LGD-4033

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 危険有害性情報

  H302：飲み込むと有害

  H315：皮膚刺激

  H319：強い眼刺激

  H335：呼吸器への刺激のおそれ

• 注意書き

  P261：粉じん/煙/ガス/ミスト/蒸気/スプレーの吸入を避ける こと。

  P264：取扱い後は皮膚をよく洗うこと。

  P264：取扱い後は手や顔をよく洗うこと。

  P270：この製品を使用する時に、飲食または喫煙をしないこ と。

  P271：屋外または換気の良い場所でのみ使用すること。

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。

  P301+P312：飲み込んだ場合：気分が悪い時は医師に連絡する こと。

  P302+P352：皮膚に付着した場合：多量の水と石鹸で洗うこと。

  P304+P340：吸入した場合：空気の新鮮な場所に移し、呼吸しやすい 姿勢で休息させること。

  P305+P351+P338：眼に入った場合：水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。

  P321：特別な処置が必要である（このラベルの．．． を見よ）。

  P330：口をすすぐこと。

  P332+P313：皮膚刺激が生じた場合：医師の診断/手当てを受けるこ と。

  P337+P313：眼の刺激が続く場合：医師の診断/手当てを受けること。

  P403+P233：換気の良い場所で保管すること。容器を密閉 しておくこと。

  P405：施錠して保管すること。

  P501：内容物/容器を．．．に廃棄すること。

LGD-4033 化学特性,用途語,生産方法

• 説明

  LGD-4033 is a Selective Androgen Receptor Modulator (SARM). SARMs are a class of non-steroidal anabolic agents that bind androgen receptors with high affinity. LGD-4033 has been shown to provide benefits similar to traditional anabolic agents, (e.g., increased muscle mass, fat loss, and improved bone density) but with far fewer side effects (e.g., oily skin, acne, over-conversion to estrogen, etc.). Both men and women may also appreciate improved libido. All of these benefits are achieved without increasing androgen levels. Its anabolic effects are roughly the same or greater than testosterone, even at low doses. Some prescribers will recommend a trial of SARMs for low testosterone levels prior to utilizing testosterone replacement therapy.

• 使用

  Ligandrol, also known as LGD-4033, is a nonsteroidal oral drug used for the treatment of muscle wasting and osteoporosis in healthy young men.

• 生物活性

  LGD-4033 is a potent nonsteroidal selective androgen receptor modulator (SARM) that binds to the androgen receptor with a Ki value of 1 nM. In animal models, LGD-4033 displays robust selectivity for muscle versus prostate tissues, anabolic activity in the muscle, and anti-resorptive and anabolic activity in bone.
  LGD 4033 has been abused as a performance-enhancing drug and the identification of its in vitro metabolites has been described.
  This product is intended for research and forensic applications.

• 作用機序

  LGD-4033 works by binding to androgen receptors in muscle and bone tissue and stimulating protein synthesis, thus helping to build muscle and strength, increase bone density, reduce inflammation, and promote tissue healing. In addition, it can also help improve body composition by reducing fat mass while preserving lean muscle mass.

• 副作用

  When taken in appropriate doses, most people experience minimal side effects, if any at all. Some users may experience mild headaches, nausea, or lightheadedness, but these are generally mild and go away quickly.

• 合成

  11.20 g Aldehyde (4-(2-(formylpyrrolidin-1-yl)-2-(trifluoromethyl)benzonitril )was dissolved in 300 ml dry tetrahydrofuran and 8.36 g CsF was added directly as a solid to the reaction mixture. It was cooled via ice bath to 0°C and stirred for 15 min. Then 25.00 g trimethyl(trifluoromethyl)silane was added via syringe over a period of 40 min. The reaction is stirred for 15 h coming from 0°C to room temperature over this time interval. The reaction solution shifts color from nearly colorless to dark brown. For stopping the reaction, it was diluted with 100 ml saturated ammonium chloride solution and then evaporated. The resulting emulsion was extracted several times with ethyl acetate and the combined phases dried over magnesium sulfate. After evaporation of all volatiles, the intermediate silyl-ether can be obtained as red-brown oil. This intermediate was converted to the final product LGD-4033 without any further purification. The intermediate was diluted with 400 ml tetrahydrofuran and cooled to 0°C. A cooled potassium hydroxide solution (4.76 g in 400 ml water) was mixed with the diluted oil and stirred at 0°C for 2h. After quenching with 300 ml water, the organic solvent was removed via evaporation from the mixture. The remaining brown oil was extracted with dichloromethane and dried over magnesium sulfate, to yield a reddish-brown oil. This crude product was chromatographed on silica gel by using hexane-ethyl acetat (8:2) as an eluent. During purification, different fractions with several product isomers can be collected . The isolated products LGD-4033 were obtained as 8.50 g yellowish oils (61%).

• 参考文献

  The Safety, Pharmacokinetics, and Effects of LGD-4033, a Novel Nonsteroidal Oral, Selective Androgen Receptor Modulator, in Healthy Young Men
  In vitro metabolism study of a black market product containing SARM LGD-4033
  Characterization of a non-approved selective androgen receptor modulator drug candidate sold via the Internet and identification of in vitro generated phase-I metabolites for human sports drug testing

LGD-4033 上流と下流の製品情報

LGD-4033 生産企業

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1165910-22-4, LGD-4033 キーワード