Art. -Nr.: HY-100676

Copy Link Print Information

GRI977143

Kundenbewertung

Based on 1 Customer Validation

GRI977143 is a specific LPA₂ receptor agonist, with an EC₅₀ of 3.3 μM .

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.29%
CAS. Nr.: 325850-81-5
Formel: C₂₂H₁₇NO₄S
Molecular Weight:391.44

Speicherung:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

GRI977143 Chemical Structure

CAS. Nr.: 325850-81-5

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

GRI977143 is a specific LPA₂ receptor agonist, with an EC₅₀ of 3.3 μM ^[1].

IC₅₀ & Target^[1].

LPA₂ Receptor

3.3 μM (EC₅₀)

Alle LPL Receptor Isoform-spezifische Produkte anzeigen :

Alle Caspase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MEF	EC₅₀	3.3 μM Compound: 3, GRI-977143	Agonist activity at human LPA2 expressed in LPA1xLPA2 double knockout mouse MEF cells by Fura-2AM dye based Ca2+ mobilization assay Agonist activity at human LPA2 expressed in LPA1xLPA2 double knockout mouse MEF cells by Fura-2AM dye based Ca2+ mobilization assay	[PMID: 25100502]
MEF	IC₅₀	6.6 μM Compound: 3, GRI-977143	Antagonist activity at human LPA3 expressed in LPA1xLPA2 double knockout mouse MEF cells assessed as reduction in LP18:1-induced calcium mobilization by Fura-2AM dye based Ca2+ mobilization assay Antagonist activity at human LPA3 expressed in LPA1xLPA2 double knockout mouse MEF cells assessed as reduction in LP18:1-induced calcium mobilization by Fura-2AM dye based Ca2+ mobilization assay	[PMID: 25100502]

In Vitro

GRI977143 (10 μM, 24-72 h) is effective in reducing activation of caspases 3, 7, 8, and 9 and inhibits poly(ADP-ribose)polymerase 1 cleavage and DNA fragmentation in different extrinsic and intrinsic models of apoptosis^[1].
GRI977143 is an effective stimulator of extracellular signal-regulated kinase 1/2 activation and promotes the assembly of a macromolecular signaling complex consisting of LPA2, Na+-H+ exchange regulatory factor 2, and thyroid receptor interacting protein 6^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

Vector- and LPA2-transduced MEF cells (2 × 10⁴)^[1].
Concentration:

10 μM.
Incubation Time:

24-72 h.
Result:

Did not cause a significant increase in vector cell proliferation except at 72 h (p < 0.05).

Apoptosis Analysis^[1].

Cell Line:

Doxorubicin-induced apoptotic signaling in vector-transduced or LPA2-transduced MEF.
Concentration:

10 μM.
Incubation Time:

24 h.
Result:

Reduced caspase 3 and 7 activation on LPA2-transduced MEF cells by 51 ± 3% and was approximately as potent as 3 μM LPA or OTP.
Protected against doxorubicin-induced apoptosis by inhibiting caspase 3, 7, 8, and 9 and reducing DNA fragmentation.

Chemical Information

CAS. Nr. 325850-81-5
Appearance Solid
Molecular Weight 391.44
Formel C₂₂H₁₇NO₄S
Color White to off-white
SMILES

O=C(O)C1=CC=CC=C1SCCCN(C(C2=CC=CC3=CC=CC4=C23)=O)C4=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (127.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5547 mL

12.7733 mL

25.5467 mL

5 mM

0.5109 mL

2.5547 mL

5.1093 mL

10 mM

0.2555 mL

1.2773 mL

2.5547 mL

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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 (5.31 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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (597 KB)
- English - EN (597 KB)
- Français - FR (597 KB)
- Deutsch - DE (597 KB)
- Norwegian - NO (597 KB)
- Español - ES (597 KB)
- Swedish - SV (597 KB)
- Italian - IT (597 KB)
- Korean - KR (597 KB)
- Portuguese - PT (597 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Gyöngyi N. Kiss, et al. Virtual Screening for LPA2-Specific Agonists Identifies a Nonlipid Compound with Antiapoptotic Actions. Mol Pharmacol. 2012 Dec; 82(6): 1162–1173. [Content Brief]

[2]. Gyöngyi Nagyné Kiss, et al. PHARMACOLOGICAL AND CELLULAR CHARACTERIZATION OF GRI977143, A NOVEL NONLIPID LPA2 RECEPTOR AGONIST IDENTIFIED BY VIRTUAL SCREENING.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5547 mL	12.7733 mL	25.5467 mL	63.8667 mL
	5 mM	0.5109 mL	2.5547 mL	5.1093 mL	12.7733 mL
	10 mM	0.2555 mL	1.2773 mL	2.5547 mL	6.3867 mL
	15 mM	0.1703 mL	0.8516 mL	1.7031 mL	4.2578 mL
	20 mM	0.1277 mL	0.6387 mL	1.2773 mL	3.1933 mL
	25 mM	0.1022 mL	0.5109 mL	1.0219 mL	2.5547 mL
	30 mM	0.0852 mL	0.4258 mL	0.8516 mL	2.1289 mL
	40 mM	0.0639 mL	0.3193 mL	0.6387 mL	1.5967 mL
	50 mM	0.0511 mL	0.2555 mL	0.5109 mL	1.2773 mL
	60 mM	0.0426 mL	0.2129 mL	0.4258 mL	1.0644 mL
	80 mM	0.0319 mL	0.1597 mL	0.3193 mL	0.7983 mL
	100 mM	0.0255 mL	0.1277 mL	0.2555 mL	0.6387 mL

Keywords

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

GRI977143

Apoptosis Compound Library

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Protease Inhibitor Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alle LPL Receptor Isoform-spezifische Produkte anzeigen

Alle Caspase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GRI977143

Apoptosis Compound Library

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Protease Inhibitor Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alle LPL Receptor Isoform-spezifische Produkte anzeigen

Alle Caspase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GRI977143 Related Classifications

HY-100676 Related Classifications