ML351

Name: ML351
Brand: MedChemExpress
SKU: HY-111310
Rating: 4.5 (1 reviews)

Cat. No.: HY-111310 Purity: 98.58%: FAQs
Data Sheet SDS COA Handling Instructions

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ML351 is a potent and highly specific 15-LOX-1 inhibitor with an IC₅₀ of 200 nM. ML351 shows excellent selectivity (>250-fold) versus the related isozymes, 5-LOX, platelet 12-LOX, 15-LOX-2, ovine COX-1, and human COX-2. ML351 prevents dysglycemia and reduces β-cell oxidative stress in nonobese diabetic mouse model of T1D.

For research use only. We do not sell to patients.

ML351 Chemical Structure

CAS No. : 847163-28-4

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 154	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 154	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 140	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 220	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 680	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 980	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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5-LOX 12-LOX 15-LOX

Biological Activity
Purity & Documentation
References
Customer Review

Description

ML351 is a potent and highly specific 15-LOX-1 inhibitor with an IC₅₀ of 200 nM. ML351 shows excellent selectivity (>250-fold) versus the related isozymes, 5-LOX, platelet 12-LOX, 15-LOX-2, ovine COX-1, and human COX-2^[1]. ML351 prevents dysglycemia and reduces β-cell oxidative stress in nonobese diabetic mouse model of T1D^[2].

Cellular Effect

Cell Line	Type	Value	Description	References
Sf9	IC₅₀	0.12 μM Compound: ML351	Inhibition of human N-terminal His6-tagged 15-LOX-1 R402L mutant expressed in sf9 cells using arachidonic acid or linoleic acid as substrate by UV-Visible spectrophotometric analysis Inhibition of human N-terminal His6-tagged 15-LOX-1 R402L mutant expressed in sf9 cells using arachidonic acid or linoleic acid as substrate by UV-Visible spectrophotometric analysis	[PMID: 27647374]
Sf9	IC₅₀	0.18 μM Compound: ML351	Inhibition of human N-terminal His6-tagged 15-LOX-1 I417A mutant expressed in sf9 cells using arachidonic acid or linoleic acid as substrate by UV-Visible spectrophotometric analysis Inhibition of human N-terminal His6-tagged 15-LOX-1 I417A mutant expressed in sf9 cells using arachidonic acid or linoleic acid as substrate by UV-Visible spectrophotometric analysis	[PMID: 27647374]
Sf9	IC₅₀	0.26 μM Compound: ML351	Inhibition of human N-terminal His6-tagged 15-LOX-1 R404L mutant expressed in sf9 cells using arachidonic acid or linoleic acid as substrate by UV-Visible spectrophotometric analysis Inhibition of human N-terminal His6-tagged 15-LOX-1 R404L mutant expressed in sf9 cells using arachidonic acid or linoleic acid as substrate by UV-Visible spectrophotometric analysis	[PMID: 27647374]
Sf9	IC₅₀	0.3 μM Compound: ML351	Inhibition of human N-terminal His6-tagged 15-LOX-1 Q547L mutant expressed in sf9 cells using arachidonic acid as substrate by UV-Visible spectrophotometric analysis Inhibition of human N-terminal His6-tagged 15-LOX-1 Q547L mutant expressed in sf9 cells using arachidonic acid as substrate by UV-Visible spectrophotometric analysis	[PMID: 27647374]
Sf9	IC₅₀	0.33 μM Compound: ML351	Inhibition of wild type human N-terminal His6-tagged 15-LOX-1 expressed in sf9 cells using arachidonic acid or linoleic acid as substrate by UV-Visible spectrophotometric analysis Inhibition of wild type human N-terminal His6-tagged 15-LOX-1 expressed in sf9 cells using arachidonic acid or linoleic acid as substrate by UV-Visible spectrophotometric analysis	[PMID: 27647374]
Sf9	IC₅₀	0.39 μM Compound: ML351	Inhibition of human N-terminal His6-tagged 15-LOX-1 L407A mutant expressed in sf9 cells using arachidonic acid as substrate by UV-Visible spectrophotometric analysis Inhibition of human N-terminal His6-tagged 15-LOX-1 L407A mutant expressed in sf9 cells using arachidonic acid as substrate by UV-Visible spectrophotometric analysis	[PMID: 27647374]
Sf9	IC₅₀	0.77 μM Compound: ML351	Inhibition of human N-terminal His6-tagged 15-LOX-1 F414W mutant expressed in sf9 cells using arachidonic acid as substrate by UV-Visible spectrophotometric analysis Inhibition of human N-terminal His6-tagged 15-LOX-1 F414W mutant expressed in sf9 cells using arachidonic acid as substrate by UV-Visible spectrophotometric analysis	[PMID: 27647374]
Sf9	IC₅₀	0.87 μM Compound: ML351	Inhibition of human N-terminal His6-tagged 15-LOX-1 E356Q mutant expressed in sf9 cells using arachidonic acid as substrate by UV-Visible spectrophotometric analysis Inhibition of human N-terminal His6-tagged 15-LOX-1 E356Q mutant expressed in sf9 cells using arachidonic acid as substrate by UV-Visible spectrophotometric analysis	[PMID: 27647374]
Sf9	IC₅₀	4.1 μM Compound: ML351	Inhibition of human N-terminal His6-tagged 15-LOX-1 F414I mutant expressed in sf9 cells using arachidonic acid or linoleic acid as substrate by UV-Visible spectrophotometric analysis Inhibition of human N-terminal His6-tagged 15-LOX-1 F414I mutant expressed in sf9 cells using arachidonic acid or linoleic acid as substrate by UV-Visible spectrophotometric analysis	[PMID: 27647374]

