MSI-1436 (Trodusquemine) (Synonyms: Trodusquemine; Aminosterol-1436)

Name: MSI-1436 (Trodusquemine)
Brand: GlpBio
SKU: GC32396
Availability: InStock
Rating: 5 (12 reviews)

カタログ番号GC32396

MSI-1436 (Trodusquemine) は、選択的かつ非競合的なタンパク質チロシンホスファターゼ1B（PTP1B）酵素の阻害剤である。

Products are for research use only. Not for human use. We do not sell to patients.

MSI-1436 (Trodusquemine) 化学構造

Cas No.: 186139-09-3

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価格

在庫数

個数

1mg	$459.00	在庫あり
5mg	$873.00	在庫あり
10mg	$1,471.00	在庫あり
50mg	$4,597.00	在庫あり

Tel：(909) 407-4943 Email: sales@glpbio.com

顧客レビュー

カスタマーレビューに基づきます。

Sample solution is provided at 25 µL, 10mM.

Product has been cited by 1 publications

Front Immunol 13 (2022): 1053856.PMID:36618415

Description Protocol Chemical Properties Quality Control Product Documents

Related Biological Data

PTP1B, immune infiltration and CSCs index in cancers. (F) The cell inhibition rate of MSI-1436 (a PTP1B inhibitor) in different cancer cell lines with different doses. (G) Sensitivity effect of MSI-1436 and PD1 inhibitor (tislelizumab) in AML patient samples.
After incubating 48 h, the cytotoxicity of MSI-1436 (GLPBIO) was measured by adding 10μL cell counting kit-8 (CCK-8) at 450 nm.
Front Immunol 13 (2022): 1053856. PMID: 36618415 IF: 7.3

Product Documents

Quality Control & SDS

View current batch:

Purity: >95.00%

Protocol

Kinase experiment [1]:
Preparation Method	Human kinases activities were measured using KINOMEscan. In brief, 256 DNA-tagged kinases, ligand affinity beads, and MSI-1436 (Trodusquemine)(10 µmol/l) were incubated at room temperature, washed, and then eluted. Phage titer in the eluates was quantitated by real-time quantitative PCR.
Reaction Conditions	10 µmol/l MSI-1436 (Trodusquemine)
Applications	Enzyme inhibition assay showed that MSI-1436 (Trodusquemine) inhibited PTP1B 200 times more in a dose-dependent manner than TCPTP (IC 50 = 1 umol/l vs. 224 umol/l).
Cell experiment [2]:
Cell lines	HepG2 cell line
Preparation Method	Hep G2 cells were pretreated with 10 µmol/l MSI-1436 (Trodusquemine) or sodium orthovanadate for 10 min at 37°C then incubated with 10 mmol/l pNPP for 30 min at 37 °C Samples of the supernatants were spectrophotometrically analyzed at OD405 for hydolyzed pNP, a direct end product of phosphatase activity.
Reaction Conditions	10 µmol/l MSI-1436 (Trodusquemine) for 10 min at 37°C
Applications	Quantification of phosphatase activity measured in intact cell assays Incubation of intact HepG2 cells with 10 umol/l MSI-1436 (Trodusquemine) resulted in a 53% inhibition of phosphatase activity compared with control (no inhibitor).
Animal experiment [3]:
Animal models	Male AKR/J mice
Preparation Method	Male AKR/J mice were randomly placed on ad libitum 10, 45, or 60% fat kcal diets.After 14 weeks, mice were randomly assigned to three treatment groups; MSI-1436 (Trodusquemine), vehicle, or pair-fed. PF animals were injected with saline and allotted the amount of food consumed daily by trodusquemine-treated animals.
Dosage form	MSI-1436 (Trodusquemine)(initial dose of 10 mg/kg followed by intraperitoneal injection of 5 mg/kg 3 times weekly) for 23 days
Applications	MSI-1436 (Trodusquemine)-treated animals demonstrated weight loss in a manner proportional to their pretreatment weights; heavier mice lost a greater overall percentage of BW.
References: [1].Lantz KA, Hart SG, et,al.Inhibition of PTP1B by trodusquemine (MSI-1436) causes fat-specific weight loss in diet-induced obese mice. Obesity (Silver Spring). 2010 Aug;18(8):1516-23. doi: 10.1038/oby.2009.444. Epub 2010 Jan 14. PMID: 20075852.

MSI-1436 (Trodusquemine) は、選択的かつ非競合的なタンパク質チロシンホスファターゼ1B（PTP1B）酵素の阻害剤である。MSI-1436のIC50は約1 µMであり、TCPTP（IC50、224 µM）よりも200倍高い選択性を持つ。さらに、抗菌活性も持っている。

10µMのMSI-1436（トロドスクエミン）でHepG2細胞をインキュベートすると、対照（阻害剤なし）と比較してホスファターゼ活性が53%抑制された。MSI-1436（トロドスクエミン）は、「ファーストインクラス」の非常に選択的なPTP1B阻害剤であり、血液脳関門を通過して摂食を抑制し、培養神経細胞においてインスリン感受性および血糖コントロールを促進する。馬のASC EMS細胞におけるPTP1Bの選択的阻害により、細胞増殖を促進し、C/EBPαおよびPPARγの発現を正常化することで脂肪細胞分化が大幅に改善された。MSI-1436（トロドスクエミン）条件下の細胞では、分泌されたアディポネクチンとPPARγのレベルが増加し、同じ条件下で総レプチンレベルが著しく低下した。

