CFM 1571 hydrochloride
目录号 : GC17431
CFM 1571 hydrochloride 是一氧化氮受体、可溶性鸟苷酸环化酶 (sGC) 的刺激剂，EC50 和 IC50 分别为 5.49 μM 和 2.84 μM。
Cas No.:1215548-30-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
IC50: 2.84 μM for platelet
Soluble guanylate cyclase (sGC) is a key signal-transduction enzyme activated by nitric oxide (NO). Impaired bioavailability and/or responsiveness to endogenous NO has been implicated in the pathogenesis of cardiovascular and other diseases. CFM 1571 is a activator of the nitric oxide receptor, soluble guanylate cyclase.
In vitro: CFM 1571 demonstrated potent activation of soluble guanylate cyclase and potent inhibition of platelet aggregation. CFM 1571 also showed enzyme activity similar to benzydamine. CFM 1571 was additionally assayed against the NOS isoforms, and minimal inhibition was observed with iNOS (25%) and nNOS (17%). Furthermore CFM 1571 shows no significant activity at any of the other enzymes studied [1].
In vivo: Pharmacokinetic studies in rats showed that compound CFM 1571 exhibits modest oral bioavailability (12%). Furthermore 32 has an excellent selectivity profile notably showing no significant inhibition of phosphodiesterases or nitric oxide synthases [1].
Clinical trial: Up to now, CFM 1571 is still in the preclinical development stage.
Reference:
[1] Selwood DL, Brummell DG, Budworth J, Burtin GE, Campbell RO, Chana SS, Charles IG, Fernandez PA, Glen RC, Goggin MC, Hobbs AJ, Kling MR, Liu Q, Madge DJ, Meillerais S, Powell KL, Reynolds K, Spacey GD, Stables JN, Tatlock MA, Wheeler KA, Wishart G, Woo CK. Synthesis and biological evaluation of novel pyrazoles and indazoles as activators of the nitric oxide receptor, soluble guanylate cyclase. J Med Chem. 2001 Jan 4;44(1):78-93.
| Cas No. | 1215548-30-3 | SDF | |
| 化学名 | 1-benzyl-3-(3-(dimethylamino)propoxy)-N-(4-methoxyphenyl)-1H-pyrazole-5-carboxamide hydrochloride | ||
| Canonical SMILES | CN(CCCOC(C=C1C(NC2=CC=C(OC)C=C2)=O)=NN1CC3=CC=CC=C3)C.Cl | ||
| 分子式 | C23H28N4O3.HCl | 分子量 | 444.95 |
| 溶解度 | DMSO : 100 mg/mL (224.74 mM; Need ultrasonic) | 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 | 2.2474 mL | 11.2372 mL | 22.4744 mL |
| 5 mM | 0.4495 mL | 2.2474 mL | 4.4949 mL |
| 10 mM | 0.2247 mL | 1.1237 mL | 2.2474 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。