OPC-28326
目录号 : GC32543
OPC-28326是一种外周血管扩张药，同时为α2-adrenergicreceptor的拮抗剂，对α2A-，α2B-和α2C肾上腺素受体的Ki值分别为2040，285和55 nM。
Cas No.:167626-17-7
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
OPC-28326 is a selective peripheral vasodilator and an angatonist of α2-adrenergic receptor, with Ki of 2040, 285, and 55 nM for α2A-, α2B- and α2C-adrenoceptors, respectively.
OPC-28326 enhances endothelial tube formation and promotes microvessel growth. OPC-28326 induces phosphorylation of eNOS and Akt in HAECs in a dose dependent-manner, while it does not affect total amounts of eNOS and Akt[1]. OPC-28326 (1-100 μM) and yohimbine (10-1000 nM) causes a rightward shift in the concentration-response curve of clonidine[2].
OPC-28326 augments blood flow recovery in murine hindlimb ischemia. OPC-28326 significantly increases the number of histologically detectable capillaries in the ischemic leg. OPC-28326 has no beneficial effects on blood flow recovery in eNOS-/- mice[1]. OPC-28326 (3-30 mg/kg, i.v.) and yohimbine causes dose-dependent rightward shift in the pressor dose-response curve induced by B-HT 920. OPC-28326 does not affect on the mydriasis in rats[2].
[1]. Sumi M, et al. OPC-28326, a selective femoral arterial vasodilator, augments ischemia induced angiogenesis. Biomed Pharmacother. 2007 May;61(4):209-15. Epub 2006 Dec 28. [2]. Orito K, et al. alpha(2)-adrenoceptor antagonist properties of OPC-28326, a novel selective peripheral vasodilator. Br J Pharmacol. 2001 Oct;134(4):763-70.
Animal experiment: | Unilateral hindlimb ischemia is induced in 30- to 35-week-old male mice by resecting the right femoral and saphenous arteries. The mice are fed on regular chow (Ctrl), chow containing 0.02% (OPC(L)) or 0.05% (OPC(H)) OPC-28326, starting one week before the surgery (n = 10 for each group). Hindlimb blood perfusion is measured using a laser Doppler perfusion imager (LDPI) system. Excess hairs are removed from the limbs using depilatory cream before imaging, and mice are placed on a heating plate at 40°C. To avoid the influence of ambient light and temperature, the results are expressed as the ratio of perfusion in the right (ischemic) versus left (untreated) limb. The thigh muscles are harvested at 4 weeks and stained for CD31 (clone MEC13.1) to detect endothelial cells. Capillaries are identified by positive staining for CD31 and their morphology. Ten different fields from each tissue preparation are randomly selected and capillaries are counted. Capillary density is expressed as the number of capillaries per square millimeter. |
References: [1]. Sumi M, et al. OPC-28326, a selective femoral arterial vasodilator, augments ischemia induced angiogenesis. Biomed Pharmacother. 2007 May;61(4):209-15. Epub 2006 Dec 28. | |
| Cas No. | 167626-17-7 | SDF | |
| Canonical SMILES | CCC(NC1=C(C)C=C(C(N2CCC(N(C)CCC3=CC=CC=C3)CC2)=O)C=C1C)=O | ||
| 分子式 | C26H35N3O2 | 分子量 | 421.58 |
| 溶解度 | Soluble in DMSO | 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.372 mL | 11.8601 mL | 23.7203 mL |
| 5 mM | 0.4744 mL | 2.372 mL | 4.7441 mL |
| 10 mM | 0.2372 mL | 1.186 mL | 2.372 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