MSI-1436（トロドスクエミン）は迅速に作用し、初回投与後に顕著な体重減少を引き起こする。安全で効果的な抗肥満療法の前提条件は、筋肉量を減少させずに脂肪を減少させることである。トロドスクエミンで処理されたマウスは、全身のタンパク質含量に減少は見られなかったが、精巣上体脂肪パッドが小さくなり、白色および褐色脂肪組織の脂肪細胞面積が減少し、全身の脂肪組成が大幅に減少した。MSI-1436（トロドスクエミン）による脂肪特異的な非カヘキシア性体重減少は、初期体重に依存した体重減少率の説明になる。MSI-1436（トロドスクエミン）の単回注射はラットの摂食量を減少させた。DAT機能に対するMSI-1436（トロドスクエミン）の効果を評価するために、迅速サイクリックボルタメトリーを使用して腹側線条体におけるDA濃度の変化を測定した。生理食塩水もMSI-1436（トロドスクエミン）も誘発された放出の大きさに有意な変化を引き起こさなかったのに対し、ブプロピオンは有意な増加を引き起こした。MSI-1436（トロドスクエミン）は、DATを温存する抗肥満治療法として評価されている。MSI-1436（トロドスクエミン）はHER2シグナル伝達を拮抗し、異種移植モデルでの腫瘍形成を抑制し、NDL2マウスモデルの乳がんにおいて転移を阻止した。これは、乳がん治療におけるPTP1Bの阻害が有効な戦略であることを裏付ける。PTP1B阻害剤MSI-1436（トロドスクエミン）はPTP1B活性を正常化し、mGluR5機能を回復させ、LMO4ノックアウトマウスの不安表現型を軽減する。

References:
[1]: Lantz KA, Hart SG, et,al. Inhibition of PTP1B by trodusquemine (MSI-1436) causes fat-specific weight loss in diet-induced obese mice. Obesity (Silver Spring). 2010 Aug;18(8):1516-23. doi: 10.1038/oby.2009.444. Epub 2010 Jan 14. PMID: 20075852.
[2]: Qin Z, Pandey NR, et,al. Functional properties of Claramine: a novel PTP1B inhibitor and insulin-mimetic compound. Biochem Biophys Res Commun. 2015 Feb 27;458(1):21-7. doi: 10.1016/j.bbrc.2015.01.040. Epub 2015 Jan 24. PMID: 25623533.
[3]: Qin Z, Zhou X, et,al. Chronic stress induces anxiety via an amygdalar intracellular cascade that impairs endocannabinoid signaling. Neuron. 2015 Mar 18;85(6):1319-31. doi: 10.1016/j.neuron.2015.02.015. Epub 2015 Mar 5. PMID: 25754825.
[4]: Bourebaba L, Kornicka-Garbowska K, et,al.MSI-1436 improves EMS adipose derived progenitor stem cells in the course of adipogenic differentiation through modulation of ER stress, apoptosis, and oxidative stress. Stem Cell Res Ther. 2021 Feb 3;12(1):97. doi: 10.1186/s13287-020-02102-x. PMID: 33536069; PMCID: PMC7860037.
[5]: Roitman MF, Wescott S, et,al. MSI-1436 reduces acute food intake without affecting dopamine transporter activity. Pharmacol Biochem Behav. 2010 Nov;97(1):138-43. doi: 10.1016/j.pbb.2010.05.010. Epub 2010 May 15. PMID: 20478327; PMCID: PMC2945616.
[6]: Shu Y, Jones SR, et,al. The synthesis of spermine analogs of the shark aminosterol squalamine. Steroids. 2002 Mar;67(3-4):291-304. doi: 10.1016/s0039-128x(01)00161-1. PMID: 11856553.
[7]: Krishnan N, Koveal D, et,al.Targeting the disordered C terminus of PTP1B with an allosteric inhibitor. Nat Chem Biol. 2014 Jul;10(7):558-66. doi: 10.1038/nchembio.1528. Epub 2014 May 20. PMID: 24845231; PMCID: PMC4062594.

Cas No.	186139-09-3	SDF
同義語	Trodusquemine; Aminosterol-1436
Canonical SMILES	NCCCNCCCCNCCCN[C@@H]1C[C@@](C[C@@H](O)[C@]2([H])[C@]3([H])CC[C@@]4(C)[C@@]2([H])CC[C@@]4([C@H](C)CC[C@@H](OS(=O)(O)=O)C(C)C)[H])([H])[C@]3(C)CC1
Formula	C₃₇H₇₂N₄O₅S	M.Wt	685.06
溶解度	Soluble in DMSO	Storage	Store at -20°C
General tips	Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition	Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
		1 mg	5 mg	10 mg
	1 mM	1.4597 mL	7.2986 mL	14.5973 mL
	5 mM	0.2919 mL	1.4597 mL	2.9195 mL
	10 mM	0.146 mL	0.7299 mL	1.4597 mL

モルアリティ計算機
希釈計算機

計算

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 12 reference(s) in Google Scholar.)

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MSI-1436 (Trodusquemine) (Synonyms: Trodusquemine; Aminosterol-1436)

顧客レビュー

GlpBio Citations

Bioactive Compounds Premium Provider

Product has been cited by 1 publications

Related Biological Data

Product Documents

Quality Control & SDS

Protocol

Complete Stock Solution Preparation Table

モルアリティ計算機

希釈計算機

In vivo Formulation Calculator (Clear solution)

レビュー

MSI-1436 (Trodusquemine) (Synonyms: Trodusquemine; Aminosterol-1436)

顧客レビュー

GlpBio Citations

Bioactive Compounds Premium Provider

Product has been cited by 1 publications

Related Biological Data

Product Documents

Quality Control & SDS

Protocol

Complete Stock Solution Preparation Table

モルアリティ計算機

希釈計算機

In vivo Formulation Calculator (Clear solution)

Related Products

レビュー