PF-03394197(Oclacitinib)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
PF-03394197(Oclacitinib)对JAK1的IC50值为10 nM.
Janus激酶(JAK)参与过敏失调细胞因子激活的细胞信号传导途径.PF-03394197(Oclacitinib)是一种新型的Janus激酶抑制剂.
体外:PF-03394197在10 ~ 99 nM浓度范围下抑制50% JAK家族成员,但不抑制38种非JAK激酶.PF-03394197最有效地抑制JAK1.PF-03394197也抑制参与过敏\炎症以及瘙痒的JAK1依赖性细胞因子的功能.PF-03394197对细胞中不激活JAK1酶的细胞因子的影响最小[1].
体内:口服给予0.4 ~ 0.6 mg/kg PF-03394197,每天2次,安全有效地控制过敏性皮炎相关瘙痒.在治疗期间的持续24小时内,PF-03394197缓解瘙痒.于第7天,在70%以上接受治疗的狗中,其瘙痒症状得以缓解[2].
临床试验:PF-03394197(Oclacitinib)(APOQUEL)于近日获美国与欧盟批准用于控制或治疗过敏性皮炎相关瘙痒以及控制或治疗犬AD[1].
参考文献：
[1] Gonzales AJ, Bowman JW, Fici GJ, Zhang M, Mann DW, Mitton-Fry M. Oclacitinib (APOQUEL()) is a novel Janus kinase inhibitor with activity against cytokines involved in allergy. J Vet Pharmacol Ther. 2014 Aug;37(4):317-24.
[2] Cosgrove SB, Wren JA, Cleaver DM, Martin DD, Walsh KF, Harfst JA, Follis SL, King VL, Boucher JF, Stegemann MR. Efficacy and safety of oclacitinib for the control of pruritus and associated skin lesions in dogs with canine allergic dermatitis. Vet Dermatol. 2013 Oct;24(5):479-e114.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 337.44 |
| Cas No. | 1208319-26-9 |
| Formula | C15H23N5O2S |
| Solubility | ≥33.7 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
| Chemical Name | N-methyl-1-((1r,4r)-4-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)cyclohexyl)methanesulfonamide |
| SDF | Download SDF |
| Canonical SMILES | CNS(C[C@@]1([H])CC[C@@](N(C2=NC=NC3=C2C=CN3)C)([H])CC1)(=O)=O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
质量控制和MSDS
- 批次:
化学结构
