2. GPCR/G Protein
  3. Prostaglandin Receptor
  4. Asapiprant

Asapiprant  (Synonyms: S-555739)

製品番号: HY-16763 純度: 99.89%
COA 取扱説明書 Technical Support

Asapiprant is a potent and selective DP1 receptor antagonist with a Ki of 0.44 nM.

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Asapiprant

Asapiprant 構造式

CAS 番号 : 932372-01-5

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 132 在庫あり
Solution
10 mM * 1 mL in DMSO USD 132 在庫あり
Solid
1 mg $41 在庫あり
5 mg $120 在庫あり
10 mg $190 在庫あり
25 mg $358 在庫あり
50 mg $573 在庫あり
100 mg $922 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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カスタマーレビュー

Based on 1 publication(s) in Google Scholar

Asapiprant 関連抗体

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  • 生物活性

  • プロトコル

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

Asapiprant is a potent and selective DP1 receptor antagonist with a Ki of 0.44 nM.

IC50 & Target[1]

DP1

0.44 nM (Ki)

体内実験

Oral administration of Asapiprant to sheep at 1 and 3 mg/kg significantly (P<0.01) suppresses the increase in nasal resistance by 82% and 92%, respectively. Oral administration of Asapiprant to sheep at 5 mg/kg suppresses Prostaglandin (PG) D2 (PGD)2-induced nasal resistance by 86%. When orally administered 1 h before the antigen challenge in pigs, Asapiprant (3, 10, and 30 mg/kg) suppresses immediate airway response (IAR) by 52%, 57%, and 96%, and late airway response (LAR) by 67%, 50%, and 79%, respectively. Orally administered with Asapiprant (5 mg/kg) for 4 days, the Asapiprant significantly (P<0.01) suppresses antigen-induced nasal resistance by 73% in sheep. Treatment with 3 and 30 mg/kg of Asapiprant in pigs significantly (P<0.01) suppresses nasal secretion by 53% and 72%, respectively. Treatment with Asapiprant in rats at 10 mg/kg significantly (P<0.05) reduces airway hyper-responsiveness (AHR), infiltration of inflammatory cells, and mucin production in bronchoalveolar lavage fluid (BALF), although treatment with Asapiprant at 0.1 mg/kg does not have a significant effect on any responses[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
分子量

501.55

分子式

C24H27N3O7S
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)COC1=CC(N2CCN(S(=O)(C3=CC=C(OC(C)C)C=C3)=O)CC2)=CC=C1C4=NC=CO4
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 : 11.11 mg/mL (22.15 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 1.9938 mL 9.9691 mL 19.9382 mL
5 mM 0.3988 mL 1.9938 mL 3.9876 mL
10 mM 0.1994 mL 0.9969 mL 1.9938 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.11 mg/mL (2.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.11 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.1 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: ≥ 1.11 mg/mL (2.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.11 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.1 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.
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).
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
参考文献
動物実験
[1]

Male Hartley guinea pigs (300 to 400 g) and male brown Norway rats (240 to 400 g) are used in this study. The guinea pigs and rats are housed in an air-conditioned room at 20 to 26°C with a relative humidity of 30 to 70%, and are fed standard laboratory chow and given water ad libitum. Female sheep (32 to 46 kg) naturally sensitive to ascaris suum antigen are also used. After the oral administration of Asapiprant to rats, guinea pigs, and sheep at 10 mg/kg in suspension with 0.5% methylcellulose solution, the plasma concentrations of the drugs are measured[1].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9938 mL 9.9691 mL 19.9382 mL 49.8455 mL
5 mM 0.3988 mL 1.9938 mL 3.9876 mL 9.9691 mL
10 mM 0.1994 mL 0.9969 mL 1.9938 mL 4.9845 mL
15 mM 0.1329 mL 0.6646 mL 1.3292 mL 3.3230 mL
20 mM 0.0997 mL 0.4985 mL 0.9969 mL 2.4923 mL
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Asapiprant 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:

Asapiprant932372-01-5S-555739S555739S 555739Prostaglandin ReceptorInhibitorinhibitorinhibit

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製品名:
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製品番号:
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