2. GPCR/G Protein Apoptosis
  3. LPL Receptor Caspase
  4. GRI977143

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

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

GRI977143 Chemical Structure

GRI977143 Chemical Structure

CAS No. : 325850-81-5

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Based on 1 publication(s) in Google Scholar

GRI977143 Related Antibodies

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Description

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

IC50 & Target[1].

LPA2 Receptor

3.3 μM (EC50)

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.

GRI977143 Related Antibodies

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.
Molecular Weight

391.44

Formula

C22H17NO4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

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

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5547 mL 12.7733 mL 25.5467 mL
5 mM 0.5109 mL 2.5547 mL 5.1093 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 (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.

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

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
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 (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.

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
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GRI977143 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:

GRI977143325850-81-5GRI 977143GRI-977143LPL ReceptorCaspaseLysophospholipid ReceptorInhibitorinhibitorinhibit

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