| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| S654911-1ml |
1ml |
期货  |
|
| 规格或纯度 | 10mM in DMSO |
|---|---|
| 英文名称 | SRX246 |
| 生化机理 | SRX246 是一种强效、中枢神经系统穿透性、高选择性、口服生物可用性的血管紧张素 1a（V1a）受体拮抗剂（对人类 V1a 的 K i =0.3 nM）。SRX246 与 V1b 和 V2 受体没有相互作用。SRX246 与其他 64 种受体的结合也可以忽略不计。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 产品介绍 |
SRX246 is a potent, CNS-penetrant, highly selective, orally bioavailable Vasotocin 1a (V1a) receptor antagonist ( K i =0.3 nM for human V1a). SRX246 has no interaction at V1b and V2 receptors. SRX246 also displays negligible binding at 64 others receptors classes, including 35 G-proteincoupled receptors. SRX246 can be used for treatment of stress-related disorders In Vivo SRX246 (2 mg/kg; i.v.) treatment shows that the C max , AUC 0-∞ and t 1/2 values are 953 ng/mL, 1141 ng ▪h/mL, and 6.02 hours, respectively, in plasma pharmacokinetics. Following an oral administration (dose 20 mg/kg), The C max , AUC 0-∞ and t 1/2 values are 98.4 ng/mL, 624 ng ▪h/mL and 2.38 hours, respectively . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Sprague-Dawley rats Dosage: 2 mg/kg (20 mg/kg for p.o.) Administration: i.v. (Pharmacokinetic Analysis) Result: Following i.v. administration, the plasma concentration declined steadily with a half-life (t 1/2 ) of 6 hours. The C max and AUC 0-∞ values are 953 ng/mL, 1141 ng ▪h/mL, 6.02 hours. Following an oral administration, the C max , AUC 0-∞ and t 1/2 values 98.4 ng/mL, 624 ng ▪h/mL and 2.38 hours, respectively. IC50& Target:Ki: 0.3 nM (human Vasotocin 1a receptor) |
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | C[C@H](C1=CC=CC=C1)NC(=O)[C@@H](CC(=O)N2CCC(CC2)N3CCCCC3)N4[C@@H]([C@@H](C4=O)N5[C@H](COC5=O)C6=CC=CC=C6)/C=C/C7=CC=CC=C7 |
| 关联CAS | 512784-93-9 |
| PubChem CID | 44428550 |
| MeSH Entry Terms | SRX246 |
| 分子量 | 703.87 |
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