MSI-1436 lactate
Based on 8 publication(s) in Google Scholar
MSI-1436 lactate is a selective, non-competitive inhibitor of the enzyme protein-tyrosine phosphatase 1B (PTP1B), with an IC50 of 1 μM, 200-fold preference over TCPTP (IC50 of 224 μM).
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- Reinheit: 98.79%
- CAS. Nr.: 1309370-86-2
- Formel: C40H78N4O8S
- Molecular Weight:1000.17
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) MSI-1436 lactate
More- Nature. 2024 Jul;631(8020):415-423. [Abstract]
- J Ginseng Res. 2025 Nov;49(6):652-662. [Abstract]
- Commun Biol. 2021 Feb 24;4(1):248. [Abstract]
- Spectrochim Acta A Mol Biomol Spectrosc. 2024 Nov 3:327:125394. [Abstract]
- Exp Neurol. 2025 Mar:385:115115. [Abstract]
- Oncol Rep. 2024 Nov;52(5):149. [Abstract]
- J Leukoc Biol. 2024 Jul 16:qiae159. [Abstract]
- Biomed Pharmacother. 2026 Jan:194:118951. [Abstract]
Biologische Aktivität
IC50: 1 μM (PTB1B), 224 μM (TCPTP)[1]
MSI-1436's inhibition of TCPTP is less than the effect on PTP1B activity, with a resulting IC50 value of 224 μM[1]. MSI-1436 (Trodusquemine, 10 μM) restores ERK phosphorylation in response to mGluR1/5 agonist DHPG in F11 neuronal cells. MSI-1436 (10 uM) rescues DHPG-induced holding currents and restores DSI in LMO4KO BLA neurons[2]. MSI-1436 (0.1-100 μM) blocks PTP1B activity[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MSI-1436 (Trodusquemine) exhibits anxiolytic effect through a restoration of endocannabinoid (eCB) signaling within the amygdala[2].
MSI-1436 (5 mg/kg, i.p.) has an anti-diabetic effect on diabetic mice, and is sufficient to suppress food intake and cause weight loss in CD1 mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1309370-86-2
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Appearance Solid
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Molecular Weight 1000.17
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Formel C40H78N4O8S
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Color White to off-white
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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.O=C(O)C(C)O.[3.5]
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Synonyms
Trodusquemine lactate; Aminosterol-1436 lactate
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications (8)
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Journal Impact Factor
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Most Recent
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Nature
2024 Jul;631(8020):415-423. PMID: 38867038 -
J Ginseng Res
(20S)-protopanaxatriol attenuates Ang II-induced renal injury via PTPN1-mediated AMPK/mTOR signaling pathway. [Abstract]2025 Nov;49(6):652-662. PMID: 41268307 -
Commun Biol
βA1-crystallin regulates glucose metabolism and mitochondrial function in mouse retinal astrocytes by modulating PTP1B activity. [Abstract]2021 Feb 24;4(1):248. PMID: 33627831 -
Spectrochim Acta A Mol Biomol Spectrosc
A novel fluorescent probe with Aggregation-Induced emission characteristics for PTP1B activity sensing and inhibitor screening. [Abstract]2024 Nov 3:327:125394. PMID: 39520822 -
Exp Neurol
Pharmacological PTP1B inhibition rescues motor learning, neuroinflammation, and hyperglycaemia in a mouse model of Alzheimer's disease. [Abstract]2025 Mar:385:115115. PMID: 39672227 -
Oncol Rep
The combination of a PTP1B inhibitor, TNFR2 blocker, and PD‑1 antibody suppresses the progression of non‑small cell lung cancer tumors by enhancing immunocompetence. [Abstract]2024 Nov;52(5):149. PMID: 39301655 -
J Leukoc Biol
Combination of microparticles vaccine with MSI-1436 exerts a strong immune response for hepatocellular carcinoma. [Abstract]2024 Jul 16:qiae159. PMID: 39012079 -
Biomed Pharmacother
Multi-target mechanisms of glabrone in ulcerative colitis: Synergistic restoration of mucosal barrier and inhibition of inflammation through SRC/HSP90 Co-modulation. [Abstract]2026 Jan:194:118951. PMID: 41496348
Lösungsmittel & Löslichkeit
DMSO : 54 mg/mL (53.99 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
0.1 M HCl : 50 mg/mL (49.99 mM; ultrasonic and adjust pH to 4 with HCl)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
Quantitation of phosphatase activity is measured using an intact cell assay. Hep G2 cells are pretreated with 10 μM MSI-1436 lactate or sodium orthovanadate (100 μM, postive control) for 10 min at 37 °C, then incubated with 10 μM pNPP (a cell permeable hydrolysable substrate) for 30 min at 37 °C. Samples of the supernatants are spectrophotometrically analyzed at OD405 for hydolyzed pNP, a direct end product of phosphatase activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Male AKR/J mice are randomly placed on ad libitum 10, 45, or 60% fat kcal diets. After 14 weeks, mice are randomly assigned to three treatment groups (n=5 to 8 mice/group); MSI-1436 lactate (initial dose of 10 mg/kg with three subsequent weekly doses of 5 mg/kg, intraperitoneally), vehicle (saline, 10 mL/kg, weekly 4×), or pair-fed (PF). PF animals are injected with saline (weekly 4×) and allotted the amount of food consumed daily by MSI-1436 lactate -treated animals. On day 23, mice are anesthetized and euthanized for blood and tissue collection, respectively. Plasma is obtained following centrifugation of blood 14,000 rpm for 10 min at 4°C[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Lantz KA, 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):1516-1523. [Content Brief]
[2]. Qin Z, et al. Chronic stress induces anxiety via an amygdalar intracellular cascade that impairs endocannabinoid signaling. Neuron. 2015 Mar 18;85(6):1319-31. [Content Brief]
[3]. Qin Z, et al. Functional properties of Claramine: a novel PTP1B inhibitor and mimetic compound. Biochem Biophys Res Commun. 2015 Feb 27;458(1):21-7. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| 0.1 M HCl / DMSO | 1 mM | 0.9998 mL | 4.9992 mL | 9.9983 mL | 24.9958 mL |
| 5 mM | 0.2000 mL | 0.9998 mL | 1.9997 mL | 4.9992 mL | |
| 10 mM | 0.1000 mL | 0.4999 mL | 0.9998 mL | 2.4996 mL | |
| 15 mM | 0.0667 mL | 0.3333 mL | 0.6666 mL | 1.6664 mL | |
| 20 mM | 0.0500 mL | 0.2500 mL | 0.4999 mL | 1.2498 mL | |
| 25 mM | 0.0400 mL | 0.2000 mL | 0.3999 mL | 0.9998 mL | |
| 30 mM | 0.0333 mL | 0.1666 mL | 0.3333 mL | 0.8332 mL | |
| 40 mM | 0.0250 mL | 0.1250 mL | 0.2500 mL | 0.6249 mL | |
| DMSO | 50 mM | 0.0200 mL | 0.1000 mL | 0.2000 mL | 0.4999 mL |
MSI-1436 lactate Related Classifications
HY-12219A Related Classifications
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