ML161

Catalog No.S2916

ML-161 is an allosteric inhibitor of PAR1 with IC50 of 0.26 μM.

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In DMSO USD 190 In stock
USD 147 In stock
USD 470 In stock
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ML161 Chemical Structure

ML161 Chemical Structure
Molecular Weight: 361.23

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

ML161 is available in the following compound libraries:

Product Information

Product Description

Biological Activity

Description ML-161 is an allosteric inhibitor of PAR1 with IC50 of 0.26 μM.
In vitro ML-161 is an allosteric inhibitor of PAR1. ML-161 displays dose-dependent inhibition of thrombin-induced platelet activation, as measured by P-selectin expression. ML-161 displays selective inhibition of SFLLRN and thrombin-induced platelet aggregation, both of which operate via PAR1, and has no effect on AYPGKF, thromboxane, or ADP-induced platelet aggregation, which are all agonists at alternative platelet GPCRs. [1]
In vivo
Features

Protocol(Only for Reference)

Kinase Assay: [2]

P-Selectin Expression Assay Blood from healthy donors who has not ingested aspirin in the 2 weeks prior to donation is collected by venipuncture into 0.4% sodium citrate. Citrate-anticoagulated blood is centrifuged at 200g for 20 minutes to prepare platelet-rich plasma. Washed platelets are subsequently prepared from platelet-rich plasma by centrifugation at 1,000g in the presence of 0.15 μM PGE1. For analysis of P-selectin expression, 20 μL washed platelets (0.5-1 × 108/mL) are incubated with the indicated agonists. Platelet activation is measured by P-selectin surface expression using PE-antihuman P-selectin and flow cytometry. Results are expressed as percent inhibition of P-selectin surface expression.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Dockendorff C, et al. ACS Med Chem Lett, 2012, 3(3), 232-237.

Chemical Information

Download ML161 SDF
Molecular Weight (MW) 361.23
Formula

C17H17BrN2O2

CAS No. 423735-93-7
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 72 mg/mL (199.31 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name Benzamide, 2-bromo-N-[3-[(1-oxobutyl)amino]phenyl]-

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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