Mozavaptan
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Cat.No：IM2510 Solarbio
CAS：137975-06-5
Storage：Powder:2-8℃，2 years
Purity：≥98%
Appearance：White to off-white Solid
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> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > GPCR & G Protein > Mozavaptan
Product Information
| CAS | 137975-06-5 |
| Name | Mozavaptan |
| Molecular Formula | C27H29N3O2 |
| Molecular Weight | 427.54 |
| Solubility | Soluble in DMSO ≥0.1mg/mL(Need ultrasonic) |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years |
| EC | EINECS 1312995-182-4 |
| MDL | MFCD00908918 |
| SMILES | CC1=CC=CC=C1C(NC2=CC=C(C(N3C(C=CC=C4)=C4C(N(C)C)CCC3)=O)C=C2)=O |
| Target Point | Vasopressin Receptor |
| Passage | GPCR & G Protein |
| Background | Mozavaptan is a vasopressin V2 receptor antagonist. |
| Biological Activity | Mozavaptan (OPC31260)是有口服活性的非肽阴道加压素(vasopressin)V2受体拮抗剂，其IC50值为14nM。[1] |
| IC50 | 14nM(vasopressin receptor)[1] |
| In Vitro | Mozavaptan引起[3H] - 精氨酸加压素(AVP)与V1和V2受体结合的竞争性置换，IC50值分别为1.2μM和14nM。在mozavaptan存在下，大鼠肝脏和肾脏中[3H] -AVP的Kd显著降低(肝脏中Kd = 1.1 nM，肾脏中Kd = 1.38 nM)[1]。 |
| In Vivo | 莫扎伐坦以10至100μg/ kg的剂量静脉注射，以剂量依赖性方式抑制外源施用的精氨酸加压素在水负荷的酒精麻醉大鼠中的抗利尿作用。 Mozavaptan没有发挥抗利尿活性，表明它不是部分V2受体激动剂。 Mozavaptan在正常清醒大鼠中以1至30 mg / kg的剂量口服给药后剂量依赖性地增加尿流量并降低尿渗透压[1]。 |
| Animal Experiment | 大鼠：将Mozavaptan以10mM的浓度溶解在DMSO中，并用测定缓冲液稀释。使用雌性Brattleboro大鼠，其为下丘脑尿崩症纯合子并且重量在180和280g之间。 Mozavaptan(30mg / kg)和载体(5％阿拉伯树胶)以2mL / kg的体积口服给药，d(CH2)5Tyr(Et)VAVP(10pgkg-1)以1mL / kg的体积给药。公斤。用代谢笼收集自发排尿的尿液6小时。在研究之前和研究期间，大鼠随意接受水和食物[1]。 |
| Kinase Experiment | 为了确定结合动力学常数，将肝脏或肾脏质膜与增加浓度的[3H] -AVP一起孵育，有或没有过量(1μM)未标记的AVP，以获得饱和曲线。为了研究mozavaptan是竞争性还是非竞争性地相互作用，在不存在和存在mozavaptan时检测[3H] -AVP的饱和结合，其中肝膜中浓度为0.3μM和1μM，肾膜中浓度为3nM，10nM。根据Scatchard的方法绘制饱和度曲线的数据，并通过回归分析拟合[1]。 |
| Data Literature Source | [1]. Yamamura Y，et al. Characterization of a novel aquaretic agent，OPC-31260，as an orally effective，nonpeptide vasopressin V2 receptor antagonist. Br J Pharmacol. 1992 Apr;105(4):787-91 |
| Unit | Bottle |
| Specification | 5mg 10mg |
是vasopressin V2受体拮抗剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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1. The products are all for scientific research use only. Do not use it for medical, clinical diagnosis or treatment, food and cosmetics, etc. Do not store them in ordinary residential areas.
2. For your safety and health, please wear laboratory clothes, disposable gloves and masks.
3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
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