Nelociguat (BAY60-4552)
(Synonyms: N-[4,6-二氨基-2-[1-[(2-氟苯基)甲基]-1H-吡唑并[3,4-B]吡啶-3-基]-5-嘧啶]-氨基甲酸甲酯,BAY60-4552) 目录号 : GC32493
A stimulator of soluble guanylate cyclase and an active metabolite of riociguat
Cas No.:625115-52-8
Sample solution is provided at 25 µL, 10mM.
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Nelociguat is a stimulator of soluble guanylate cyclase (sGC) and an active metabolite of riociguat .1,2 It is formed from riociguat by the cytochrome P450 (CYP) isoform CYP1A1.3 Nelociguat increases phosphorylation of the protein kinase G (PKG) substrate vasodilator-stimulator protein (VASP) in isolated rat aortic smooth muscle cells (EC50 = 353 nM).1 It induces vasodilation in rat aortic rings (EC50 = 75 nM). Nelociguat (3 mg/kg) decreases urine output and cardiac hypertrophy, as well as improves survival, in spontaneously hypertensive stroke-prone rats fed a high-salt high-fat diet. It improves erectile responses to electrical stimulation of the cavernous nerve in a rat model of cavernous nerve crush injury when administered at doses of 0.03 and 0.3 mg/kg.2
1.Costell, M.H., Ancellin, N., Bernard, R.E., et al.Comparison of soluble guanylate cyclase stimulators and activators in models of cardiovascular disease associated with oxidative stressFront. Pharmacol.3128(2012) 2.Oudot, A., Behr-Roussel, D., Poirier, S., et al.Combination of BAY 60-4552 and vardenafil exerts proerectile facilitator effects in rats with cavernous nerve injury: A proof of concept study for the treatment of phosphodiesterase type 5 inhibitor failureEur. Urol.60(5)1020-1026(2011) 3.Hlo?ek, T., ?tícha, M., Bursová, M., et al.Sensitive CE-MS method for monitoring of riociguat and desmethylriociguat levels in human serumElectrophoresis41(18-19)1564-1567(2020)
Animal experiment: | Rats: Rats are orally gavaged with vehicle (0.5% HPMC, 5% DMSO, and 0.1% Tween 80; 10 mL/kg; n=14), GSK2181236A (0.1 or 1.0 mg/kg; n=11-14), or BAY 60-4552 (0.3 or 3.0 mg/kg; n=10-12) 2 h prior to ischemia. Blood is collected at the initiation of ischemia and after 24 h reperfusion. Plasma is obtained for analysis[1]. |
References: [1]. Costell MH, et al. Comparison of soluble guanylate cyclase stimulators and activators in models of cardiovascular disease associated with oxidative stress. Front Pharmacol. 2012 Jul 5;3:128. | |
| Cas No. | 625115-52-8 | SDF | |
| 别名 | N-[4,6-二氨基-2-[1-[(2-氟苯基)甲基]-1H-吡唑并[3,4-B]吡啶-3-基]-5-嘧啶]-氨基甲酸甲酯,BAY60-4552 | ||
| Canonical SMILES | O=C(OC)NC1=C(N)N=C(C2=NN(CC3=CC=CC=C3F)C4=NC=CC=C42)N=C1N | ||
| 分子式 | C19H17FN8O2 | 分子量 | 408.39 |
| 溶解度 | DMSO : 105 mg/mL (257.11 mM) | 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 | 2.4486 mL | 12.2432 mL | 24.4864 mL |
| 5 mM | 0.4897 mL | 2.4486 mL | 4.8973 mL |
| 10 mM | 0.2449 mL | 1.2243 mL | 2.4486 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet