MSI-1436 lactate_product_DataBase

Bioactivity	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).
Target	IC50: 1 μM (PTB1B), 224 μM (TCPTP)
Invitro	MSI-1436's inhibition of TCPTP is approximately two logs 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].
In Vivo	MSI-1436 (10 mg/kg, i.p.) causes obesity-dependent body weight, reduces total body fat content and adipocyte size and lipid content of white adipose tissue of mice[1]. 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].
Name	MSI-1436 lactate
CAS	1309370-86-2
Formula	C40H78N4O8S
Molar Mass	1000.17
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Reference	[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. [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. [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.

PeptideDB

MSI-1436 lactate

CAS: 1309370-86-2 F: C40H78N4O8S W: 1000.17