BP 897
Based on 1 Customer Validation
BP 897 is a potent and partial dopamine D3 receptor agonist and a weak D2 receptor antagonist. BP 897 displays a high affinity at the dopamine D3 receptor (Ki=0.92 nM) and a 70 times lower affinity at the D2 receptor (Ki=61 nM).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.12%
- CAS 番号: 192384-87-5
- 分子式: C26H31N3O2
- 分子量:417.54
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Dopamine Receptor アイソフォーム固有の製品をすべて表示
More
生物活性
製品説明
IC50 & Target
|
D2 Receptor |
D3 Receptor |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
1.8 nM
Compound: BP-897
|
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
|
[PMID: 12361386] |
| CHO | EC50 |
1.8 nM
Compound: 3a
|
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assay
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assay
|
[PMID: 16759104] |
体外実験
BP 897 also displays low affinities at D1 and D4 receptors (Ki=3 and 0.3 μM, respectively), as well as at α1 and α2 adrenergic receptors (Ki=60 and 83 nM, respectively), 5HT1A and 5HT7 receptors (Ki=84 and 345 nM, respectively), and negligible affinities (Ki>1 μM) atmuscarinic, histamine and opiate receptors[1].
In NG 108-15 cells expressing the human D3 receptor, BP 897 inhibits forskolin-induced cyclic AMP accumulation with an EC50 of 1 nM. BP 897 activates mitogenesis and this response is antagonized by the preferential D3 receptor antagonist Nafadotride (1 μM). BP 897 also partially antagonized the response induced by quinpirole (10 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
-
Animal Model:Male Listar hooded rats[1]
-
Dosage:0.05, 0.5, 1 mg/kg
-
Administration:i.p.; 30 min before the session
-
Result:Reduced cocaine-seeking behaviour before the first infusion of cocaine, in a dose-dependent manner, at doses similar to those at which BP 897 produced its responses on rotations and c-fos expression.
化学情報
-
CAS 番号 192384-87-5
-
性状 Solid
-
分子量 417.54
-
分子式 C26H31N3O2
-
Color White to off-white
-
SMILES
COC1=C(N2CCN(CCCCNC(C3=CC4=C(C=CC=C4)C=C3)=O)CC2)C=CC=C1
-
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 : 50 mg/mL (119.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.99 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal 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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
-
データシート (272 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 | 2.3950 mL | 11.9749 mL | 23.9498 mL | 59.8745 mL |
| 5 mM | 0.4790 mL | 2.3950 mL | 4.7900 mL | 11.9749 mL | |
| 10 mM | 0.2395 mL | 1.1975 mL | 2.3950 mL | 5.9875 mL | |
| 15 mM | 0.1597 mL | 0.7983 mL | 1.5967 mL | 3.9916 mL | |
| 20 mM | 0.1197 mL | 0.5987 mL | 1.1975 mL | 2.9937 mL | |
| 25 mM | 0.0958 mL | 0.4790 mL | 0.9580 mL | 2.3950 mL | |
| 30 mM | 0.0798 mL | 0.3992 mL | 0.7983 mL | 1.9958 mL | |
| 40 mM | 0.0599 mL | 0.2994 mL | 0.5987 mL | 1.4969 mL | |
| 50 mM | 0.0479 mL | 0.2395 mL | 0.4790 mL | 1.1975 mL | |
| 60 mM | 0.0399 mL | 0.1996 mL | 0.3992 mL | 0.9979 mL | |
| 80 mM | 0.0299 mL | 0.1497 mL | 0.2994 mL | 0.7484 mL | |
| 100 mM | 0.0239 mL | 0.1197 mL | 0.2395 mL | 0.5987 mL |