Description Biological activity Uses
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Tapinarof

Description Biological activity Uses
Product Name
Tapinarof
CAS No.
79338-84-4
Chemical Name
Tapinarof
Synonyms
Tapinarof;Bennvitimod;(E)-2-Isopropyl-5-styrylbenzene-1,3-diol;WB-1001;WBI-1001;Benvitimo;Benvitimod;GSK2894512);Tapinarof (WBI 1001;Tapinarof (Benvitimod
CBNumber
CB31119935
Molecular Formula
C17H18O2
Formula Weight
254.32
MOL File
79338-84-4.mol
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Tapinarof Property

Melting point:
140 - 142°C
Boiling point:
431.8±20.0 °C(Predicted)
Density 
1.158
storage temp. 
2-8°C
solubility 
Chloroform (Slightly), Methanol (Slightly)
pka
9.86±0.15(Predicted)
form 
Solid
color 
Pale Brown to Light Brown
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML3430
Product name
Benvitimod
Purity
≥98% (HPLC)
Packaging
10MG
Price
$79
Updated
2023/06/20
Sigma-Aldrich
Product number
SML3430
Product name
Benvitimod
Purity
≥98% (HPLC)
Packaging
50MG
Price
$255
Updated
2023/06/20
AK Scientific
Product number
8547CP
Product name
3,5-Dihydroxy-4-isopropylstilbene
Packaging
50mg
Price
$293
Updated
2021/12/16
ChemScene
Product number
CS-0031487
Product name
Tapinarof
Purity
99.74%
Packaging
10mg
Price
$350
Updated
2021/12/16
Biosynth Carbosynth
Product number
FD167852
Product name
Benvitimod
Packaging
250mg
Price
$400
Updated
2021/12/16
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Tapinarof Chemical Properties,Usage,Production

Description

Tapinarof is a small molecule stilbene compound, with a chemical name of 3,5-Dihydroxy-4-isopropylstilbene,which was originally isolated from the metabolite of photorhabdus iuminescence, a soil nematode (Heterorhabditis sp.), and has been synthesized artificially.

Biological activity

Tapinarof(GSK2894512) is a natural agonist of aryl hydrocarbon receptor (AhR) that induces nuclear translocation of AhR in immortalized keratinocytes (HaCaT) with EC50 of 0.16 nM. Benvitimod induces apoptosis in CD4+ T cells in a dose-dependent manner with an IC50 value of 5.2 μM.

Uses

Clinically, tapinarof was first used in the treatment of psoriasis and atopic dermatitis. Clinical trials conducted abroad have shown that Benzenemod cream has good efficacy and safety on atopic dermatitis and psoriasis. In China, as a class 1.1 new drug, Benzenemod cream has undergone phase I-II clinical trials, and the results show that it has good efficacy and safety for plaque psoriasis.

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.

References

[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 Preparation Products And Raw materials

Raw materials

Preparation Products

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Tapinarof Suppliers

Hangzhou LinghepharmTechnology Co.,Ltd.
Tel
+86-18571465433 18571465433
Email
sales@linghepharm.com
Country
China
ProdList
49
Advantage
58
Wuhan HSN Pharmaresearch CO., LTD.
Tel
027-63499089 18086100502
Fax
027-86589137
Email
linwell@126.com
Country
China
ProdList
208
Advantage
50
Hubei wei shi reagent group ltd., company
Tel
027-59105166 13125137732
Email
2853863890@qq.com
Country
China
ProdList
2981
Advantage
58
Suzhou Biosyntech Co., Ltd.
Tel
0512-63001269 15720870325
Email
sales2@biosyntech-suzhou.com
Country
China
ProdList
55
Advantage
58
Hubei Innerse Biotechnology Co., Ltd.
Tel
027-88189299 18186187538
Email
sales@innersebio.com
Country
China
ProdList
72
Advantage
58
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6005
Advantage
61
Beijing HwrkChemical Technology Co., Ltd
Tel
010-89508211 18501085097
Fax
010-89508210
Email
sales.bj@hwrkchemical.com
Country
China
ProdList
8418
Advantage
55
Adamas Reagent, Ltd.
Tel
400-6009262 16621234537
Fax
021-64823266
Email
chenyj@titansci.com
Country
China
ProdList
14103
Advantage
59
Nanjing Chemlin Chemical Co., Ltd
Tel
025-83697070
Fax
+86-25-83453306
Email
info@chemlin.com.cn
Country
China
ProdList
19172
Advantage
64
Chengdu Biopurify Phytochemicals Ltd.
Tel
+86-028-82633397 18982077548
Fax
+86-28-82633165
Email
cwb1@biopurify.cn
Country
China
ProdList
2376
Advantage
60
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View Lastest Price from Tapinarof manufacturers

Shaanxi Dideu Medichem Co. Ltd
Product
3,5-Dihydroxy-4-isopropylstilbene 79338-84-4
Price
US $1.00-1.00/KG
Min. Order
1g
Purity
99%
Supply Ability
50tons
Release date
2020-04-29
Zibo Hangyu Biotechnology Development Co., Ltd
Product
Benvitimod 79338-84-4
Price
US $40.00-319.00/mg
Min. Order
50mg
Purity
99.5%
Supply Ability
50
Release date
2024-07-09
Shandong Hanjiang Chemical Co., Ltd
Product
Benvitimod 79338-84-4
Price
US $0.00/KG
Min. Order
1KG
Purity
99.5%
Supply Ability
500kg
Release date
2024-05-10

79338-84-4, TapinarofRelated Search:


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  • Tapinarof
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  • 3,5-Dihydroxy-4-isopropylstilbene USP/EP/BP
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  • (E)- 3,5-Dihydroxy-4-isopropylstilbene
  • 79338-84-4