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Oclacitinib Maleate(PF-03394197)

Oclacitinib Maleate(PF-03394197) Struktur
1208319-27-0
CAS-Nr.
1208319-27-0
Englisch Name:
Oclacitinib Maleate(PF-03394197)
Synonyma:
Oclacitinib Maleate;N-methyl-1-((1r,4r)-4-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)cyclohexyl)methanesulfonamide Maleate;PF 03394197-11;olatinib maleate;Oclacitinib Meleate;Oclacitinib Maleate [VET];Oclacitinib Maleate(PF-03394197);Oclacitinib maleate (PF-03394197 maleate);Oclacitinib maleate Good Supplier In China;N-methyl-1-[4-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclohexyl]methanesulfonamide
CBNumber:
CB52730825
Summenformel:
C19H27N5O6S
Molgewicht:
453.51
MOL-Datei:
1208319-27-0.mol

Oclacitinib Maleate(PF-03394197) Eigenschaften

Schmelzpunkt:
135 - 137°C
storage temp. 
-20°C, Inert atmosphere
L?slichkeit
DMSO (Slightly), Methanol (Slightly, Sonicated)
Aggregatzustand
Solid
Farbe
White to Off-White
InChIKey
VQIGDTLRBSNOBV-VQIYXBGXNA-N
SMILES
C(/C(=O)O)=C/C(=O)O.N([C@@H]1CC[C@@H](CS(=O)(=O)NC)CC1)(C1N=CN=C2NC=CC=12)C |&1:9,12,r|

Sicherheit

Oclacitinib Maleate(PF-03394197) Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

APOQUEL (oclacitinib maleate) was the first selective Janus kinase (JAK) inhibitor to be developed for dogs. It was recently approved for the control of pruritus associated with allergic dermatitis and control of atopic dermatitis in dogs at least 12 months of age. In recent years, there has been a significant evolution in understanding regarding the pathophysiology of allergic and atopic diseases. The molecular mechanisms involved in stimulating the itch response have been elaborated (Marsella et al., 2012), and it is now understood that cytokines play a key role in initiating the neuronal itch stimulation which triggers pruritic behavior (scratching, rubbing, chewing, etc.) in dogs. This leads to the establishment of a vicious cycle of itch that exacerbates skin lesions and amplifies defects in the skin barrier function in clinically affected dogs. This progress provided the opportunity to develop new treatments (Marsella et al., 2012). Specifically, Janus kinases play a central role in cytokine signaling and are involved in signal transduction of many pro-inflammatory, pro-allergic, and pruritogenic cytokines including IL-2, IL-4, IL-6, IL-13, and IL-31 that are implicated in allergic conditions (Ong & Leung, 2006; Carmi-Levy et al., 2011).

Verwenden

Oclacitinib is labeled to treat atopic dermatitis and itchiness (pruritus) caused by allergies in dogs, though it has also been used to reduce the itchiness and dermatitis caused by flea infestations. It is considered to be highly effective in dogs, and has been established as safe for at least short-term use. Its efficacy equals that of prednisolone at first, though oclacitinib has been found to be more effective in the short term in terms of itchiness and dermatitis, long term safety is unknown. It has been found to have a faster onset and cause less gastrointestinal issues than cyclosporine. While safe in the short term, oclacitinib's long-term safety is unknown. While some say it is best only for acute flares of itchiness, others claim that it is also useful in chronic atopic dermatitis.

Pharmakokinetik

The pharmacokinetics of oclacitinib maleate was evaluated in four separate studies. The absolute bioavailability study used a crossover design with 10 dogs. The effect of food on bioavailability was investigated in a crossover study with 18 dogs. The breed effect on pharmacokinetics was assessed in a crossover study in beagles and mongrels dogs. Dose proportionality and multiple dose pharmacokinetics were evaluated in a parallel design study with eight dogs per group. In all four studies, serial blood samples for plasma were collected. Oclacitinib maleate was rapidly and well absorbed following oral administration, with a time to peak plasma concentration of<1 h and an absolute bioavailability of 89%. The prandial state of dogs did not significantly affect the rate or extent of absorption of oclacitinib maleate when dosed orally, as demonstrated by the lack of significant differences in pharmacokinetic parameters between the oral fasted and oral fed treatment groups. The pharmacokinetics of oclacitinib in laboratory populations of beagles and mixed breed dogs also appeared similar. Following oral administration, the exposure of oclacitinib maleate increased dose proportionally from 0.6 to 3.0 mg/kg. Additionally, across the pharmacokinetic studies, there were no apparent differences in oclacitinib pharmacokinetics attributable to sex

Nebenwirkungen

There are several caveats to the use of Oclacitinib maleate. This medication is meant to control the symptoms of itching. For many patients, ending itching also ends scratching and chewing. Ending scratching and chewing ends infections and a vicious cycle can finally be broken. The problem is that while oclacitinb maleate can control itching, it does may not control the disease that is causing the itching. If there is an infection present, it will continue to be present; it simply will not be itchy. It is important not to let skin disease persist simply because the dog is comfortable. The disease must be controlled as well. The oclacitinib maleate label contains a caution against use in patients with cancer. While oclacitinib maleate does not cause cancer, there is question about whether it can interfere with natural protective mechanisms that help control cancer. If a patient is known to have cancer or known to have an undefined growth on its body or if there is any reason to suspect a patient might be harboring cancer, it is important to discuss this caution with one's veterinarian before use of this medication. Oclacitinib maleate appears to promote or support Demodex skin mites. It should not be used to control itching associated with Demodectic Mange.

Oclacitinib Maleate(PF-03394197) Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


Oclacitinib Maleate(PF-03394197) Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 131)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
ENBRIDGE PHARMTECH CO., LTD.
+8613812269233
tinayang@enbridgepharm.com China 322 58
GIHI CHEMICALS CO.,LIMITED
+8618058761490
info@gihichemicals.com China 49978 58
XI'AN TIANGUANGYUAN BIOTECH CO., LTD.
+86-029-86333380 18829239519
sales06@tgybio.com China 901 58
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+undefined17712220823
admin@guyunchem.com China 615 58
Henan Fengda Chemical Co., Ltd
+86-371-86557731 +86-13613820652
info@fdachem.com China 20283 58
Shanghai Daken Advanced Materials Co.,Ltd
+86-371-66670886
info@dakenam.com China 18751 58
Henan Tianfu Chemical Co.,Ltd.
+86-0371-55170693 +86-19937530512
info@tianfuchem.com China 21634 55
Hangzhou FandaChem Co.,Ltd.
+8615858145714
FandaChem@Gmail.com China 8936 55
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795
ivan@atkchemical.com China 32956 60
TianYuan Pharmaceutical CO.,LTD
+86-755-23284190 13684996853
sales@tianpharm.com CHINA 304 58

  • Oclacitinib Maleate(PF-03394197)
  • PF 03394197-11
  • Oclacitinib Meleate
  • Oclacitinib maleate (PF-03394197 maleate)
  • N-methyl-1-[4-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclohexyl]methanesulfonamide
  • Oclacitinib Maleate [VET]
  • N-methyl-1-((1r,4r)-4-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)cyclohexyl)methanesulfonamide Maleate
  • Oclacitinib Maleate
  • N-methyl-1-(trans-4-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)cyclohexyl)methanesulfonamide maleate(1:x)
  • Oclacitinib maleate Good Supplier In China
  • olatinib maleate
  • 1208319-27-0
  • C15H23N5O2SxC4H4O4
  • C19H27N5O6S
  • API
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