[CAS NO. 1640292-55-2] Oclacitinib maleate
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PRODUCTS SPECIFICATIONS [1640292-55-2]
Store
Catalog
SLK-S8195
Brand
Selleck
CAS
1640292-55-2
DESCRIPTION [1640292-55-2]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 453.51 |
| Molecular Formula | C15H23N5O2S.C4H4O4 |
| SMILES | O=S(C[C@H]1CC[C@H](N(C)C2=C3C(NC=C3)=NC=N2)CC1)(NC)=O.O=C(O)/C=C/C(O)=O |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2050 mL | 11.0251 mL | 22.0502 mL |
| 5 mM | 0.4410 mL | 2.2050 mL | 4.4100 mL |
| 10 mM | 0.2205 mL | 1.1025 mL | 2.2050 mL |
| 50 mM | 0.0441 mL | 0.2205 mL | 0.4410 mL |
Description
Oclacitinib maleate (PF-03394197) is a novel inhibitor of family members with ranging from 10 to 99 nM and JAK1-dependent cytokines with ranging from 36 to 249 nM. It does not inhibit a panel of 38 non-JAK kinases.
Targets
In vitro
PF-03394197 inhibits JAK family members by 50% at concentrations ranging from 10 to 99 nM and does not inhibit a panel of 38 non-JAK kinases. PF-03394197 is most potent at inhibiting JAK1. PF-03394197 also inhibits the function of JAK1-dependent cytokines involved in allergy and inflammation as well as pruritus. PF-03394197 has minimal effects on cytokines which does not activate the JAK1 enzyme in cells.
In vivo
PF-03394197 administered orally at a dose of 0.4–0.6 mg/kg twice daily is safe and efficacious in controlling the pruritus associated with allergic dermatitis. PF-03394197 provides itch relief within 24 h that persistes through the treatment period, with over 70% of the treated dogs achieving a >50% reduction in pruritus by day 7.
References
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