Deuruxolitinib
Based on 1 Customer Validation
Deuruxolitinib, a deuterated Ruxolitinib (HY-50856), is an orally active JAK1 and JAK2 inhibitor. Deuruxolitinib demonstrates significant hair regrowth effects. Deuruxolitinib can be used for the research of alopecia areata.
For research use only. We do not sell to patients.
- Purity: 99.18%
- CAS No.: 1513883-39-0
- Formula: C17H10D8N6
- Molecular Weight:314.41
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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JAK1 |
JAK2 |
"Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[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 drug 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 drug metabolism.
(4) Improve drug safety. Deuterated compounds may reduce or eliminate adverse side effects of pharmaceutical 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.
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MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
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. 1513883-39-0
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Unlabeled Cas 941678-49-5
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Appearance Solid
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Molecular Weight 314.41
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Formula C17H10D8N6
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Color White to off-white
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SMILES
N#CC[C@@H](N1N=CC(C2=C3C(NC=C3)=NC=N2)=C1)C4C([2H])(C([2H])(C([2H])(C4([2H])[2H])[2H])[2H])[2H]
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Synonyms
CTP-543; Ruxolitinib d8; Deuterated Ruxolitinib
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 116.67 mg/mL (371.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Brett King, et al. Efficacy and safety of deuruxolitinib, an oral selective Janus kinase inhibitor, in adults with alopecia areata: Results from the Phase 3 randomized, controlled trial (THRIVE-AA1). J Am Acad Dermatol. 2024 Nov;91(5):880-888. [Content Brief]
[2]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 3.1806 mL | 15.9028 mL | 31.8056 mL | 79.5140 mL |
| 5 mM | 0.6361 mL | 3.1806 mL | 6.3611 mL | 15.9028 mL | |
| 10 mM | 0.3181 mL | 1.5903 mL | 3.1806 mL | 7.9514 mL | |
| 15 mM | 0.2120 mL | 1.0602 mL | 2.1204 mL | 5.3009 mL | |
| 20 mM | 0.1590 mL | 0.7951 mL | 1.5903 mL | 3.9757 mL | |
| 25 mM | 0.1272 mL | 0.6361 mL | 1.2722 mL | 3.1806 mL | |
| 30 mM | 0.1060 mL | 0.5301 mL | 1.0602 mL | 2.6505 mL | |
| 40 mM | 0.0795 mL | 0.3976 mL | 0.7951 mL | 1.9879 mL | |
| 50 mM | 0.0636 mL | 0.3181 mL | 0.6361 mL | 1.5903 mL | |
| 60 mM | 0.0530 mL | 0.2650 mL | 0.5301 mL | 1.3252 mL | |
| 80 mM | 0.0398 mL | 0.1988 mL | 0.3976 mL | 0.9939 mL | |
| 100 mM | 0.0318 mL | 0.1590 mL | 0.3181 mL | 0.7951 mL |
Deuruxolitinib Related Classifications
HY-50856S Related Classifications
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