MSI-1436 lactate is a selective, non-competitive inhibitor of the enzyme protein-tyrosine phosphatase 1B (PTB1B), with an IC50 of 1 μM, 200-fold preference over TCPTP (IC50 of 224 μM).

Product information

CAS Number: 1309370-86-2

Molecular Weight: 775.13

Formula: C40H78N4O8S

Chemical Name: 2-hydroxypropanoic acid; {[(3R,6R)-6-[(1R,3aS,3bR,4R,5aR,7S,9aS,9bS,11aR)-7-{[3-({4-[(3-aminopropyl)amino]butyl}amino)propyl]amino}-4-hydroxy-9a,11a-dimethyl-hexadecahydro-1H-cyclopenta[a]phenanthren-1-yl]-2-methylheptan-3-yl]oxy}sulfonic acid

Smiles: CC(C)[C@@H](CC[C@@H](C)[C@H]1CC[C@H]2[C@H]3[C@H](CC[C@@]21C)[C@@]1(C)CC[C@@H](C[C@@H]1C[C@H]3O)NCCCNCCCCNCCCN)OS(O)(=O)=O.CC(O)C(O)=O

InChiKey: IVOWHCPDKHVRGQ-GMEVOBQHSA-N

InChi: InChI=1S/C37H72N4O5S.C3H6O3/c1-26(2)34(46-47(43,44)45)13-10-27(3)30-11-12-31-35-32(15-17-37(30,31)5)36(4)16-14-29(24-28(36)25-33(35)42)41-23-9-22-40-20-7-6-19-39-21-8-18-38;1-2(4)3(5)6/h26-35,39-42H,6-25,38H2,1-5H3,(H,43,44,45);2,4H,1H3,(H,5,6)/t27-,28-,29+,30-,31+,32+,33-,34-,35+,36+,37-;/m1./s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 54 mg/mL (53.99 mM; Need ultrasonic and warming). H2O : ≥ 33.33 mg/mL (33.32 mM).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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. 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. MSI-1436 (0.1-100 µM) blocks PTP1B activity.

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. MSI-1436 (Trodusquemine) exhibits anxiolytic effect through a restoration of endocannabinoid (eCB) signaling within the amygdala. 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.

Products are for research use only. Not for human use.