2. GPCR/G Protein
  3. LPL Receptor
  4. AS2717638

AS2717638 is a highly selective, brain-penetrant and orally active lysophosphatidic acid receptor 5 (LPA5) antagonist with an IC50 value of 38 nM. AS2717638 is highly selective and shows no significant antagonistic activity against other LPA receptors (LPA1, LPA2, and LPA3). AS2717638 can be used in the research of pain and neuroinflammation-related diseases.

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AS2717638

AS2717638 構造式

CAS 番号 : 2148339-28-8

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 170 在庫あり
Solution
10 mM * 1 mL in DMSO USD 170 在庫あり
Solid
5 mg $155 在庫あり
10 mg $255 在庫あり
25 mg $510 在庫あり
50 mg $820 在庫あり
100 mg $1300 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

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

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Based on 2 publication(s) in Google Scholar

AS2717638 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

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

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製品説明

AS2717638 is a highly selective, brain-penetrant and orally active lysophosphatidic acid receptor 5 (LPA5) antagonist with an IC50 value of 38 nM. AS2717638 is highly selective and shows no significant antagonistic activity against other LPA receptors (LPA1, LPA2, and LPA3). AS2717638 can be used in the research of pain and neuroinflammation-related diseases[1][2].

IC50 & Target[1]

LPA5 Receptor

38 nM (IC50, Human)

LPA5 Receptor

9.1 nM (Ki, Human)

LPA5 Receptor

16 nM (Ki, Rat)

LPA5 Receptor

7.3 nM (Ki, Mouse)

体外実験

AS2717638 (0.038 μM; 20 min) inhibits LPA-induced cAMP accumulation in the cAMP accumulation assay using CHO cells expressing human LPA5[2].
AS2717638 (0.1 μM, 1 μM; 24 h) has no effect on MTT reduction in BV-2 cells, and the cell viability is not significantly affected; at 10 μM (24 h), the cell viability is reduced by 50%[2].
AS2717638 (0.1-1 μM; 2-24 h) inhibits the phosphorylation of STAT1, p65, and c-Jun in LPS-stimulated BV-2 cells. AS2717638 reduces the expression of TLR4 and COX2, and decreases NO production in LPS-stimulated BV-2 cells[2].
AS2717638 (0.1-1 μM; 2-24 h) reduces the secretion of cytokines and chemokines such as TNFα, IL-6, CXCL10, CXCL2, and CCL5 in the supernatants of LPS-stimulated BV-2 cell cultures[2].

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

AS2717638 関連抗体

Cell Viability Assay[2]

Cell Line: BV-2 microglia
Concentration: 0.1 μM, 1 μM, 10 μM
Incubation Time: 24 h
Result: At 0.1 μM and 1 μM, had no significant effect on cell viability as indicated by MTT reduction. At 10 μM, it compromised cell viability by 50%.

Western Blot Analysis[2]

Cell Line: BV-2 microglia
Concentration: 0.1 μM, 1 μM
Incubation Time: 2 h, 8 h, 24 h
Result: Inhibited the phosphorylation of STAT1, p65, and c-Jun, reduced the expression of TLR4 and COX2, decreased NO production, and reduced the secretion of TNFα, IL-6, CXCL10, CXCL2, and CCL5 in LPS-stimulated BV-2 cells.
体内実験

AS2717638 (3-30 mg/kg; oral administration; 1 h before the experiment; single dose) inhibits allodynia in mouse models of allodynia induced by LPA or GGPP[1].
AS2717638 (10-30 mg/kg; oral administration; 1 h before the experiment; single dose) alleviates allodynia in mouse models of allodynia induced by PGE2, PGF2α, or AMPA[1].
AS2717638 (10 mg/kg; oral administration; 2 h before the experiment; single dose) ameliorates static mechanical allodynia and thermal hyperalgesia in a rat model of neuropathic pain induced by chronic constriction injury (CCI)[1].
AS2717638 (10 mg/kg; oral administration; 2 h before the experiment; single dose) improves hind paw weight - bearing ability in a rat model of inflammatory pain induced by adjuvant[1].
AS2717638 (10 mg/kg; oral administration; before the experiment; single dose) reduces LPS (HY-D1056)-induced iNOS, TNFα, IL-6, and CXCL2 mRNA expression, improves the expression of neuroinflammation - related proteins, and reduces peripheral cytokine concentrations in a mouse endotoxemia model[2].

