1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. Sarpogrelate hydrochloride

Sarpogrelate hydrochloride (Synonyms: MCI-9042)

Cat. No.: HY-10564 Purity: ≥98.0%
Handling Instructions

Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis.

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

Sarpogrelate hydrochloride Chemical Structure

Sarpogrelate hydrochloride Chemical Structure

CAS No. : 135159-51-2

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 83 In-stock
Estimated Time of Arrival: December 31
10 mg USD 75 In-stock
Estimated Time of Arrival: December 31
50 mg USD 235 In-stock
Estimated Time of Arrival: December 31
100 mg USD 320 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

Publications Citing Use of MCE Sarpogrelate hydrochloride

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis[1][2][3].

IC50 & Target[1]

5-HT2A Receptor

8.52 (pKi)

5-HT2B Receptor

6.57 (pKi)

5-HT2C Receptor

7.43 (pKi)

In Vitro

Sarpogrelate is selective for 5-HT2 (pKi=7.54) over 5-HT1 (pKi=4.58), α1-, α2-, and β-adrenergic (pKi=3.17-6.19), and muscarinic receptors (pKi=4.39)[2].
Sarpogrelate (10 μM) significantly reduces the number of platelet-rich plasma (PRP)-induced THP-1 cell that adheres to human umbilical vein endothelial cells (HUVECs)[3].
Sarpogrelate (10 μM) significantly reduces the expression of PRP-induced E-selectin in HUVECs[3].

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

In Vivo

Sarpogrelate (5 mg/kg; i.p. daily for 4 weeks) inhibits HFFD-induced obesity and decreases leukocyte-endothelial interactions in mice[3].

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

Animal Model: Male C57BL/6 mice (7 weeks old) are fed normal chow (NC) or a high-fat diet with 30% fructose in the drinking water (HFFD)[3]
Dosage: 5 mg/kg
Administration: I.p. daily for 4 weeks
Result: Prevented the HFFD-induced increases of the body weight, visceral fat weight, and serum monocyte chemoattractant protein-1 levels.
Decreased leukocyte-endothelial interactions and serum monocyte chemoattractant protein-1 (MCP-1) level.
Clinical Trial
Molecular Weight

465.97

Formula

C₂₄H₃₂ClNO₆

CAS No.

135159-51-2

SMILES

COC1=CC=CC(CCC2=CC=CC=C2OCC(CN(C)C)OC(CCC(O)=O)=O)=C1.Cl

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 : ≥ 62 mg/mL (133.06 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1461 mL 10.7303 mL 21.4606 mL
5 mM 0.4292 mL 2.1461 mL 4.2921 mL
10 mM 0.2146 mL 1.0730 mL 2.1461 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: ≥ 2.5 mg/mL (5.37 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (5.37 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (5.37 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

SarpogrelateMCI-9042MCI9042MCI 90425-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT2RvascularthrombosisInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Sarpogrelate hydrochloride
Cat. No.:
HY-10564
Quantity:
MCE Japan Authorized Agent: