BW 245C
目录号 : GC14212A selective DP1 receptor agonist
Cas No.:72814-32-5
Sample solution is provided at 25 µL, 10mM.
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Target: DP1 receptor
IC50: 2.5 nM
Ki: 0.9 nM
BW 245C is a kind of prostaglandin analogue with stable chemical properties which functions as a potent inhibitor of platelet aggregation. BW 245C could selectively active the DP1 receptor, and inhibit [3H]-PGD2 binding to isolated human platelet membranes, with the Ki value of 0.9 nM [1].
In Vitro: BW 245C could inhibit the aggregation of human and rat platelets induced by ADP in a dose dependent manner, with the IC50 values of 8.7 nM and 9.9 nM, respectively [1]. Besides, in HEK293 cells stably expressing the hDP receptor, BW 245C could significantly increase cAMP production, with the EC50 value of 0.7 nM [2].
In Vivo: In spontaneously hypertensive rats, intravenous bolus injection with BW 245C at the dose of 250 μg/kg could reduce the systolic and diastolic blood pressure by 23% and 34%, respectively [1].
Clinical trial: In four healthy male volunteers, intravenous injection of BW 245C (1, 2 and 4 ng kg-1 min-1) exerted a progressive increase in heart rate and pulse pressure [3].
References:
[1] Town H C, Casalsstenzel J, Schillinger E, et al. Pharmacological and cardiovascular properties of a hydantoin derivative, BW 245 C, with high affinity and selectivity for PGD2 receptors[J]. Prostaglandins, 1983, 25(1): 13-28.
[2] Boie Y, Sawyer N, Slipetz D, et al. MOLECULAR CLONING AND CHARACTERIZATION OF THE HUMAN PROSTANOID DP RECEPTOR[J]. Journal of Biological Chemistry, 1995, 270(32): 18910-18916.
[3] Orchard M A, Ritter J M, Shepherd G L, et al. Cardiovascular and platelet effects in man of BW 245C, a stable mimic of epoprostenol (PGI2)[J]. British journal of clinical pharmacology, 1983, 15(5): 509-511.
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Animal experiment: |
The mice are untreated or given an i.p. injection of the vehicle (1% DMSO) or 0.2-mg/kg BW245C. Thirty minutes after the injection, the mice are anesthetized and placed on a thermoregulated pad to maintain body temperature, and 3 mm of the tail tip is excised. The tail is immediately dipped in warm PBS (37.0±0.5°C) and time to visible cessation of bleeding is recorded. |
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References: [1]. Ahmad AS, et al. PGD2 DP1 receptor stimulation following stroke ameliorates cerebral blood flow and outcomes. Neuroscience. 2014 Oct 24;279:260-8. |
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| Cas No. | 72814-32-5 | SDF | |
| 化学名 | (4S)-(3-[(3R,S)-3-cyclohexyl-3-hydroxypropyl]-2,5-dioxo)-4-imidazolidineheptanoic acid | ||
| Canonical SMILES | O=C(N1[H])[C@H](CCCCCCC(O)=O)N(CCC(O)C2CCCCC2)C1=O | ||
| 分子式 | C19H32N2O5 | 分子量 | 368.5 |
| 溶解度 | ≤50mg/ml in ethanol;50mg/ml in DMSO;50mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7137 mL | 13.5685 mL | 27.137 mL |
| 5 mM | 0.5427 mL | 2.7137 mL | 5.4274 mL |
| 10 mM | 0.2714 mL | 1.3569 mL | 2.7137 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet