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ピメチルクロリムス(ELIエリデル

ピメチルクロリムス(ELIエリデル 化学構造式
137071-32-0
CAS番号.
137071-32-0
化学名:
ピメチルクロリムス(ELIエリデル
别名:
ピメチルクロリムス(ELIエリデル;ピメチルクロリムス;ピメクロリムス;ピメクロリムス (JAN)
英語化学名:
Pimecrolimus
英語别名:
Elidel;CS-1835;ASM 981;Picrolimus;SDZ-ASM 981;Pimecrolimus;Unii-7kyv510875;PiMecroliMus(Elidel);Pimecrolimus (SDZ-ASM 981);PiMecroliMus(Elidel, SDZ-ASM-981)
CBNumber:
CB71086808
化学式:
C43H68ClNO11
分子量:
810.459
MOL File:
137071-32-0.mol

ピメチルクロリムス(ELIエリデル 物理性質

融点 :
135-136 °C
沸点 :
866.1±75.0 °C(Predicted)
比重(密度) :
1.19
貯蔵温度 :
-20°C Freezer
酸解離定数(Pka):
9.97±0.70(Predicted)

安全性情報

ピメチルクロリムス(ELIエリデル 価格 もっと(10)

メーカー 製品番号 製品説明 CAS番号 包装 価格 更新時間 購入
富士フイルム和光純薬株式会社(wako) W01BVI1593-25
Pimecrolimus
137071-32-0 25mg ¥72300 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01BVI1593-5
Pimecrolimus
137071-32-0 5mg ¥33800 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01LKTP3348 ピメチルクロリムス
Pimecrolimus
137071-32-0 25mg ¥45900 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01COBQJ-4456 ピメチルクロリムス
Pimecrolimus
137071-32-0 100mg ¥270000 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01COBQJ-4456 ピメチルクロリムス
Pimecrolimus
137071-32-0 500mg ¥806400 2018-12-26 購入

ピメチルクロリムス(ELIエリデル 化学特性,用途語,生産方法

効能

免疫抑制薬, カルシニューリン阻害薬

説明

Pimecrolimus is an ascomycin macrolactam derivative, developed as a topical formulation (1% cream) for the treatment of mild to moderate atopic dermatitis for patients aged two years and over in whom the use of conventional therapies is inadvisable. Pimecrolimus is an inflammatory cytokine inhibitor that works by selectively targeting T-cells in the skin. It inhibits in vitro the production and release of pro-inflammatory cytokines after antigen-specific or non-specific stimulation in T cells and mast cells. Pimecrolimus binds specifically to cytosolic receptor macrophilin-12 at nanomolar concentrations leading to inhibition of the Ca2+/calmodulin-dependent phosphatase, calcineurin. Pimecrolimus is a chlorine derivative of the known FK-520, from which it can be synthesized. In a pig model of dinitrofluorobenzene-induced allergic contact dermatitis, pimecrolimus was shown to inhibit erythema and induration, had equivalent efficacy compared to clobetasol-17- propionate, but did not cause atrophogenic effects. In a mouse model of allergic contact dermatitis, pimecrolimus given orally was as potent as tacrolimus and more effective than cyclosporin. The agent also decreased the intensity of cutaneous manifestations in an atopic dermatitis model involving hypomagnesemic hairless mice. Both in adults and in pediatric patients with atopic dermatitis, treatment with pimecrolimus has demonstrated greater efficiency than conventional treatment in reducing the incidence of disease flares, as well as the use of second-line corticosteroids. Moreover, in a 26 week study, in pediatric patients (2-17 years), from 65% of subjects showing improvement, 85% were cleared of the disease. Oral pimecrolimus administration resulted in an elimination half-life of about 30 to 40 h. It is not metabolized or degraded during skin permeation after topical administration. However, following oral administration, it is metabolized via the liver CYP3A4 pathway and excreted mainly in the feces. Pimecrolimus is well tolerated; no systemic accumulation is seen and the most commonly reported side effect is reaction at the site of application. Moreover, pimecrolimus did not cause skin atrophy in contrast to corticosteroids. At this time, as a replacement therapy for topical corticosteroids, the only competing agent for pimecrolimus is topical tacrolimus (ointment). Preliminary studies demonstrated comparable efficacy and safety between these two agents.

化学的特性

White Solid

Originator

Novartis (USA)

使用

Pimecrolimus is a semi-synthetic, macrocyclic lactone derived from ascomycin by activation of the 32-hydroxy group with a triflate ester, and nucleophilic substitution with chloride under phase transfer conditions to provide the chloro analogue. Pimecrolimus has been targeted for treatment of inflammatory skin disorders. Like all tacrolimus analogues, pimecrolimus binds to receptor protein, FKBP12. The complex then binds to mTOR preventing it from interacting with target proteins. Pimecrolimus is extensively cited in the literature with over 2,000 citations.

