MLR 1023

Selective allosteric activator of Lyn kinase CAS# 41964-07-2

MLR 1023

Catalog No. BCC6232----Order now to get a substantial discount!

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Chemical structure

MLR 1023

3D structure

Chemical Properties of MLR 1023

Cas No. 41964-07-2 SDF Download SDF
PubChem ID 39065 Appearance Powder
Formula C11H10N2O2 M.Wt 202.21
Type of Compound N/A Storage Desiccate at -20°C
Synonyms MLR-1023
Solubility DMSO : 150 mg/mL (741.80 mM; Need ultrasonic)
Chemical Name 5-(3-methylphenoxy)-1H-pyrimidin-2-one
SMILES CC1=CC(=CC=C1)OC2=CNC(=O)N=C2
Standard InChIKey HJQILFPVRNHTIG-UHFFFAOYSA-N
Standard InChI InChI=1S/C11H10N2O2/c1-8-3-2-4-9(5-8)15-10-6-12-11(14)13-7-10/h2-7H,1H3,(H,12,13,14)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of MLR 1023

DescriptionSelective allosteric activator of Lyn kinase (EC50 = 63 nM); displays no significant activity against a range of 47 other kinases, including other Src family kinases such as Fyn, Lck and Src kinase. Reduces blood glucose levels without affecting in vivo insulin secretion. Orally bioavailable.

MLR 1023 Dilution Calculator

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MLR 1023 Molarity Calculator

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Preparing Stock Solutions of MLR 1023

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 4.9454 mL 24.7268 mL 49.4535 mL 98.9071 mL 123.6338 mL
5 mM 0.9891 mL 4.9454 mL 9.8907 mL 19.7814 mL 24.7268 mL
10 mM 0.4945 mL 2.4727 mL 4.9454 mL 9.8907 mL 12.3634 mL
50 mM 0.0989 mL 0.4945 mL 0.9891 mL 1.9781 mL 2.4727 mL
100 mM 0.0495 mL 0.2473 mL 0.4945 mL 0.9891 mL 1.2363 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on MLR 1023

Tolimidone is a potent and selective allosteric activator of Lyn kinase with an EC50 of 63 nM.

In Vitro:Incubation of Tolimidone (MLR-1023) with Lyn kinase elicits a repeatable 50% increase in enzyme activity. Tolimidone elicits a concentration-dependent increase in Lyn kinase activation with a 2.3- and 2.1-fold increase achieved at concentrations of 3 and 10 μM, respectively. Inclusion of Tolimidone (100 μM) increases Lyn kinase activity by 3-fold at each ATP concentration tested (Vmax=2601 U/mg). Tolimidone-mediated activation of Lyn kinase increases in proportion to the length of preincubation period in the absence of ATP[1].

In Vivo:Administration of Tolimidone (MLR-1023) (30 mg/kg i.p.) significantly (p<0.05) lowers blood glucose levels to 148 and 158 mg/dL, 30 and 90 min after administration, respectively. Tolimidone significantly increases adipocyte differentiation and adiponectin production by 3.7- and 19-fold, respectively[1]. Tolimidone elicits a dose-dependent potentiation of the insulin response, with a maximal effect observed with a dose level of 30 mg/kg[2].

References:
[1]. Saporito MS, et al. MLR-1023 is a potent and selective allosteric activator of Lyn kinase in vitro that improves glucose tolerance in vivo. J Pharmacol Exp Ther. 2012 Jul;342(1):15-22. [2]. Ochman AR, et al. The Lyn kinase activator MLR-1023 is a novel insulin receptor potentiator that elicits a rapid-onset and durable improvement in glucose homeostasis in animal models of type 2 diabetes. J Pharmacol Exp Ther. 2012 Jul;342(1):23-32.

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References on MLR 1023

MLR-1023 is a potent and selective allosteric activator of Lyn kinase in vitro that improves glucose tolerance in vivo.[Pubmed:22473614]

J Pharmacol Exp Ther. 2012 Jul;342(1):15-22.

2(1H)-pyrimidinone,5-(3-methylphenoxy) (MLR-1023) is a candidate for the treatment of type 2 diabetes. The current studies were aimed at determining the mechanism by which MLR-1023 mediates glycemic control. In these studies, we showed that MLR-1023 reduced blood glucose levels without increasing insulin secretion in vivo. We have further determined that MLR-1023 did not activate peroxisome proliferator-activated alpha, delta, and gamma receptors or glucagon-like peptide-1 receptors or inhibit dipeptidyl peptidase-4 or alpha-glucosidase enzyme activity. However, in an in vitro broad kinase screen MLR-1023 activated the nonreceptor-linked Src-related tyrosine kinase Lyn. MLR-1023 increased the V(max) of Lyn with an EC(50) of 63 nM. This Lyn kinase activation was ATP binding site independent, indicating that MLR-1023 regulated the kinase through an allosteric mechanism. We have established a link between Lyn activation and blood glucose lowering with studies showing that the glucose-lowering effects of MLR-1023 were abolished in Lyn knockout mice, consistent with existing literature linking Lyn kinase and the insulin-signaling pathway. In summary, these studies describe MLR-1023 as a unique blood glucose-lowering agent and show that MLR-1023-mediated blood glucose lowering depends on Lyn kinase activity. These results, coupled with other results (J Pharmacol Exp Ther 342:23-32, 2012), suggest that MLR-1023 and Lyn kinase activation may be a new treatment modality for type 2 diabetes.

The Lyn kinase activator MLR-1023 is a novel insulin receptor potentiator that elicits a rapid-onset and durable improvement in glucose homeostasis in animal models of type 2 diabetes.[Pubmed:22431203]

J Pharmacol Exp Ther. 2012 Jul;342(1):23-32.

MLR-1023 [Tolimidone; CP-26154; 2(1H)-pyrimidinone, 5-(3-methylphenoxy)] is an allosteric Lyn kinase activator that reduces blood glucose levels in mice subjected to an oral glucose tolerance test (J Pharmacol Exp Ther 342:15-22, 2012). The current studies were designed to define the role of insulin in MLR-1023-mediated blood glucose lowering, to evaluate it in animal models of type 2 diabetes, and to compare it to the activities of selected existing diabetes therapeutics. Results from these studies show that in an acute oral glucose tolerance test MLR-1023 evoked a dose-dependent blood glucose-lowering response that was equivalent in magnitude to that of metformin without eliciting a hypoglycemic response. In streptozotocin-treated, insulin-depleted mice, MLR-1023 administration did not affect blood glucose levels. However, MLR-1023 potentiated the glucose-lowering activity of exogenously administered insulin, showing that MLR-1023-mediated blood glucose lowering was insulin-dependent. In a hyperinsulinemic/euglycemic clamp study, orally administered MLR-1023 increased the glucose infusion rate required to sustain blood glucose levels, demonstrating that MLR-1023 increased insulin receptor sensitivity. In chronically treated db/db mice, MLR-1023 elicited a dose-dependent and durable glucose-lowering effect, reduction in HbA1c levels and preservation of pancreatic beta-cells. The magnitude of effect was equivalent to that seen with rosiglitazone but with a faster onset of action and without causing weight gain. These studies show that MLR-1023 is an insulin receptor-potentiating agent that produces a rapid-onset and durable blood glucose-lowering activity in diabetic animals.

Description

Tolimidone is a potent and selective allosteric activator of Lyn kinase with an EC50 of 63 nM.

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