1. GPCR/G Protein
  2. Protease-Activated Receptor (PAR)
  3. Parmodulin 2

Parmodulin 2 (Synonyms: ML161)

Cat. No.: HY-13965 Purity: 98.03%
Handling Instructions

Parmodulin 2 (ML161) is an allosteric inhibitor of protease-activated receptor 1 (PAR1) with an IC50 of 0.26 μM. Parmodulin 2 is a potent and non-competitive inhibitor of SFLLRN-induced P-selectin expression leading to inhibition of platelet aggregation in vitro and platelet thrombus formation in vivo.

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

Parmodulin 2 Chemical Structure

Parmodulin 2 Chemical Structure

CAS No. : 423735-93-7

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 56 In-stock
Estimated Time of Arrival: December 31
5 mg USD 70 In-stock
Estimated Time of Arrival: December 31
10 mg USD 100 In-stock
Estimated Time of Arrival: December 31
25 mg USD 190 In-stock
Estimated Time of Arrival: December 31
50 mg USD 330 In-stock
Estimated Time of Arrival: December 31
100 mg USD 600 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

Parmodulin 2 (ML161) is an allosteric inhibitor of protease-activated receptor 1 (PAR1) with an IC50 of 0.26 μM[1]. Parmodulin 2 is a potent and non-competitive inhibitor of SFLLRN-induced P-selectin expression leading to inhibition of platelet aggregation in vitro and platelet thrombus formation in vivo[2].

IC50 & Target

IC50: 0.26 μM (PAR1)[1]

In Vitro

Parmodulin 2 (ML161; 10 µM; for 30 minutes) inhibits proinflammatory signaling in endothelial HUVECs cells[3].

In Vivo

Parmodulin 2 (ML161; 5 mg/kg; IV) significantly inhibits platelet thrombus formation, with a 73% inhibition in AUC (area under the curve)[2].
Parmodulin 2 inhibits platelet thrombus formation in vivo, and it does not prolong bleeding time. Parmodulin 2 selectively inhibits platelet aggregation through Par1 and the α2A-adrenergic receptor[2].

Animal Model: C57BL/6J wild type mice[2]
Dosage: 5 mg/kg (Pharmacokinetic Analysis)
Administration: IV
Result: Significantly inhibited platelet thrombus formation, with a 73% inhibition in AUC.
Molecular Weight

361.23

Formula

C₁₇H₁₇BrN₂O₂

CAS No.

423735-93-7

SMILES

O=C(NC1=CC=CC(NC(CCC)=O)=C1)C2=CC=CC=C2Br

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 : 100 mg/mL (276.83 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7683 mL 13.8416 mL 27.6832 mL
5 mM 0.5537 mL 2.7683 mL 5.5366 mL
10 mM 0.2768 mL 1.3842 mL 2.7683 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.83 mg/mL (2.30 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.83 mg/mL (2.30 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 0.83 mg/mL (2.30 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

Parmodulin 2ML161Parmodulin2Parmodulin-2ML 161ML-161Protease-Activated Receptor (PAR)Thrombin receptorsprotease-activatedreceptor1PAR1SFLLRN-inducedP-selectinplateletaggregationthrombusformationInhibitorinhibitorinhibit

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Product Name:
Parmodulin 2
Cat. No.:
HY-13965
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