使用

Macrolactam ascomycin derivative; inhibits production of pro-inflammatory cytokines by T cells and mast cells. Immunosuppresant

使用

Pimecrolimus caused a strong and dose-dependent inhibition of anti-IgE–induced release of histamine from mast cells and basophils (maximally 73% and 82%, respectively, at 500 nmol/L pimecrolimus) and of mast cell tryptase (maximally 75%) and a less pronou

適応症

Pimecrolimus (SDZ ASM 981, Elidel) is another recently approved macrolide immunosuppressant that acts by inhibiting calcineurin and blocking the release of proinflammatory cytokines from T lymphocytes. The parent compound, ascomycin, was originally isolated from Streptomyces hygroscopicus var ascomyceticus. Like tacrolimus, pimecrolimus is approved for the topical treatment of moderate to severe atopic dermatitis that is refractory to other therapies.Transient local irritation is a common side effect.

brand name

Elidel (Novartis);Elide1.

Veterinary Drugs and Treatments

A relatively new addition to the human topical armamentarium, pimecrolimus cream may be of benefit in veterinary patients in the adjunctive treatment of atopic dermatitis, discoid lupus erythematosus, pemphigus erythematosus or foliaceous, pinnal vascular disease, alopecia areata, vitiligo and for perianal fistulas (terminal phase or maintenance treatment after cyclosporine therapy). Unlike topical corticosteroids, tacrolimus or pimecrolimus do not have atrophogenic or metabolic effects associated with long-term or large area treatment.
Pimecrolimus acts similarly as cyclosporine and tacrolimus, namely inhibiting T-lymphocyte activation primarily by inhibiting the phosphatase activity of calcineurin. It also inhibits the release of inflammatory cytokines and mediators from mast cells and basophils. Pimecrolimus may not have identical mechanisms of action as tacrolimus, as it did not impair the primary immune response (as did tacrolimus) in mice after a contact sensitizer was applied. Both drugs did impair the secondary response however. Any clinical significance associated with this difference is not yet clear.

ピメチルクロリムス(ELIエリデル 上流と下流の製品情報

原材料

準備製品


ピメチルクロリムス(ELIエリデル 生産企業

Global( 191)Suppliers
名前 電話番号 ファックス番号 電子メール 国籍 製品カタログ 優位度
ENBRIDGE PHARMTECH CO., LTD.
13812269233
0510-83591909 sales@enbridgepharm.com CHINA 133 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22626 55
Shanghai Yingrui Biopharma Co., Ltd.
+86-21-33585366 E-mail:sales03@shyrchem.com
+86-21-34979012 sales03@shyrchem.com CHINA 739 60
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 24723 60
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 30045 58
Shanghai Arbor Chemical Co., Ltd.
021-60451682
021-60451683 act@arborchemical.com CHINA 906 58
TianYuan Pharmaceutical CO.,LTD
+86-755-23284190 13684996853
+86-755-23284190 sales@tianpharm.com CHINA 305 58
Hubei Jusheng Technology Co.,Ltd.
86-18871470254
027-59599243 linda@hubeijusheng.com CHINA 28234 58
Casorganics US Corp
+17326109938
sales@casorganics.com CHINA 175 58
QUALITY CONTROL CHEMICALS INC.
(323) 306-3136
(626) 453-0409 orders@qcchemical.com United States 8406 58

137071-32-0(ピメチルクロリムス(ELIエリデル)キーワード:


  • 137071-32-0
  • CS-1835
  • Picrolimus
  • ASM 981
  • Elidel
  • SDZ-ASM 981
  • Pimecrolimus
  • 15,19-Epoxy-3H-pyrido(2,1-C)(1,4)oxaazacyclotricosine-1,7,20,21(4H,23H)-tetrone, 3-((1E)-2-((1R,3R,4S)-4-chloro-3-methoxycyclohexyl)-1-methylethenyl)-8-ethyl-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26A-hexadecahydro-5,19-dihydroxy-14,16-dimethoxy-4,10,12,18-tetramethyl-, (3S,4R,5S,8R,9E,12S,14S,15R,16S,18R,19R,26as)-
  • 15,19-Epoxy-3H-pyrido(2,1-C)(1,4)oxaazacyclotricosine-1,7,20,21(4H,23H)-tetrone, 3-(2-(4-chloro-3-methoxycyclohexyl)-1-methylethenyl)-8-ethyl-, 5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26A-hexadecahydro-5,19-dihydroxy-14,16-dimethoxy-4,10,12,18-tetramethyl-, (3S-(3R*(E(1S*,3S*,4R*)),4S*,5R*,8S*,9E,12R*,14R*,15S*,16R*,18S*,19S*,26ar*))-
  • Unii-7kyv510875
  • PiMecroliMus(Elidel, SDZ-ASM-981)
  • PiMecroliMus(Elidel)
  • (9E)-3S-[(1E)-2-[(1R,3R,4S)-4R-chloro-3-methoxycyclohexyl]-1-methylethenyl]-8-ethyl-5S,6,8R,11,12S,13,14S,15R,16S,17,18R,19R,24,25,26,26aS-hexadecahydro-5,19-dihydroxy-14,16-dimethoxy-4,10,12,18-tetramethyl-15,19
  • Pimecrolimus (SDZ-ASM 981)
  • 15,19-Epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclotricosine-1,7,20,21(4H,23H)-tetrone, 3-[(1E)-2-[(1R,3R,4S)-4-chloro-3-methoxycyclohexyl]-1-methylethenyl]-8-ethyl-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-5,19-dihydroxy-1
  • ピメチルクロリムス(ELIエリデル
  • ピメチルクロリムス
  • ピメクロリムス
  • ピメクロリムス (JAN)
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