Tapinarof

Bezeichnung:Tapinarof

CAS-Nr79338-84-4

Englisch Name:Tapinarof

CBNumberCB31119935

SummenformelC17H18O2

Molgewicht254.32

MOL-Datei79338-84-4.mol

Tapinarof physikalisch-chemischer Eigenschaften

Schmelzpunkt	140 - 142°C
Siedepunkt	431.8±20.0 °C(Predicted)
Dichte	1.158
storage temp.	2-8°C
Löslichkeit	Chloroform (Slightly), Methanol (Slightly)
pka	9.86±0.15(Predicted)
Aggregatzustand	Solid
Farbe	Pale Brown to Light Brown

Gefahreninformationscode (GHS)

Tapinarof Chemische Eigenschaften,Einsatz,Produktion Methoden

Clinical Use
Tapinarof is a novel small molecule topical therapeutic AhR ( aryl hydrocarbon receptor)-modulating agent that has been recently approved by the FDA for the topical treatment of plaque psoriasis in adults. Tapinarof 1% cream has shown to be effective and to have a favorable safety profile in the treatment of psoriatic patients[1]. It could decrease the expression of multiple essential cytokines involved in the pathological IL-23/IL-17/IL-22 axis and ameliorate IMQ-induced psoriatic dermatitis, inhibiting keratinocyte proliferation and abnormal differentiation. But tapinarof may have different effects on varied types of psoriasis[2]. Tapinarof can also specifically bind to and activate AHR leading to downregulation of TNF-α/IL-23/IL-17 and inhibition of IL-4/IL-13 mediated STAT6 activation, to achieve the purpose of treating nonulcerated necrobiosis lipoidica[3].
in vivo
Tapinarof acts through AhR to reduce inflammation in IMQ-treated mice. AhR-sufficient mice on a C57Bl/6 background exhibit a reduced clinical score after treatment with Tapinarof or 6-formylindolo(3,2-b)carbazole (FICZ). In contrast, AhR KO mice do not respond to the anti-inflammatory effects of Tapinarof. FICZ is used as a comparator in these studies and yields similar results, with dramatically reduced inflammatory responses in wild-type, but not AhR KO mice.
Einzelnachweise
[1] Bissonnette R, et al. Tapinarof for psoriasis and atopic dermatitis: 15?years of clinical research. Journal of the European Academy of Dermatology and Venereology, 2023; 37: 1168-1174.
[2] Zhu X, et al. The opposite effect of tapinarof between IMQ and IL-23 induced psoriasis mouse models. Experimental Dermatology, 2023.
[3] Palomares S, et al. Nonulcerated Necrobiosis Lipoidica Successfully Treated with Tapinarof: A Case Report. Clinical, Cosmetic and Investigational Dermatology, 2023; 16: 1373-1376.

Tapinarof Upstream-Materialien And Downstream Produkte

Tapinarof Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

79338-84-4, Tapinarof Verwandte Suche:

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