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

Sarpogrelate hydrochloride  (Synonyms: MCI-9042)

Cat. No.: HY-10564 Purity: 99.09%
COA
SDS
Handling Instructions Technical Support

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.

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Sarpogrelate hydrochloride

Sarpogrelate hydrochloride 화학구조

CAS No. : 135159-51-2

사이즈 가격 재고 수량
무료 샘플 (0.1 - 0.2 mg)   지금 신청하기  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
5 mg 해외재고보유
10 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

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This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 1 publication(s) in Google Scholar

Other Forms of Sarpogrelate hydrochloride:

Sarpogrelate hydrochloride Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Sarpogrelate hydrochloride

View All 5-HT Receptor Isoform Specific Products:

View All Isoforms
5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

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

 

5-HT2B Receptor

 

5-HT2C Receptor

 

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].

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

Sarpogrelate hydrochloride Related Antibodies
In Vivo

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

MedChemExpress (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.
분자량

465.97

화학식

C24H32ClNO6
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
보관

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

용액&용해도
In Vitro: 

DMSO : ≥ 62 mg/mL (133.06 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 33.33 mg/mL (71.53 mM; Need ultrasonic)

*"≥" 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
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • 몰농도 계산기

  • 농도 희석 계산기

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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    40% PEG300    5% Tween-80    45% Saline

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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

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:  PBS

    Solubility: 10 mg/mL (21.46 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
순도&문서
References

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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.1461 mL 10.7303 mL 21.4606 mL 53.6515 mL
5 mM 0.4292 mL 2.1461 mL 4.2921 mL 10.7303 mL
10 mM 0.2146 mL 1.0730 mL 2.1461 mL 5.3652 mL
15 mM 0.1431 mL 0.7154 mL 1.4307 mL 3.5768 mL
20 mM 0.1073 mL 0.5365 mL 1.0730 mL 2.6826 mL
25 mM 0.0858 mL 0.4292 mL 0.8584 mL 2.1461 mL
30 mM 0.0715 mL 0.3577 mL 0.7154 mL 1.7884 mL
40 mM 0.0537 mL 0.2683 mL 0.5365 mL 1.3413 mL
50 mM 0.0429 mL 0.2146 mL 0.4292 mL 1.0730 mL
60 mM 0.0358 mL 0.1788 mL 0.3577 mL 0.8942 mL
DMSO 80 mM 0.0268 mL 0.1341 mL 0.2683 mL 0.6706 mL
100 mM 0.0215 mL 0.1073 mL 0.2146 mL 0.5365 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Sarpogrelate hydrochloride Related Classifications

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:

Sarpogrelate135159-51-2MCI-9042MCI9042MCI 90425-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT2RvascularthrombosisInhibitorinhibitorinhibit

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상품명:
Sarpogrelate hydrochloride
Cat. No.:
HY-10564
수량:
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