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 .

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GRI977143

GRI977143 構造式

CAS 番号 : 325850-81-5

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 104 在庫あり
Solution
10 mM * 1 mL in DMSO USD 104 在庫あり
Solid
5 mg $95 在庫あり
10 mg $165 在庫あり
25 mg $345 在庫あり
50 mg $550 在庫あり
100 mg $950 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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GRI977143 関連抗体

Top Publications Citing Use of Products

LPL Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
LPAR1 LPAR2 LPAR3 LPAR5 S1PR1 S1PR2 S1PR3 S1PR4 S1PR5

Caspase アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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  • 純度とドキュメンテーション

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製品説明

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

IC50 & Target[1].

LPA2 Receptor

3.3 μM (EC50)

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]
体外実験

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 関連抗体

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.
分子量

391.44

分子式

C22H17NO4S
CAS 番号
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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, protect from light

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

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
10 mM 0.2555 mL 1.2773 mL 2.5547 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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    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

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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.29%

COA (252 KB) HNMR (135 KB) RP-HPLC (277 KB) LCMS (236 KB)

取扱説明書 (2659 KB)
参考文献

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

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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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製品名:
GRI977143
製品番号:
HY-100676
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