of candidate compounds[2].
Potential advantages of deuterated compounds:
(1) Extend the half-life in vivo. Deuterated compounds may be able to prolong the pharmacokinetic characteristics of the compound, that is, prolong the half-life in vivo. This can improve compound safety, efficacy and tolerability, and increase ease of administration.
(2) Improve oral bioavailability. Deuterated compounds may reduce the degree of unwanted metabolism (first-pass metabolism) in the gut wall and liver, allowing a greater proportion of the unmetabolized candidate compound to reach its target site of action. High bioavailability determines its activity at low doses and better tolerance.
(3) Improve metabolic characteristics. Deuterated compounds may reduce the formation of toxic or reactive metabolites and improve compound metabolism.
(4) Improve compound safety. Deuterated compounds may reduce or eliminate adverse side effects of candidate compounds and are safe.
(5) Preserve the therapeutic properties. Deuterated compounds are expected to retain similar biochemical potency and selectivity to hydrogen analogs in previous studies.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Application
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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CAS No. 2147706-60-1
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Molecular Weight 412.41
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Formula C17H13D8N6O4P
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SMILES
O=P(O)(O)O.N#CC[C@H](C1C([2H])([2H])C([2H])([2H])C([2H])([2H])C1([2H])[2H])N2C=C(C=N2)C3=C4C(NC=C4)=NC=N3
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Synonyms
CTP-543 phosphate; Ruxolitinib-d8 phosphate; INCB18424-d8 (phospha
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)