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

Animal Model: Male ICR mice, LPA- and GGPP-induced allodynia model[1]
Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg (dissolved in 30% propylene glycol solvent in distilled water)
Administration: Orally, administered once, 1 h before i.t. injection of LPA or GGPP
Result: Significantly inhibited LPA- and GGPP-induced allodynia.
Animal Model: Male ICR mice, PGE2-, PGF2α- or AMPA-induced allodynia model[1]
Dosage: 3 mg/kg, 10 mg/kg, 30 mg/kg (dissolved in 30% propylene glycol solvent in distilled water)
Administration: Orally, administered once, 1 h before i.t. injection of PGE2, PGF2α, or AMPA
Result: Significantly alleviated allodynia in all three pain sensitizer-induced pain models.
Animal Model: Male Sprague-Dawley rats, chronic constriction injury (CCI)-induced neuropathic pain model[1]
Dosage: 10 mg/kg (dissolved in 30% propylene glycol solvent in distilled water)
Administration: Orally, administered once, 2 h before the von Frey and plantar tests
Result: Significantly ameliorated both static mechanical allodynia and thermal hyperalgesia in CCI rats.
Animal Model: Female Lewis rats, adjuvant-induced inflammatory pain model[1]
Dosage: 10 mg/kg (dissolved in 30% propylene glycol solvent in distilled water)
Administration: 10 mg/kg (dissolved in 30% propylene glycol solvent in distilled water)
Result: Significantly improved weight bearing difference in a rat model of adjuvant-induced inflammatory pain.
Animal Model: C57BL/6J mice (8-10 weeks, 20-30 g), mouse endotoxemia model[2]
Dosage: 10 mg/kg
Administration: Orally, administered once, 24 h before sacrifice
Result: Significantly reduced the mRNA expression of iNOS, TNFα, IL6, and CXCL2.
Also amended the expression of neuroinflammatory parameters such as TLR4, Iba1, GFAP, COX-2, and the Bax/Bcl2 ratio.
分子量

447.48

分子式

C25H25N3O5
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C1N(C=C(C2=C1C=C(C(OC)=C2)OC)C(N3CCCCC3)=O)C4=NOC5=C4C=C(C=C5)C
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 60 mg/mL (134.08 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 2.2347 mL 11.1737 mL 22.3474 mL
5 mM 0.4469 mL 2.2347 mL 4.4695 mL
10 mM 0.2235 mL 1.1174 mL 2.2347 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. 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)

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Volume
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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

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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 6 mg/mL (13.41 mM); Clear solution

    This protocol yields a clear solution of ≥ 6 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (60.0 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% Corn Oil

    Solubility: ≥ 6 mg/mL (13.41 mM); Clear solution

    This protocol yields a clear solution of ≥ 6 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 (60.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

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mg/kg

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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 +
% 
+
%
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%
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).
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: 99.85%

COA (257 KB) HNMR (356 KB) LCMS (95 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. 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 2.2347 mL 11.1737 mL 22.3474 mL 55.8684 mL
5 mM 0.4469 mL 2.2347 mL 4.4695 mL 11.1737 mL
10 mM 0.2235 mL 1.1174 mL 2.2347 mL 5.5868 mL
15 mM 0.1490 mL 0.7449 mL 1.4898 mL 3.7246 mL
20 mM 0.1117 mL 0.5587 mL 1.1174 mL 2.7934 mL
25 mM 0.0894 mL 0.4469 mL 0.8939 mL 2.2347 mL
30 mM 0.0745 mL 0.3725 mL 0.7449 mL 1.8623 mL
40 mM 0.0559 mL 0.2793 mL 0.5587 mL 1.3967 mL
50 mM 0.0447 mL 0.2235 mL 0.4469 mL 1.1174 mL
60 mM 0.0372 mL 0.1862 mL 0.3725 mL 0.9311 mL
80 mM 0.0279 mL 0.1397 mL 0.2793 mL 0.6984 mL
100 mM 0.0223 mL 0.1117 mL 0.2235 mL 0.5587 mL
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AS2717638 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:

AS27176382148339-28-8AS 2717638AS-2717638LPL ReceptorLysophospholipid Receptorbrain-penetrantorally activeLPA5Inhibitorinhibitorinhibit

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製品名:
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製品番号:
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