In Vitro

ML351 (1-50 μM; 24 hours) displays no deleterious effects on cellular apoptosis (by caspase activity assay)^[2].
ML351 (10-50 μM; 24 h) protects mouse islets in a T1D model in vitro. Islets exposed to proinflammatory cytokines exhibits increased insulin release at 2.5 mM glucose and impaired insulin release in response to 25 mM glucose. However, ML351 restores insulin secretion at 2.5 mmol/L glucose to control levels, and insulin release in response to 25 mM glucose is significantly improved compared with treatment with proinflammatory cytokines alone^[2].
ML351 reverses the stimulation of ROS production in mouse islets in response to proinflammatory cytokines in vitro^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

ML351 (0-48 mg/kg; before the beginning of the STZ series and concluding 5 days after the last dose of STZ) protects against diabetes development in an STZ β-cell injury model. ML351 at 24 mg/kg (M24)+ STZ shows significantly less weight reduction compares with control group. M24 shows almost complete protection from hyperglycemia. But M48 and M0 exhibits frank hyperglycemia by day 9 of the study and significantly impaired GTTs^[2].
ML351 (intraperitoneal injection; 0-24 mg/kg; daily for 2 weeks) leads to improved glycemic control and significantly reduced insulitis. The reduction of β-cell death in NOD mice has been suggested to lead to reductions in insulitis, likely by mitigating the chemotactic signals released by dying β-cells. NOD + M24 animals exhibited improved glycemic control compared with NOD + M0 animals^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Nine-week-old male C57BL/6J mice^[2]
Dosage:	0 mg/kg; 24 mg/kg; 48 mg/kg;
Administration:	Intraperitoneal injection before the beginning of the STZ series and concluding 5 days after the last dose of STZ
Result:	Protected against diabetes development in an STZ β-cell injury model that mimics the inflammation seen in T1D.

Animal Model:	Female NOD mice develop spontaneous autoimmune diabetes between 12 and 24 weeks of age^[2]
Dosage:	0 mg/kg; 24 mg/kg; 48 mg/kg;
Administration:	Intraperitoneal injection before the beginning of the STZ series and concluding 5 days after the last dose of STZ
Result:	Protected Against Early Glycemic Deterioration in NOD Mice.

Molecular Weight

249.27

Formula

C₁₅H₁₁N₃O

CAS No.

847163-28-4

Appearance

Solid

Color

White to light yellow

SMILES

N#CC1=C(NC)OC(C2=C3C=CC=CC3=CC=C2)=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (200.59 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	4.0117 mL	20.0586 mL	40.1171 mL
5 mM	0.8023 mL	4.0117 mL	8.0234 mL
10 mM	0.4012 mL	2.0059 mL	4.0117 mL

View the 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (8.34 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.

Protocol 1

Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 5 mg/mL (20.06 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 98.58%

Select Batch:

Data Sheet (279 KB) SDS (419 KB)

COA (253 KB) LCMS (96 KB)

Handling Instructions (2659 KB)

References

[1]. Thomas Gaberel, et al. Impact of 12/15-Lipoxygenase on Brain Injury After Subarachnoid Hemorrhage. Stroke. 2019 Feb;50(2):520-523. [Content Brief]

[2]. Ganesha Rai, et al. Discovery of ML351, a Potent and Selective Inhibitor of Human 15-Lipoxygenase-1 [Content Brief]

[3]. Marimar Hernandez-Perez, et al. Inhibition of 12/15-Lipoxygenase Protects Against β-Cell Oxidative Stress and Glycemic Deterioration in Mouse Models of Type 1 Diabetes. Diabetes. 2017 Nov;66(11):2875-2887. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	4.0117 mL	20.0586 mL	40.1171 mL	100.2929 mL
	5 mM	0.8023 mL	4.0117 mL	8.0234 mL	20.0586 mL
	10 mM	0.4012 mL	2.0059 mL	4.0117 mL	10.0293 mL
	15 mM	0.2674 mL	1.3372 mL	2.6745 mL	6.6862 mL
	20 mM	0.2006 mL	1.0029 mL	2.0059 mL	5.0146 mL
	25 mM	0.1605 mL	0.8023 mL	1.6047 mL	4.0117 mL
	30 mM	0.1337 mL	0.6686 mL	1.3372 mL	3.3431 mL
	40 mM	0.1003 mL	0.5015 mL	1.0029 mL	2.5073 mL
	50 mM	0.0802 mL	0.4012 mL	0.8023 mL	2.0059 mL
	60 mM	0.0669 mL	0.3343 mL	0.6686 mL	1.6715 mL
	80 mM	0.0501 mL	0.2507 mL	0.5015 mL	1.2537 mL
	100 mM	0.0401 mL	0.2006 mL	0.4012 mL	1.0029 mL

ML351 Related Classifications

Neurological Disease Metabolic Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ML351847163-28-4ML 351ML-351LipoxygenaseLOXSubarachnoid hemorrhageSAHneuronalβ-celloxidative stressnon-obese diabeticT1DInhibitorinhibitorinhibit

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ML351

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Complete Stock Solution Preparation Table

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