Sparsentan (RE-021)
(Synonyms: 4'-[(2-丁基-4-氧代-1,3-二氮杂螺[4.4]壬-1-烯-3-基)甲基]-N-(4,5-二甲基-3-异恶唑基)-2'-(乙氧基甲基)-[1,1'-联苯]-2-磺酰胺,RE-021; DARA-a) 目录号 : GC32479
A dual antagonist of AT1 and ETA
Cas No.:254740-64-2
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');)
;)
Sparsentan is a dual antagonist of angiotensin II type 1 (AT1) and endothelin receptor type A (ETA; Kis = 0.8 and 9.3 nM, respectively, for the human receptors).1 It is selective for these receptors over AT2 and ETB receptors (Kis = >10 ?M for both). Sparsentan inhibits angiotensin II-induced pressor responses in conscious normotensive rats (ED50 = 3.6 ?mol/kg, p.o). It reduces mean arterial pressure in spontaneously hypertensive rats when administered orally at doses of 10, 30, or 100 ?mol/kg per day. Dietary administration of sparsentan (1,800 ppm) reduces albuminuria and inhibits development of glomerulosclerosis in the gddY mouse model of IgA nephropathy.2
1.Murugesan, N., Gu, Z., Fadnis, L., et al.Dual angiotensin II and endothelin A receptor antagonists: Synthesis of 2'-substituted N-3-isoxazolyl biphenylsulfonamides with improved potency and pharmacokineticsJ. Med. Chem.48(1)171-179(2005) 2.Nagasawa, H., Suzuki, H., Jenkinson, C., et al.The dual endothelin ETA and angiotensin AT1 receptor blocker sparsentan protects against the development of albuminuria and glomerulosclerosis in the gddY mouse model of IgANephrol. Dial. Transplant.35(Suppl. 3)P0348(2020)
Animal experiment: | Rats: Rats are gavaged with vehicle, and immediately thereafter the first bolus (intravenous) iv injection of angiotensin II served as the control pressor response. Irbesartan (30 µmol/kg) and Sparsentan (30 µmol/kg) are given by oral gavage (po), and the rats are re-challenged with angiotensin II at various intervals up to 240 min. There are 6-8 rats per drug dose. The difference between the maximum blood pressure increase before and after drug is reported as the percent (%) inhibition of the angiotensin II pressor effect[1]. |
References: [1]. Murugesan N, et al. Dual angiotensin II and endothelin A receptor antagonists: synthesis of 2'-substituted N-3-isoxazolyl biphenylsulfonamides with improved potency and pharmacokinetics. J Med Chem. 2005 Jan 13;48(1):171-9. | |
| Cas No. | 254740-64-2 | SDF | |
| 别名 | 4'-[(2-丁基-4-氧代-1,3-二氮杂螺[4.4]壬-1-烯-3-基)甲基]-N-(4,5-二甲基-3-异恶唑基)-2'-(乙氧基甲基)-[1,1'-联苯]-2-磺酰胺,RE-021; DARA-a | ||
| Canonical SMILES | O=S(C1=CC=CC=C1C2=CC=C(CN3C(CCCC)=NC4(CCCC4)C3=O)C=C2COCC)(NC5=NOC(C)=C5C)=O | ||
| 分子式 | C32H40N4O5S | 分子量 | 592.75 |
| 溶解度 | DMSO: 250 mg/mL (421.76 mM); Water: < 0.1 mg/mL (insoluble) | 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 | 1.6871 mL | 8.4353 mL | 16.8705 mL |
| 5 mM | 0.3374 mL | 1.6871 mL | 3.3741 mL |
| 10 mM | 0.1687 mL | 0.8435 mL | 1.6871 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: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet